Gene:
UGT1A1
UDP glucuronosyltransferase 1 family, polypeptide A1

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for irinotecan and UGT1A1

Summary

Reduce the starting dose of irinotecan for UGT1A1*28 homozygous patients receiving more than 250 mg/m^2.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for irinotecan based on UGT1A1 genotype (PMID:21412232). They recommend reducing the dose for *28 homozygous patients receiving more than 250 mg/m^2.

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
*1/*28 None. Published controlled studies of moderate quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints.. Clinical effect (S): death; arrhythmia; unanticipated myelosuppression.
*28/*28 Dose >250mg/m^2: reduce initial dose by 30%. Increase dose in response to neutrophil count. Dose <=250mg/m^2: no dose adjustment. Published controlled studies of moderate quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Clinical effect (S): Failure of lifesaving therapy e.g. anticipated myelosuppression; prevention of breast cancer relapse; arrhythmia; neutropenia < 0.5x10^9/l; leucopenia < 1.0x10^9/l; thrombocytopenia < 25x10^9/l; life-threatening complications from diarrhea.

PharmGKB gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.



last updated 10/25/2013

FDA Label for indacaterol and UGT1A1

This label is on the FDA Biomarker List
Informative PGx

Summary

Steady-state AUC and Cmax of indacaterol were 1.2-fold higher in patients with the (TA)7, (TA)7 (*28) genotype than in patients with the (TA)6, (TA)6 genotype, suggesting no relevant effect of UGT1A1 genotype of indacaterol exposure

There's more of this label. Read more.


last updated 10/25/2013

FDA Label for irinotecan and UGT1A1

This label is on the FDA Biomarker List
Actionable PGx

Summary

Individuals who are homozygous for the UGT1A1*28 allele (UGT1A1 7/7 genotype) are at increased risk for neutropenia following initiation of CAMPTOSAR treatment. A reduction in the starting dose by at least one level of CAMPTOSAR should be considered for patients known to be homozygous for the UGT1A1*28 allele

There's more of this label. Read more.


last updated 10/25/2013

FDA Label for nilotinib and ABL1, BCR, UGT1A1

This label is on the FDA Biomarker List
Genetic testing required

Summary

Nilotinib is indicated for use in patients diagnosed with Philadelphia chromosome positive (presence of a BCR-ABL1 gene fusion) chronic myeloid leukemia, due to its mechanism of action. Individuals with the UGT1A1*28 genotype (TA)7/(TA)7 (rs8175347) are at an increased risk of hyperbilirubinemia when taking nilotinib (testing is not required for UGT1A1).

There's more of this label. Read more.


last updated 02/15/2014

FDA Label for pazopanib and UGT1A1

This label is on the FDA Biomarker List
Actionable PGx

Summary

The drug label for pazopanib (VOTRIENT) states that patients with the UGT1A1 (TA)7/(TA)7 genotype (UGT1A1*28/*28) have an increased incidence of hyperbilirubinemia when taking pazopanib, as compared to those with the (TA)6/(TA)7 or (TA)6/(TA)6 genotype.

There's more of this label. Read more.



last updated 10/25/2013

European Medicines Agency (EMA) Label for erlotinib and EGFR, UGT1A1

Genetic testing required

Summary

The EMA European Public Assessment Report (EPAR) requires testing tumours for EGFR mutations in patients with non-small cell lung cancer prior to treatment with erlotinib and recommends using a well-validated method of testing. The drug should be used with caution in patients with low expression of UGT1A1 or Gilbert's disease (caused by genetic variants in UGT1A1 gene), due to the inhibitory effects of erlotinib on glucuronidation by UGT1A1 (UGT1A1 genetic testing is not required).

There's more of this label. Read more.


last updated 06/05/2014

European Medicines Agency (EMA) Label for pazopanib and UGT1A1

Actionable PGx

Summary

The EMA European Public Assessment Report (EPAR) for pazopanib (Votrient) states that the drug may cause mild hyperbilirubinemia in patients with Gilbert's syndrome (associated with reduced UGT1A1 activity and in some cases is caused by an underlying UGT1A1*28 variant) because it is an inhibitor of UGT1A1. It also states that pazopanib may have a greater effect on irinotecan active metabolite exposure in patients with the UGT1A1*28 variant.

There's more of this label. Read more.


last updated 06/26/2014

European Medicines Agency (EMA) Label for regorafenib and KRAS, UGT1A1

Informative PGx

Summary

The EMA European Public Assessment Report (EPAR) for regorafenib (Stivarga) is indicated in adult patients with metastatic colorectal cancer who have been previously treated with or are not considered candidates for other available therapies, including patients with KRAS mutant tumors, though physicians are recommended to carefully evaluate benefits and risks when prescribing regorafenib in patients with KRAS mutant tumours. It potentially blocks targets multiple protein kinases. It is also an inhibitor of UGT1A1 and therefore hyperbilirubinemia may occur in patients with Gilbert's syndrome (can be caused by genetic variants in the UGT1A1 gene).

There's more of this label. Read more.


PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the table.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Related Drugs?
UGT1A1 (Camptosar/Irinotecan) GenotypR UGT1A1 UGT1A1*28
Invader UGT1A1 Molecular Assay UGT1A1 UGT1A1*28

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page on the appropriate tab.

Links in the "Drugs" column lead to PharmGKB Drug Pages.

Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA *1 N/A N/A N/A
No VIP available No VIP available VA *6 N/A N/A N/A
No VIP available No VIP available VA *28 N/A N/A N/A
No VIP available No VIP available VA *36 N/A N/A N/A
No VIP available No VIP available VA *37 N/A N/A N/A
No VIP available No VIP available VA *60 N/A N/A N/A
No VIP available No VIP available VA *91 N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs10929302 -1791C>T, 172393G>A, 234665782G>A, 61-9898G>A, 612041G>A, 856-9898G>A, 862-9898G>A, 868-9898G>A, UGT1A1*93, UGT1A1:-3156G>A, UGT1A1:G-3156A
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs2003569 -997G>A, 174548G>A, 234667937G>A, 61-7743G>A, 614196G>A, 856-7743G>A, 862-7743G>A, 868-7743G>A, UGT1A1(-997)G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs34993780 1447T>A, 1447T>G, 1453T>A, 1453T>G, 1456T>A, 1456T>G, 1459T>A, 1459T>G, 187670T>A, 187670T>G, 234681059T>A, 234681059T>G, 627318T>A, 627318T>G, 652T>A, 652T>G, Tyr218Asn, Tyr218Asp, Tyr483Asn, Tyr483Asp, Tyr485Asn, Tyr485Asp, Tyr486Asn, Tyr486Asp, Tyr487Asn, Tyr487Asp
T > G
T > A
Missense
Tyr483Asp
No VIP available No Clinical Annotations available VA
rs35350960 176230C>A, 176230C>T, 234669619C>A, 234669619C>T, 61-6061C>A, 61-6061C>T, 615878C>A, 615878C>T, 686C>A, 686C>T, 856-6061C>A, 856-6061C>T, 862-6061C>A, 862-6061C>T, 868-6061C>A, 868-6061C>T, Pro229Gln, Pro229Leu, UGT1A1*27, UGT1A1:Pro229Glu
C > T
C > A
Intronic
Pro229Gln
No VIP available No Clinical Annotations available VA
rs3755319 -1352A>C, 174193A>C, 234667582A>C, 61-8098A>C, 613841A>C, 856-8098A>C, 862-8098A>C, 868-8098A>C, UGT1A1(-1352)A>C
A > C
Intronic
No VIP available No Clinical Annotations available VA
rs3771342 179274G>T, 234672663G>T, 61-3017G>T, 618922G>T, 856-3017G>T, 862-3017G>T, 864+2866G>T, 868-3017G>T
G > T
Intronic
No VIP available CA VA
rs4124874 -1668A>C, 172270T>G, 234665659T>G, 61-10021T>G, 611918T>G, 856-10021T>G, 862-10021T>G, 868-10021T>G, UGT1A1*60, UGT1A1:-3263T>G, UGT1A1:-3279T>G
T > G
5' Flanking
rs4148323 175755G>A, 211G>A, 234669144G>A, 61-6536G>A, 615403G>A, 856-6536G>A, 862-6536G>A, 868-6536G>A, Gly71Arg, UGT1A1*6, UGT1A1: G71R, UGT1A1:211G>A, UGT1A1:G211A, UGT1A1:Gly71Arg
G > A
Intronic
Gly71Arg
No VIP available No Clinical Annotations available VA
rs72551344 176242T>G, 234669631T>G, 61-6049T>G, 615890T>G, 698T>G, 856-6049T>G, 862-6049T>G, 868-6049T>G, Leu233Arg
T > G
Intronic
Leu233Arg
rs8175347 233760235_233760236TA[5][6][7][8], 5-TA insertion in promoter, 7-TA insertion in promoter, 8-TA insertion in promoter, UGT1A1*28, UGT1A1*36, UGT1A1*37, microsatellite, short tandem repeat
(TA)6 > (TA)8
(TA)6 > (TA)5
(TA)6 > (TA)7
Not Available
No VIP available CA VA
rs887829 -364C>T, 175181C>T, 234668570C>T, 61-7110C>T, 614829C>T, 856-7110C>T, 862-7110C>T, 868-7110C>T, UGT1A1(-364)T>C
C > T
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138

Overview

Alternate Names:  None
Alternate Symbols:  UGT1A
PharmGKB Accession Id: PA420

Details

Cytogenetic Location: chr2 : q37.1 - q37.1
GP mRNA Boundary: chr2 : 234668919 - 234681945
GP Gene Boundary: chr2 : 234658919 - 234684945
Strand: plus
The mRNA boundaries are calculated using the gene's default feature set from NCBI, mapped onto the UCSC Golden Path. PharmGKB sets gene boundaries by expanding the mRNA boundaries by no less than 10,000 bases upstream (5') and 3,000 bases downstream (3') to allow for potential regulatory regions.

The uridine diphosphate glucuronosyltransferase (UGT) enzymes are a superfamily of enzymes responsible for the glucuronidation of target substrates. The transfer of glucuronic acid renders xenobiotics and other endogenous compounds water soluble, allowing for their biliary or renal elimination [Article:18518849]. The UGT family is responsible for the glucuronidation of hundreds of compounds, including hormones, flavonoids and environmental mutagens [Article:18518849]. Most of the members of the UGT family are expressed in the liver, as well as in other types of tissues, such as intestinal, stomach or breast tissue. A few members are expressed only extrahepatically, such as UGT1A7, UGT1A8, UGT1A10 and UGT2A1 [Article:12893990]. Four families exist within the UGT superfamily: UGT1A, UGT2, UGT3 and UGT8 [Article:16141793]. UGT2 is further divided into two subfamilies, UGT2A and UGT2B, both of which are present on chromosome 4 [Article:12893990]. UGT2A enzymes are involved in the glucuronidation of compounds such as phenolic odorants and polycyclic aromatic hydrocarbon metabolites, though limited studies have been done on this subfamily [Article:23086198]; UGT2B proteins are mainly responsible for the metabolism of steroids [Article:11159850]. The roles of UGT3 and UGT8 family members have not been well characterized [Article:16141793]. The UGT1A family is located on chromosome 2q37, and the members of this group glucuronidate a large variety of compounds. Pharmaceutical drugs are also a common substrate of the UGT family [Article:18518849], which makes the enzymes in this group relevant to pharmacogenetic research.

The UGT1A gene locus

The UGT1A gene locus enables the transcription of nine unique enzymes, UGT1A1, and UGT1A3 through UGT1A10 [Articles:8467709, 18518849]. This occurs by exon sharing, in which one of nine unique exon 1 sequences at the 5' end of the gene is combined with the common exons 2-4 and 5a at the 3' end, forming individual UGT1A transcripts [Article:11434514] (Figure 1). Alternatively spliced isoforms of UGT1A exist, and are formed when exon 5b (seen in the common exon region) is used instead of, or in addition to, exon 5a [Article:18004212]. These alternative isoforms are known as isoforms 2 or UGT1As_i2, and are enzymatically inactive [Articles:18004212, 19997083]. Additionally, four UGT1A pseudogenes exist: UGT1A2p, 11p, 12p and 13p [Articles:11434514, 15179404]. These pseudogenes can be seen in Figure 1, along with the location of two principal UGT1A1 pharmacogenetic variants, *28 and *6, both of which are discussed in detail further on within this summary.

Figure 1. A graphic representation of the human UGT1A locus (not drawn to scale). (A) The locus spans approximately 200 kbp and contains multiple alternative first exons, which together constitute exon 1. Each unique first exon has its own promoter site. The individual exons for each isoform are combined with the common exons 2-4 and 5a by splicing out any intervening sequence. Exons 2-4 and 5a are therefore present in every UGT1A isoform. However, alternatively spliced UGT1A isoforms do exist, and are known as isoforms 2 or UGT1As_i2; these are created when exon 5b is used instead of, or in addition to, exon 5a. An example of the formation of UGT1A4 mRNA is also shown. In (A) the promoter for UGT1A4 can be seen upstream of the gene, (B) shows the pre-mRNA formed after transcription, and (C) shows the final UGT1A4 mRNA transcript after splicing. Though splicing occurring for common exons 2-5a has not been shown in this figure, it is important to note the absence of exon 5b in (C); this alternative exon has been spliced out in order to create the classical form of UGT1A4. The figure also shows the location of two important UGT1A1 pharmacogenetic variants, *28 and *6, both of which are discussed in detail further on. Adapted from [Articles:18491077, 19794410].

UGT1A1

UGT1A1 function

One of the transcripts encoded by the UGT1A locus is UGT1A1, which is at the furthest 3' end of the UGT1A exon 1 region. UGT1A1 is expressed hepatically as well as within the colon, intestine and stomach [Articles:10748067, 9765507]. One of the main functions of UGT1A1 lies within the liver, where it is the sole enzyme responsible for the metabolism of bilirubin, the hydrophobic breakdown product of heme catabolism [Articles:8027054, 18518849]. In general, UGT1A enzymes have considerable overlap in substrate specificities [Article:10836148], however no other isozyme can substitute for the bilirubin glucuronidation activity of UGT1A1 [Article:18518849]. Additionally, no effective alternative pathways exist for the detoxification and elimination of bilirubin, excluding that of photoisomeration, a relatively inefficient pathway as compared to UGT1A1 glucuronidation [Article:12891498]. Patients with Crigler-Najjar Type I (CN1) disease (discussed below) act as models for this concept: they are either homozygotes or compound heterozygotes for inactive enzyme variants, and are also incapable of glucuronidating or eliminating bilirubin [Article:15712364].

UGT1A1 variants

Currently, 113 different UGT1A1 variants have been described throughout the gene. These variants can confer reduced or increased activities, as well as inactive or normal enzymatic phenotypes. These individual variants are described as alleles by the UGT nomenclature committee, and denoted by the * symbol followed by a number.

UGT1A1 alleles and their role in disease

Homozygotes or compound heterozygotes for inactive UGT1A1 alleles have a complete absence of bilirubin glucuronidation and removal, leading to a high serum level of unconjugated bilirubin (hyperbilirubinemia), and a serious condition known as Crigler-Najjar Type I (CN1) disease [Article:18518849]. If left untreated, CN1 is invariably fatal [Article:19830808]. The development of hyperbilirubinemia results in kernicterus, or the buildup of bilirubin within brain tissue. This causes irreversible neurological damage, leading to severe disability or death. Intensive phototherapy can keep bilirubin levels in check, but becomes less effective with age, and the only definitive treatment is liver transplantation [Article:12891498].

Crigler-Najjar Type 2 (CN2), also results from mutations within the UGT1A1 gene, but some residual enzymatic activity remains, conferring a milder phenotype [Article:19830808]. This type can be treated successfully with phenobarbital, which induces expression of UGT1A1, allowing for reduction of unconjugated bilirubin to innocuous levels [Articles:4897277, 3306242, 7989595]. Kernicterus may still develop, however, if bilirubin levels are enhanced, such as during sepsis or trauma [Article:19830808].

Gilbert's syndrome represents the least severe of the inherited unconjugated hyperbilirubinemia conditions [Article:11013440], and results from UGT1A1 glucuronidation activity that is approximately 30% of normal [Article:7565971]. Patients with Gilbert's have fluctuating bilirubin levels, which are often within the standard range [Article:7565971]. Illness, stress or fasting can precipitate a rise in bilirubin levels, leading to hyperbilirubinemia, and symptoms such as jaundice or abdominal discomfort. However, these symptoms will typically resolve themselves, and the syndrome is harmless in adults [Article:7565971]. Though the condition is benign in itself, it is an indicator of reduced UGT1A1 activity, and is therefore important to consider in the context of drug toxicity. Gilbert's syndrome can be caused by a variety of genetic changes, but within Caucasian and African American populations it is most commonly attributed to the UGT1A1*28 variant allele (rs8175347) [Article:9653159]. This allele represents seven thymine-adenine (TA) repeats within the promoter region, as opposed to six that characterizes the wild-type allele (UGT1A1*1) [Article:17898154]. These extra repeats impair proper transcription of the gene, resulting in decreased transcriptional activity of the gene by approximately 70% [Articles:7565971, 12181419]. A different allele, UGT1A1*37, has eight TA repeats at this site, and results in reduced promoter activity to levels lower than that of promoters with the UGT1A1*28 allele [Articles:10091406, 9653159]. In contrast, the allele UGT1A1*36 has only five repeats, and is associated with increased promoter activity of the gene and a reduced risk of neonatal hyperbilirubinemia, a common and typically benign condition [Articles:9653159, 10190918]. In Asian populations, the UGT1A1*6 allele is more common [Article:9784835]. This variant results from a glycine to arginine change at position 71 within the coding region (Arg71Gly; 211G>A; rs4148323) [Article:16609363]. Individuals homozygous for this allele have enzymatic activity at 32% of normal, and can present with Gilbert's syndrome [Article:9630669] as well as neonatal hyperbilirubinemia [Article:10353933].

UGT1A1 alleles have also been associated with the development of various cancers. Along with bilirubin and pharmaceuticals, UGT1A1 enzymes have been seen to glucuronidate benzo(α)pyrene-trans-7,8-dihydrodiol, a precursor to the potent carcinogen
benzo(α)pyrene-7,8-dihydrodiol-9,10-epoxide, which is found in charbroiled food, coal tar, and cigarette smoke [Article:11929814]. They have also been noted to glucuronidate estradiol [Article:12386134], as well as 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine (PhIP), another carcinogen present in cooked meat [Article:15986396]. UGT1A1 therefore exhibits a protective effect against benzo(α)pyrene and PhIP-mediated carcinogenicity, and modulates levels of estradiol within the body [Articles:11929814, 12386134, 15986396]. The *28 allele has been shown to increase the risk of developing colorectal and breast cancer across multiple studies in Chinese and Caucasian populations 15111762, 10706110, 22559977. The *6 allele was seen to increase the risk of colorectal cancer in one study in a Chinese cohort [Article:15929176]. Since these alleles result in reduced UGT1A1 activity, any associations seen are potentially due to increased exposure to carcinogens and estradiol [Article:18518849]; increased levels of the latter are associated with the development of breast cancer [Article:21813404]. However, several studies have shown no associations between the *28 allele and risk of breast cancer [Articles:17949292, 11401924], and one showed a decreased risk of breast cancer in *28 carriers [Article:15318931].

There is also evidence suggesting that the UGT1A1*28 allele may offer protection from cardiovascular disease (CVD). Bilirubin is a known antioxidant, and is thought to be capable of preventing plaque formation leading to atherosclerosis [Article:20693308]. Multiple studies have found a link between low bilirubin concentrations and an increased risk of CVD [Article:20562445], though this association may be affected by confounders such as obesity or cholesterol levels [Articles:20562445, 22416852]. Since the *28 allele impairs transcription of the UGT1A1 gene, it is associated with significantly increased bilirubin concentrations, and therefore could be an important biomarker for predicting those at decreased risk of CVD [Article:21411679]. Additionally, testing for associations between the *28 allele and CVD allows for a Mendelian randomization approach, which helps avoid confounding or reverse causation, limitations present in the studies linking bilirubin levels with CVD [Articles:22416852, 22805420]. A 2006 study utilizing the Framingham Heart Study population followed 1780 individuals for 24 years, and found that those with the *28/*28 genotype had one third the risk for cardiovascular disease as compared to those with the *1/*28 or *1/*1 genotypes [Article:17000907]. However, additional studies and meta-analyses [Articles:20562445, 12816916], including one with over 67,000 participants [Article:22805420], have failed to find a link between the *28 allele or bilirubin levels and risk for cardiovascular disease or myocardial infarction. (Note: PMID 22805420 conducted analyses using the rs6742078 variant, shown to be in strong linkage disequilbrium with rs8175347).

UGT1A1 allele frequencies

UGT1A1*28 occurs with a frequency of 0.26 - 0.31 in Caucasians, and 0.42 - 0.56 in African Americans, and only 0.09 - 0.16 in Asian populations [Articles:10591539, 9653159]. UGT1A1*6 has allele frequencies in Japanese, Korean and Chinese populations of 0.13, 0.23 and 0.23, respectively [Article:9784835]. Both UGT1A1*36 and UGT1A1*37 occur almost exclusively in populations of African origin, with estimated allele frequencies of 0.03 - 0.10 and 0.02 - 0.07, respectively [Articles:9653159, 10591539, 15388579].

UGT1A1 Pharmacogenetics

Both the *28 and *6 alleles have been well studied in regard to pharmaceutical toxicities. In particular, both alleles have shown associations with the development of irinotecan toxicities [Articles:20562211, 17728214, 19390945]. Irinotecan is a topoisomerase I inhibitor, and is primarily used to treat colorectal cancer, though it is also used to treat solid tumors within other organs [Article:19852077]. As a pro-drug, irinotecan is converted by carboxylesterases to SN-38, a metabolite which has 100-fold higher anti-tumor activity than its parent compound [Article:1651156]. UGT1A1 is the predominant isoform responsible for the glucuronidation of this toxic metabolite, enabling its eventual excretion. However, in vitro studies show that UGT1A7 and UGT1A9 are also involved in SN-38 glucuronidation [Article:12181437]. Irinotecan has a very narrow therapeutic range, and treatment can lead to a variety of side effects, mainly neutropenia and diarrhea, which can be severe enough to reduce dosage or discontinue the drug [Article:18349289]. Indeed, approximately 7% patients who undergo irinotecan treatment and present with severe neutropenia and fever will die from these complications [Article:18466101]. Several studies have also shown that genotyping for the *28 allele before irinotecan treatment for colorectal cancer is cost-effective [Articles:18466101, 19517472], suggesting that testing for this allele may have a place in clinical practice.

Besides irinotecan, UGT1A1 is also responsible for the glucuronidation of drugs such as raloxifene [Article:12019197] and etoposide [Article:12969965], and some associations have been reported between the *28 allele and pharmacokinetic and pharmacodynamic parameters for these drugs [Articles:19371317, 12969965]. Additionally, the development of hyperbilirubinemia during treatment with inhibitors of UGT1A1, such as atazanavir and tranilast, has also been linked to the presence of the *28 allele [Articles:14647407, 17058217].

It has been suggested that including variants from other UGT1A isoforms may lead to stronger associations with drug side effects and pharmacokinetic measures. UGT1A7 exhibits a five-fold higher specific activity for the SN-38 metabolite than UGT1A1 [Articles:10381366, 12181437], and the inclusion of UGT1A7 alleles into association studies with irinotecan toxicity have shown persuasive results: the combination of UGT1A1*28 with UGT1A7*2 and UGT1A7 -57T/G alleles was superior for prediction of neutropenia and dose reduction, as compared to the UGT1A7 or UGT1A1*28 alleles alone. Indeed, UGT1A1*28 allele by itself showed no association with neutropenia or dose reduction in this particular study [Article:18349289]. The UGT1A7 alleles analyzed were associated with a reduction in either glucuronidation activity or transcription activity, providing a mechanistic explanation for the increased risk of toxicity seen [Article:18349289]. A later study by Cecchin et al. found that in multivariate analyses, UGT1A7*3 was the only significant predictor of hematologic toxicity in the first cycle of treatment with FOLFIRI (fluorouracil, leucovorin and irinotecan); UGT1A1*28 was not a predictor of toxicity [Article:19364970]. Another study by Lévesque et al. in patients taking FOLFIRI found in multivariate analyses that UGT1A7*4 (rs11692021) and UGT1A6*5 (rs2070959) were both significant predictors of neutropenia, while UGT1A1*28 was not [Article:23386248]. UGT1A7*4 is associated with a reduction in glucuronidation activity [Articles:12181437, 11037804] which may explain its association with increased risk for neutropenia. UGT1A6 has been shown to glucuronidate SN-38 [Articles:12181437, 10381366], though no information is currently available on how the *5 allele may affect the enzyme. The study also found a dosage effect when considering multiple alleles: assessing UGT1A7*4 and UGT1A6*5 together as a haplotype gave an odds ratio of 2.18 for the development of neutropenia; including the UGT1A9 -688A/C variant allele in the haplotype increased the odds ratio to 5.28. This result suggests that considering multiple UGT1A variants may improve risk prediction for neutropenia [Article:23386248]. In patients taking atazanavir, Lankish et al. found that the combination of the UGT1A1*28, UGT1A7 -57G and UGT1A7*2, and UGT1A3 -66C variants was associated with increased risk of jaundice and hyperbilirubinemia [Article:17058217]. Approximately 20% of atazanavir-treated subjects were homozygous for this haplotype, compared to 40% of atazanavir-treated subjects who presented with grade 3 or 4 hyperbilirubinemia a statistically significant difference. In subjects with exclusively grade 4 hyperbilirubinemia, 100% were homozygous for the haplotype [Article:17058217]. However, it remains uncertain how variants in UGT1A isoforms that are not directly involved in bilirubin metabolism lead to a propensity for atazanavir-induced hyperbiliriubinemia [Article:17058217]. The alleles present in this study were not in linkage disequilibrium (LD) [Article:17058217], but variants within the UGT1A gene cluster often do show high levels of linkage. This suggests the need for more haplotype-based studies, which can determine interactions among UGT1A variants, and potentially provide better predictions of drug toxicities [Article:19364970].

Citation PharmGKB summary: very important pharmacogene information for UGT1A1. Pharmacogenetics and genomics. 2014. Barbarino Julia M, Haidar Cyrine E, Klein Teri E, Altman Russ B. PubMed
History

Submitted by Eden V. Haverfield (PAAR) (January 6, 2006)

Updated by Julia Barbarino (February 21, 2013)

Key Publications
  1. Refining the UGT1A haplotype associated with irinotecan-induced hematological toxicity in metastatic colorectal cancer patients treated with 5-fluorouracil/irinotecan-based regimens. The Journal of pharmacology and experimental therapeutics. 2013. Lévesque Eric, Bélanger Anne-Sophie, Harvey Mario, Couture Félix, Jonker Derek, Innocenti Federico, Cecchin Erica, Toffoli Giuseppe, Guillemette Chantal. PubMed
  2. Genetically elevated bilirubin and risk of ischaemic heart disease: three Mendelian randomization studies and a meta-analysis. Journal of internal medicine. 2013. Stender S, Frikke-Schmidt R, Nordestgaard B G, Grande P, Tybjaerg-Hansen A. PubMed
  3. Dose-dependent association between UGT1A1*28 genotype and irinotecan-induced neutropenia: low doses also increase risk. Clinical cancer research : an official journal of the American Association for Cancer Research. 2010. Hu Zhe-Yi, Yu Qi, Pei Qi, Guo Cheng. PubMed
  4. Dose-dependent association between UGT1A1*28 polymorphism and irinotecan-induced diarrhoea: a meta-analysis. European journal of cancer (Oxford, England : 1990). 2010. Hu Zhe-Yi, Yu Qi, Zhao Yuan-Sheng. PubMed
  5. Crigler-Najjar syndrome in The Netherlands: identification of four novel UGT1A1 alleles, genotype-phenotype correlation, and functional analysis of 10 missense mutants. Human mutation. 2010. Sneitz Nina, Bakker Conny T, de Knegt Robert J, Halley Dicky J J, Finel Moshe, Bosma Piter J. PubMed
  6. Predictive role of the UGT1A1, UGT1A7, and UGT1A9 genetic variants and their haplotypes on the outcome of metastatic colorectal cancer patients treated with fluorouracil, leucovorin, and irinotecan. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2009. Cecchin Erika, Innocenti Federico, D'Andrea Mario, Corona Giuseppe, De Mattia Elena, Biason Paola, Buonadonna Angela, Toffoli Giuseppe. PubMed
  7. UGT1A1*6 polymorphism is most predictive of severe neutropenia induced by irinotecan in Japanese cancer patients. International journal of clinical oncology / Japan Society of Clinical Oncology. 2009. Onoue Masahide, Terada Tomohiro, Kobayashi Masahiko, Katsura Toshiya, Matsumoto Shigemi, Yanagihara Kazuhiro, Nishimura Takafumi, Kanai Masashi, Teramukai Satoshi, Shimizu Akira, Fukushima Masanori, Inui Ken-ichi. PubMed
  8. Pharmacogenetics of Gilbert's syndrome. Pharmacogenomics. 2008. Strassburg Christian P. PubMed
  9. Genetic diversity at the UGT1 locus is amplified by a novel 3' alternative splicing mechanism leading to nine additional UGT1A proteins that act as regulators of glucuronidation activity. Pharmacogenetics and genomics. 2007. Girard Hugo, Lévesque Eric, Bellemare Judith, Journault Kim, Caillier Bertrand, Guillemette Chantal. PubMed
  10. UGT1A1*28 genotype and irinotecan-induced neutropenia: dose matters. Journal of the National Cancer Institute. 2007. Hoskins Janelle M, Goldberg Richard M, Qu Pingping, Ibrahim Joseph G, McLeod Howard L. PubMed
  11. Gilbert's disease and atazanavir: from phenotype to UDP-glucuronosyltransferase haplotype. Hepatology (Baltimore, Md.). 2006. Lankisch Tim O, Moebius Ulrike, Wehmeier Michael, Behrens Georg, Manns Michael P, Schmidt Reinhold E, Strassburg Christian P. PubMed
  12. Association between the UGT1A1*28 allele, bilirubin levels, and coronary heart disease in the Framingham Heart Study. Circulation. 2006. Lin Jing-Ping, O'Donnell Christopher J, Schwaiger Johannes P, Cupples L Adrienne, Lingenhel Arno, Hunt Steven C, Yang Song, Kronenberg Florian. PubMed
  13. Relationship between hyperbilirubinaemia and UDP-glucuronosyltransferase 1A1 (UGT1A1) polymorphism in adult HIV-infected Thai patients treated with indinavir. Pharmacogenetics and genomics. 2006. Boyd Mark A, Srasuebkul Preeyaporn, Ruxrungtham Kiat, Mackenzie Peter I, Uchaipichat Verawan, Stek Michael, Lange Joep M A, Phanuphak Praphan, Cooper David A, Udomuksorn Wandee, Miners John O. PubMed
  14. Gilbert syndrome and the development of antiretroviral therapy-associated hyperbilirubinemia. The Journal of infectious diseases. 2005. Rotger Margalida, Taffe Patrick, Bleiber Gabriela, Gunthard Huldrych F, Furrer Hansjakob, Vernazza Pietro, Drechsler Henning, Bernasconi Enos, Rickenbach Martin, Telenti Amalio, Swiss HIV Cohort Study. PubMed
  15. Genetic lesions of bilirubin uridine-diphosphoglucuronate glucuronosyltransferase (UGT1A1) causing Crigler-Najjar and Gilbert syndromes: correlation of genotype to phenotype. Human mutation. 2000. Kadakol A, Ghosh S S, Sappal B S, Sharma G, Chowdhury J R, Chowdhury N R. PubMed
  16. Gilbert's syndrome is a contributory factor in prolonged unconjugated hyperbilirubinemia of the newborn. The Journal of pediatrics. 1999. Monaghan G, McLellan A, McGeehan A, Li Volti S, Mollica F, Salemi I, Din Z, Cassidy A, Hume R, Burchell B. PubMed
  17. The genetic basis of the reduced expression of bilirubin UDP-glucuronosyltransferase 1 in Gilbert's syndrome. The New England journal of medicine. 1995. Bosma P J, Chowdhury J R, Bakker C, Gantla S, de Boer A, Oostra B A, Lindhout D, Tytgat G N, Jansen P L, Oude Elferink R P. PubMed
Variant Summaries rs4148323, rs8175347
Drugs
Drug Substrate (3)
Drug Inhibitor (3)
Chemical (1)
bilirubin7,8
Diseases
Pathways

Haplotype Overview

UGT1A1 haplotypes are sourced from either the UGT Alleles Nomenclature page or from several different publications (IA and IB haplotypes from [Article:15179405], I-X haplotypes from [Article:12464801] and the remainder from [Article:15572581] or [Article:15179405]).

Notes on the UGT Alleles Nomenclature page:

Please refer to the UGT1A1 VIP Summary for an explanation of the different UGT1A isoforms, and the composition of the UGT1A locus.

  • For each UGT1A isoform, the UGT Alleles Nomenclature page provides a table of the haplotypes and a list of the SNPs within that gene. If available, associated rsIDs are provided in the SNPs list.
  • Any nucleotide changes or nucleotide positions listed in the haplotype tables or SNPs lists refer to genomic DNA.
  • The list of SNPs consists of nucleotide changes ranging from the promoter region of each UGT1A isoform to the intervening sequence between that isoform and the next one (i.e the 5' to 3' direction down the UGT1A locus). For example, the list of SNPs for UGT1A7 begins with SNPs in the promoter region of that isoform and concludes with SNPs within the intervening sequence between UGT1A7 and UGT1A6.
  • Therefore, when looking at the UGT Alleles Nomenclature page for all rs numbers sorted by nucleotide position, note that the SNPs in the promoter region for UGT1A8 are at the beginning of the list, and the SNPs within the common exon region (exons 2-5) are at the end.

Source: PharmGKB

Haplotypes for UGT1A1 (publication haplotypes)

Haplotypes for UGT1A1 (UGT Alleles Nomenclature page)

All alleles in the download file are on the positive chromosomal strand. PharmGKB considers the first haplotype listed in each table as the reference haplotype for that set.

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Acetaminophen Pathway, Pharmacokinetics
    Stylized diagram showing acetaminophen metabolism and transport in the liver and kidney.
  1. Atorvastatin/Lovastatin/Simvastatin Pathway, Pharmacokinetics
    Drug-specific representation of the candidate genes involved in transport, metabolism and clearance.
  1. Codeine and Morphine Pathway, Pharmacokinetics
    Representation of the candidate genes involved in metabolism of codeine and morphine.
  1. Efavirenz Pathway, Pharmacokinetics/Pharmacodynamics
    Schematic representation of efavirenz metabolism and mechanism of action against HIV.
  1. Erlotinib Pathway, Pharmacokinetics
    Model human liver cell showing genes involved in the transportation and metabolism of Erlotinib.
  1. Estrogen Metabolism Pathway
    Estrogen metabolism in the liver.
  1. Etoposide Pathway, Pharmacokinetics/Pharmacodynamics
    Etoposide cellular disposition and effects.
  1. Fluvastatin Pathway, Pharmacokinetics
    Drug-specific representation of the candidate genes involved in transport, metabolism and clearance.
  1. Irinotecan Pathway, Pharmacodynamics
    Model non-tissue specific cancer cell displaying genes which may be involved in the irinotecan pathway.
  1. Irinotecan Pathway, Pharmacokinetics
    Model human liver cell showing blood, bile and intestinal compartments, indicating tissue specific involvement of genes in the irinotecan pathway.
  1. Losartan Pathway, Pharmacokinetics
    Representation of the candidate genes involved in the metabolism of losartan.
  1. Phenytoin Pathway, Pharmacokinetics
    Genes involved in the metabolism of phenytoin in the human liver cell.
  1. Statin Pathway - Generalized, Pharmacokinetics
    Representation of the superset of all genes involved in the transport, metabolism and clearance of statin class drugs.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this gene. To report a pathway, click here.

No related genes are available

Curated Information ?

Curated Information ?

Publications related to UGT1A1: 242

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
UGT1A and UGT2B genetic variation alters nicotine and nitrosamine glucuronidation in European and African American smokers. Cancer epidemiology, biomarkers & prevention : a publication of the American Association for Cancer Research, cosponsored by the American Society of Preventive Oncology. 2014. Wassenaar Catherine A, et al. PubMed
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Exploring the roles of UGT1A1 and UGT1A3 in oral clearance of GSK2190915, a 5-lipoxygenase-activating protein inhibitor. Pharmacogenetics and genomics. 2014. Mosteller Michael, et al. PubMed
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Effect of UGT1A1, UGT1A3, DIO1 and DIO2 polymorphisms on L-thyroxine doses required for TSH suppression in patients with differentiated thyroid cancer. British journal of clinical pharmacology. 2014. Santoro Ana B, et al. PubMed
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An atlas of genetic influences on human blood metabolites. Nature genetics. 2014. Shin So-Youn, et al. PubMed
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Development of a broad-based ADME panel for use in pharmacogenomic studies. Pharmacogenomics. 2014. Brown Andrew Mk, et al. PubMed
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Personalized pharmacogenomics profiling using whole-genome sequencing. Pharmacogenomics. 2014. Mizzi Clint, et al. PubMed
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UGT1A1*28 polymorphisms: a potential pharmacological biomarker of irinotecan-based chemotherapies in colorectal cancer. Pharmacogenomics. 2014. Liu Xiang, et al. PubMed
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Genetic Factors Affecting Gene Transcription and Catalytic Activity of UDP-Glucuronosyltransferases in Human Liver. Human molecular genetics. 2014. Liu Wanqing, et al. PubMed
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Associations between UGT1A1*6 or UGT1A1*6/*28 polymorphisms and irinotecan-induced neutropenia in Asian cancer patients. Cancer chemotherapy and pharmacology. 2014. Han Fei-fei, et al. PubMed
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Association analysis of UGT1A genotype and haplotype with SN-38 glucuronidation in human livers. Pharmacogenomics. 2014. Wang Huijuan, et al. PubMed
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The effect of the UGT1A1*28 allele on survival after irinotecan-based chemotherapy: a collaborative meta-analysis. The pharmacogenomics journal. 2014. Dias M M, et al. PubMed
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UGT1A1*6 polymorphisms are correlated with irinotecan-induced toxicity: a system review and meta-analysis in Asians. Cancer chemotherapy and pharmacology. 2014. Cheng Lei, et al. PubMed
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PharmGKB summary: very important pharmacogene information for UGT1A1. Pharmacogenetics and genomics. 2014. Barbarino Julia M, et al. PubMed
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In vitro OATP1B1 and OATP1B3 inhibition is associated with observations of benign clinical unconjugated hyperbilirubinemia. Xenobiotica; the fate of foreign compounds in biological systems. 2014. Chiou William J, et al. PubMed
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The association of UGT1A1*6 and UGT1A1*28 with irinotecan-induced neutropenia in Asians: a meta-analysis. Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals. 2014. Chen Yi-Jing, et al. PubMed
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High prevalence of the UGT1A1*28 variant in HIV-infected individuals in Greece. International journal of STD & AIDS. 2014. Panagopoulos P, et al. PubMed
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Genomewide association study of atazanavir pharmacokinetics and hyperbilirubinemia in AIDS Clinical Trials Group protocol A5202. Pharmacogenetics and genomics. 2014. Johnson Daniel H, et al. PubMed
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Pharmacokinetics, safety, and efficacy of FOLFIRI plus bevacizumab in Japanese colorectal cancer patients with UGT1A1 gene polymorphisms. Journal of clinical pharmacology. 2014. Suenaga Mitsukuni, et al. PubMed
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Evaluation of the effect of UGT1A1 polymorphisms on dolutegravir pharmacokinetics. Pharmacogenomics. 2014. Chen Shuguang, et al. PubMed
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Correction: Glucuronidation by UGT1A1 Is the Dominant Pathway of the Metabolic Disposition of Belinostat in Liver Cancer Patients. PloS one. 2014. Wang Ling-Zhi, et al. PubMed
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Prognostic advantage of irinotecan dose escalation according to uridine diphosphate glucuronosyltransferase 1A1 (UGT1A1) genotyping in patients with metastatic colorectal cancer treated with bevacizumab combined with 5-fluorouracil/leucovorin with irinotecan in a first-line setting. Translational research : the journal of laboratory and clinical medicine. 2014. Lu Chien-Yu, et al. PubMed
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Extended mathematical model for "in vivo" quantification of the interaction betweeen atazanavir and bilirubin. Journal of clinical pharmacology. 2013. Lozano Roberto, et al. PubMed
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Pregnancy and pharmacogenomics in the context of drug metabolism and response. Pharmacogenomics. 2013. Helldén Anders, et al. PubMed
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Clinical and pharmacogenetic factors affecting neonatal bilirubinemia following atazanavir treatment of mothers during pregnancy. AIDS research and human retroviruses. 2013. Eley Timothy, et al. PubMed
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S-1 plus irinotecan and oxaliplatin for the first-line treatment of patients with metastatic colorectal cancer: a prospective phase II study and pharmacogenetic analysis. British journal of cancer. 2013. Kim S Y, et al. PubMed
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Evaluating the in vitro inhibition of UGT1A1, OATP1B1, OATP1B3, MRP2, and BSEP in predicting drug-induced hyperbilirubinemia. Molecular pharmaceutics. 2013. Chang Jae H, et al. PubMed
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Characterization of raloxifene glucuronidation: potential role of UGT1A8 genotype on raloxifene metabolism in vivo. Cancer prevention research (Philadelphia, Pa.). 2013. Sun Dongxiao, et al. PubMed
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Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
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Polymorphisms influencing olanzapine metabolism and adverse effects in healthy subjects. Human psychopharmacology. 2013. Cabaleiro Teresa, et al. PubMed
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Preclinical discovery of candidate genes to guide pharmacogenetics during phase I development: the example of the novel anticancer agent ABT-751. Pharmacogenetics and genomics. 2013. Innocenti Federico, et al. PubMed
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TokyoGreen derivatives as specific and practical fluorescent probes for UDP-glucuronosyltransferase (UGT) 1A1. Chemical communications (Cambridge, England). 2013. Terai Takuya, et al. PubMed
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CYP2C19 genotype has a major influence on labetalol pharmacokinetics in healthy male Chinese subjects. European journal of clinical pharmacology. 2013. Chan Sze Wa, et al. PubMed
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Anti-Parkinson's disease drugs and pharmacogenetic considerations. Expert opinion on drug metabolism & toxicology. 2013. Agúndez José A G, et al. PubMed
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Association between severe toxicity of nilotinib and UGT1A1 polymorphisms in Japanese patients with chronic myelogenous leukemia. International journal of clinical oncology. 2013. Shibata Takashi, et al. PubMed
Refining the UGT1A haplotype associated with irinotecan-induced hematological toxicity in metastatic colorectal cancer patients treated with 5-fluorouracil/irinotecan-based regimens. The Journal of pharmacology and experimental therapeutics. 2013. Lévesque Eric, et al. PubMed
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Association of UGT1A1*28 polymorphisms with irinotecan-induced toxicities in colorectal cancer: a meta-analysis in Caucasians. The pharmacogenomics journal. 2013. Liu X, et al. PubMed
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Impact of UGT1A1 Gilbert variant on discontinuation of ritonavir-boosted atazanavir in AIDS Clinical Trials Group Study A5202. The Journal of infectious diseases. 2013. Ribaudo Heather J, et al. PubMed
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Genetically elevated bilirubin and risk of ischaemic heart disease: three Mendelian randomization studies and a meta-analysis. Journal of internal medicine. 2013. Stender S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cost-effectiveness analysis of UGT1A1 genetic testing to inform antiretroviral prescribing in HIV disease. Antiviral therapy. 2013. Schackman Bruce R, et al. PubMed
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Acetaminophen administration in a patient with Gilbert's syndrome. Pediatrics international : official journal of the Japan Pediatric Society. 2012. Nakagawa Taku, et al. PubMed
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Glucuronidation by UGT1A1 Is the Dominant Pathway of the Metabolic Disposition of Belinostat in Liver Cancer Patients. PloS one. 2013. Wang Ling-Zhi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Large-Scale Gene-Centric Meta-analysis across 32 Studies Identifies Multiple Lipid Loci. American journal of human genetics. 2012. Asselbergs Folkert W, et al. PubMed
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Potential effect of pharmacogenetics on maternal, fetal and infant antiretroviral drug exposure during pregnancy and breastfeeding. Pharmacogenomics. 2012. Olagunju Adeniyi, et al. PubMed
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Short communication: UGT1A1*28 variant allele is a predictor of severe hyperbilirubinemia in HIV-infected patients on HAART in southern Brazil. AIDS research and human retroviruses. 2012. Turatti Lisiane, et al. PubMed
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Switching to unboosted atazanavir reduces bilirubin and triglycerides without compromising treatment efficacy in UGT1A1*28 polymorphism carriers. The Journal of antimicrobial chemotherapy. 2012. Ferraris Laurenzia, et al. PubMed
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Glucuronidation of the second-generation antipsychotic clozapine and its active metabolite N-desmethylclozapine. Potential importance of the UGT1A1 A(TA)₇TAA and UGT1A4 L48V polymorphisms. Pharmacogenetics and genomics. 2012. Erickson-Ridout Kathryn K, et al. PubMed
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The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological reviews. 2012. Michaud Veronique, et al. PubMed
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PharmGKB summary: phenytoin pathway. Pharmacogenetics and genomics. 2012. Thorn Caroline F, et al. PubMed
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Impact of the UGT1A1*28 allele on response to irinotecan: a systematic review and meta-analysis. Pharmacogenomics. 2012. Dias Mafalda M, et al. PubMed
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Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. European journal of clinical pharmacology. 2012. Brennan Meghan, et al. PubMed
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Lapatinib-induced liver injury characterized by class II HLA and Gilbert's syndrome genotypes. Clinical pharmacology and therapeutics. 2012. Spraggs C F, et al. PubMed
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Association between bilirubin and cardiovascular disease risk factors: using Mendelian randomization to assess causal inference. BMC cardiovascular disorders. 2012. McArdle Patrick F, et al. PubMed
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Effect of efavirenz on UDP-glucuronosyltransferase 1A1, 1A4, 1A6, and 1A9 activities in human liver microsomes. Molecules (Basel, Switzerland). 2012. Ji Hye Young, et al. PubMed
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Methylenetetrahydrofolate reductase genetic polymorphisms and toxicity to 5-FU-based chemoradiation in rectal cancer. British journal of cancer. 2011. Thomas F, et al. PubMed
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Single nucleotide polymorphisms of ABCC5 and ABCG1 transporter genes correlate to irinotecan-associated gastrointestinal toxicity in colorectal cancer patients: A DMET microarray profiling study. Cancer biology & therapy. 2011. Di Martino Maria Teresa, et al. PubMed
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Clinical pharmacology profile of raltegravir, an HIV-1 integrase strand transfer inhibitor. Journal of clinical pharmacology. 2011. Brainard Diana M, et al. PubMed
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Quantitative distribution of mRNAs encoding the 19 human UDP-glucuronosyltransferase enzymes in 26 adult and 3 fetal tissues. Xenobiotica; the fate of foreign compounds in biological systems. 2011. Court Michael H, et al. PubMed
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Perspectives on Epigenetics and Its Relevance to Adverse Drug Reactions. Clinical pharmacology and therapeutics. 2011. Kacevska M, et al. PubMed
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Drug Interactions Between the Immunosuppressant Tacrolimus and the Cholesterol Absorption Inhibitor Ezetimibe in Healthy Volunteers. Clinical pharmacology and therapeutics. 2011. Oswald S, et al. PubMed
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Pharmacogenetics: From Bench to Byte- An Update of Guidelines. Clinical pharmacology and therapeutics. 2011. Swen J J, et al. PubMed
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Pharmacogenomics of the RNA world: structural RNA polymorphisms in drug therapy. Clinical pharmacology and therapeutics. 2011. Sadee W, et al. PubMed
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Detrimental effect of atazanavir plasma concentrations on total serum bilirubin levels in the presence of UGT1A1 polymorphisms. Journal of acquired immune deficiency syndromes (1999). 2011. Cicconi Paola, et al. PubMed
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Genomics and drug response. The New England journal of medicine. 2011. Wang Liewei, et al. PubMed
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Associations of various gene polymorphisms with toxicity in colorectal cancer patients receiving oral uracil and tegafur plus leucovorin: a prospective study. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO. 2011. Tsunoda A, et al. PubMed
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Databases in the area of pharmacogenetics. Human mutation. 2011. Sim Sarah C, et al. PubMed
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Prediction of irinotecan and 5-fluorouracil toxicity and response in patients with advanced colorectal cancer. The pharmacogenomics journal. 2011. Glimelius B, et al. PubMed
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Pharmacogenetic Tailoring of Irinotecan-based First-line Chemotherapy in Metastatic Colorectal Cancer: Results of a Pilot Study. Anticancer research. 2011. Freyer Gilles, et al. PubMed
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Association of pharmacogenetic markers with premature discontinuation of first-line anti-HIV therapy: an observational cohort study. The Journal of infectious diseases. 2011. Lubomirov Rubin, et al. PubMed
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Pharmacogenetic tests in cancer chemotherapy: what physicians should know for clinical application. The Journal of pathology. 2011. Lee Soo-Youn, et al. PubMed
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Pharmacogenomic contribution to drug response. Cancer journal (Sudbury, Mass.). 2011. Watson Roshawn G, et al. PubMed
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Successful tacrolimus treatment following renal transplant in a HIV-infected patient with raltegravir previously treated with a protease inhibitor based regimen. Drug metabolism and drug interactions. 2011. Cousins Darren, et al. PubMed
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Exposure-related effects of atazanavir on the pharmacokinetics of raltegravir in HIV-1-infected patients. Therapeutic drug monitoring. 2010. Cattaneo Dario, et al. PubMed
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Systematic review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, et al. PubMed
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Characterization of 107 genomic DNA reference materials for CYP2D6, CYP2C19, CYP2C9, VKORC1, and UGT1A1: a GeT-RM and Association for Molecular Pathology collaborative project. The Journal of molecular diagnostics : JMD. 2010. Pratt Victoria M, et al. PubMed
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Alternative-splicing forms of the major phase II conjugating UGT1A gene negatively regulate glucuronidation in human carcinoma cell lines. The pharmacogenomics journal. 2010. Bellemare J, et al. PubMed
Dose-dependent association between UGT1A1*28 genotype and irinotecan-induced neutropenia: low doses also increase risk. Clinical cancer research : an official journal of the American Association for Cancer Research. 2010. Hu Zhe-Yi, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP2B6. Pharmacogenetics and genomics. 2010. Thorn Caroline F, et al. PubMed
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Relation of ADRB1, CYP2D6, and UGT1A1 polymorphisms with dose of, and response to, carvedilol or metoprolol therapy in patients with chronic heart failure. The American journal of cardiology. 2010. Baudhuin Linnea M, et al. PubMed
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Genetic factors influencing severe atazanavir-associated hyperbilirubinemia in a population with low UDP-glucuronosyltransferase 1A1*28 allele frequency. Clinical infectious diseases : an official publication of the Infectious Diseases Society of America. 2010. Park Wan Beom, et al. PubMed
Dose-dependent association between UGT1A1*28 polymorphism and irinotecan-induced diarrhoea: a meta-analysis. European journal of cancer (Oxford, England : 1990). 2010. Hu Zhe-Yi, et al. PubMed
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The UGT1A1*28 polymorphism correlates with erlotinib's effect on SN-38 glucuronidation. European journal of cancer (Oxford, England : 1990). 2010. Liu Yong, et al. PubMed
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Pharmacogenetic predictors of adverse events and response to chemotherapy in metastatic colorectal cancer: results from North American Gastrointestinal Intergroup Trial N9741. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. McLeod Howard L, et al. PubMed
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Genetic profile of patients with epilepsy on first-line antiepileptic drugs and potential directions for personalized treatment. Pharmacogenomics. 2010. Grover Sandeep, et al. PubMed
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Pharmacokinetic and pharmacodynamic interactions between the immunosuppressant sirolimus and the lipid-lowering drug ezetimibe in healthy volunteers. Clinical pharmacology and therapeutics. 2010. Oswald S, et al. PubMed
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Pharmacogenetic assessment of toxicity and outcome in patients with metastatic colorectal cancer treated with LV5FU2, FOLFOX, and FOLFIRI: FFCD 2000-05. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Boige Valérie, et al. PubMed
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Pazopanib-induced hyperbilirubinemia is associated with Gilbert's syndrome UGT1A1 polymorphism. British journal of cancer. 2010. Xu C-F, et al. PubMed
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Uridine 5'-diphospho-glucuronosyltransferase genetic polymorphisms and response to cancer chemotherapy. Future oncology (London, England). 2010. Ramírez Jacqueline, et al. PubMed
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Association of SUMO1 and UBC9 genotypes with tumor response in non-small-cell lung cancer treated with irinotecan-based chemotherapy. The pharmacogenomics journal. 2010. Han Ji-Youn, et al. PubMed
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Oxaliplatin, irinotecan and capecitabine as first-line therapy in metastatic colorectal cancer (mCRC): a dose-finding study and pharmacogenomic analysis. British journal of cancer. 2010. Zarate R, et al. PubMed
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An overview of the recent progress in irinotecan pharmacogenetics. Pharmacogenomics. 2010. Fujiwara Yutaka, et al. PubMed
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Gilbert-Meulengracht's syndrome and pharmacogenetics: is jaundice just the tip of the iceberg?. Drug metabolism reviews. 2010. Strassburg Christian P. PubMed
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Pharmacogenetics of antiretrovirals. Antiviral research. 2010. Tozzi Valerio. PubMed
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Individualizing dosing of irinotecan. Clinical cancer research : an official journal of the American Association for Cancer Research. 2010. Ratain Mark J, et al. PubMed
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UDP-glucuronosyltransferase (UGT) polymorphisms affect atorvastatin lactonization in vitro and in vivo. Clinical pharmacology and therapeutics. 2010. Riedmaier S, et al. PubMed
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Comparison of the drug-drug interactions potential of erlotinib and gefitinib via inhibition of UDP-glucuronosyltransferases. Drug metabolism and disposition: the biological fate of chemicals. 2010. Liu Yong, et al. PubMed
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Crigler-Najjar syndrome in The Netherlands: identification of four novel UGT1A1 alleles, genotype-phenotype correlation, and functional analysis of 10 missense mutants. Human mutation. 2010. Sneitz Nina, et al. PubMed
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UGT1A1 polymorphism and hyperbilirubinemia in a patient who received sorafenib. Cancer chemotherapy and pharmacology. 2009. Meza-Junco Judith, et al. PubMed
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Leveraging learning from a phase III colorectal cancer clinical trial: outcomes, methodology, meta-analysis and pharmacogenetics. Transactions of the American Clinical and Climatological Association. 2010. Goldberg Richard M, et al. PubMed
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Genetic polymorphisms of drug-metabolizing enzymes and anti-TB drug-induced hepatitis. Pharmacogenomics. 2009. Kim Sang-Heon, et al. PubMed
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Cost effectiveness of pharmacogenetic testing for uridine diphosphate glucuronosyltransferase 1A1 before irinotecan administration for metastatic colorectal cancer. Cancer. 2009. Gold Heather Taffet, et al. PubMed
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Genetic polymorphisms in the TATA box and upstream phenobarbital-responsive enhancer module of the UGT1A1 promoter have combined effects on UDP-glucuronosyltransferase 1A1 transcription mediated by constitutive androstane receptor, pregnane X receptor, or glucocorticoid receptor in human liver. Drug metabolism and disposition: the biological fate of chemicals. 2009. Li Ye, et al. PubMed
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Methadone induces the expression of hepatic drug-metabolizing enzymes through the activation of pregnane X receptor and constitutive androstane receptor. Drug metabolism and disposition: the biological fate of chemicals. 2009. Tolson Antonia H, et al. PubMed
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The increasing role of pharmacogenetics in the treatment of gastrointestinal cancers. Gastrointestinal cancer research : GCR. 2009. Yalçin Suayib. PubMed
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Addressing the challenges of the clinical application of pharmacogenetic testing. Clinical pharmacology and therapeutics. 2009. Ikediobi O N, et al. PubMed
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Clinically available pharmacogenomics tests. Clinical pharmacology and therapeutics. 2009. Flockhart D A, et al. PubMed
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Pharmacokinetics of raltegravir in individuals with UGT1A1 polymorphisms. Clinical pharmacology and therapeutics. 2009. Wenning L A, et al. PubMed
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Pharmacogenetics and biomarkers in colorectal cancer. The pharmacogenomics journal. 2009. Strimpakos A S, et al. PubMed
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ADME pharmacogenetics: current practices and future outlook. Expert opinion on drug metabolism & toxicology. 2009. Grossman Iris. PubMed
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Predictive role of the UGT1A1, UGT1A7, and UGT1A9 genetic variants and their haplotypes on the outcome of metastatic colorectal cancer patients treated with fluorouracil, leucovorin, and irinotecan. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2009. Cecchin Erika, et al. PubMed
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UGT1A1*28 genotype predicts gastrointestinal toxicity in patients treated with intermediate-dose irinotecan. Pharmacogenomics. 2009. Ferraldeschi Roberta, et al. PubMed
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Pharmacogenetic study in Hodgkin lymphomas reveals the impact of UGT1A1 polymorphisms on patient prognosis. Blood. 2009. Ribrag Vincent, et al. PubMed
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Effects of UGT1A1*28 polymorphism on raloxifene pharmacokinetics and pharmacodynamics. British journal of clinical pharmacology. 2009. Trontelj Jurij, et al. PubMed
UGT1A1*6 polymorphism is most predictive of severe neutropenia induced by irinotecan in Japanese cancer patients. International journal of clinical oncology / Japan Society of Clinical Oncology. 2009. Onoue Masahide, et al. PubMed
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Common variants of four bilirubin metabolism genes and their association with serum bilirubin and coronary artery disease in Chinese Han population. Pharmacogenetics and genomics. 2009. Lin Rong, et al. PubMed
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Data-driven methods to discover molecular determinants of serious adverse drug events. Clinical pharmacology and therapeutics. 2009. Chiang A P, et al. PubMed
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Ethnic differences in drug metabolism and toxicity from chemotherapy. Expert opinion on drug metabolism & toxicology. 2009. Phan Viet Hong, et al. PubMed
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Phase I trial of oral irinotecan and temozolomide for children with relapsed high-risk neuroblastoma: a new approach to neuroblastoma therapy consortium study. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2009. Wagner Lars M, et al. PubMed
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Phase I/II pharmacokinetic and pharmacogenomic study of UGT1A1 polymorphism in elderly patients with advanced non-small cell lung cancer treated with irinotecan. Clinical pharmacology and therapeutics. 2009. Yamamoto N, et al. PubMed
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Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer. Lung cancer (Amsterdam, Netherlands). 2009. Han Ji-Youn, et al. PubMed
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Pharmacogenetics and pharmacogenomics of anticancer agents. CA: a cancer journal for clinicians. 2009. Huang R Stephanie, et al. PubMed
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UGT1A1, UGT1A6 and UGT1A7 genetic analysis: repercussion for irinotecan pharmacogenetics in the São Miguel Island Population (Azores, Portugal). Molecular diagnosis & therapy. 2009. Pacheco Paula R, et al. PubMed
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Clinical significance of UDP-glucuronosyltransferase 1A1*6 for toxicities of combination chemotherapy with irinotecan and cisplatin in gynecologic cancers: a prospective multi-institutional study. Oncology. 2009. Takano Masashi, et al. PubMed
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Predictive Factors for Response and Toxicity in Chemotherapy: Pharmacogenomics. Seminars in colon & rectal surgery. 2008. Sanoff Hanna K, et al. PubMed
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Pharmacokinetic and pharmacogenetic determinants of the activity and toxicity of irinotecan in metastatic colorectal cancer patients. British journal of cancer. 2008. Rouits E, et al. PubMed
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Irinotecan and uridine diphosphate glucuronosyltransferase 1A1 pharmacogenetics: to test or not to test, that is the question. Cancer. 2008. Deeken John F, et al. PubMed
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The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan. Biochemical pharmacology. 2008. Alonen Anna, et al. PubMed
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Pharmacogenetic pathway analysis of irinotecan. Clinical pharmacology and therapeutics. 2008. Rosner G L, et al. PubMed
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Pharmacogenetic insights into codeine analgesia: implications to pediatric codeine use. Pharmacogenomics. 2008. Madadi Parvaz, et al. PubMed
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Variations in the UDP-glucuronosyltransferase 1A1 gene for the development of unconjugated hyperbilirubinemia in Taiwanese. Pharmacogenomics. 2008. Huang Yang-Yang, et al. PubMed
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Pathway based analysis of SNPs with relevance to 5-FU therapy: relation to intratumoral mRNA expression and survival. International journal of cancer. Journal international du cancer. 2008. Nordgard Silje H, et al. PubMed
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Pharmacogenetics in colorectal cancer: a systematic review. Pharmacogenomics. 2008. Funke Silvia, et al. PubMed
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Pharmacogenetic profiling in patients with advanced colorectal cancer treated with first-line FOLFIRI chemotherapy. The pharmacogenomics journal. 2008. Ruzzo A, et al. PubMed
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In vitro characterisation of human renal and hepatic frusemide glucuronidation and identification of the UDP-glucuronosyltransferase enzymes involved in this pathway. Biochemical pharmacology. 2008. Kerdpin Oranun, et al. PubMed
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UGT1A1*28 genotype and irinotecan dosage in patients with metastatic colorectal cancer: a Dutch Colorectal Cancer Group study. British journal of cancer. 2008. Kweekel D M, et al. PubMed
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Pharmacogenetics of Gilbert's syndrome. Pharmacogenomics. 2008. Strassburg Christian P. PubMed
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UGT1A1*28 polymorphism predicts irinotecan-induced severe toxicities without affecting treatment outcome and survival in patients with metastatic colorectal carcinoma. Cancer. 2008. Liu Chun-Yu, et al. PubMed
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Pharmacogenetics: from bench to byte. Clinical pharmacology and therapeutics. 2008. Swen J J, et al. PubMed
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Pharmacogenetics of antiretroviral agents. Current opinion in HIV and AIDS. 2008. Owen Andrew, et al. PubMed
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Cost-effectiveness of UGT1A1 genotyping in second-line, high-dose, once every 3 weeks irinotecan monotherapy treatment of colorectal cancer. Pharmacogenomics. 2008. Obradovic Marko, et al. PubMed
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Lopinavir-ritonavir dramatically affects the pharmacokinetics of irinotecan in HIV patients with Kaposi's sarcoma. Clinical pharmacology and therapeutics. 2008. Corona G, et al. PubMed
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Contribution of UDP-glucuronosyltransferase 1A1 and 1A8 to morphine-6-glucuronidation and its kinetic properties. Drug metabolism and disposition: the biological fate of chemicals. 2008. Ohno Shuji, et al. PubMed
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Gilbert's Syndrome and irinotecan toxicity: combination with UDP-glucuronosyltransferase 1A7 variants increases risk. Cancer epidemiology, biomarkers & prevention : a publication of the American Association for Cancer Research, cosponsored by the American Society of Preventive Oncology. 2008. Lankisch Tim O, et al. PubMed
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Glucose-6-phosphate dehydrogenase deficiency. Lancet. 2008. Cappellini M D, et al. PubMed
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A genomic "roadmap" to "better" drugs. Drug metabolism reviews. 2008. Liao Guochun, et al. PubMed
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Pharmacogenetics of mycophenolate mofetil: a promising different approach to tailoring immunosuppression?. Journal of nephrology. 2008. Betonico G N, et al. PubMed
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Genetic diversity at the UGT1 locus is amplified by a novel 3' alternative splicing mechanism leading to nine additional UGT1A proteins that act as regulators of glucuronidation activity. Pharmacogenetics and genomics. 2007. Girard Hugo, et al. PubMed
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Influence of mutations associated with Gilbert and Crigler-Najjar type II syndromes on the glucuronidation kinetics of bilirubin and other UDP-glucuronosyltransferase 1A substrates. Pharmacogenetics and genomics. 2007. Udomuksorn Wandee, et al. PubMed
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UGT1A1 promoter polymorphism increases risk of nilotinib-induced hyperbilirubinemia. Leukemia : official journal of the Leukemia Society of America, Leukemia Research Fund, U.K. 2007. Singer J B, et al. PubMed
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In silico and in vitro pharmacogenetic analysis in mice. Proceedings of the National Academy of Sciences of the United States of America. 2007. Guo Yingying, et al. PubMed
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Intra-ethnic differences in genetic variants of the UGT-glucuronosyltransferase 1A1 gene in Chinese populations. The pharmacogenomics journal. 2007. Zhang A, et al. PubMed
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Role of UGT1A1*6, UGT1A1*28 and ABCG2 c.421C>A polymorphisms in irinotecan-induced neutropenia in Asian cancer patients. Cancer science. 2007. Jada Srinivasa Rao, et al. PubMed
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Stereoselective glucuronidation of 5-(4'-hydroxyphenyl)-5-phenylhydantoin by human UDP-glucuronosyltransferase (UGT) 1A1, UGT1A9, and UGT2B15: effects of UGT-UGT interactions. Drug metabolism and disposition: the biological fate of chemicals. 2007. Nakajima Miki, et al. PubMed
UGT1A1*28 genotype and irinotecan-induced neutropenia: dose matters. Journal of the National Cancer Institute. 2007. Hoskins Janelle M, et al. PubMed
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UGT1A1 polymorphism can predict hematologic toxicity in patients treated with irinotecan. Clinical cancer research : an official journal of the American Association for Cancer Research. 2007. Côté Jean-François, et al. PubMed
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UGT1A1 promoter genotype correlates with SN-38 pharmacokinetics, but not severe toxicity in patients receiving low-dose irinotecan. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2007. Stewart Clinton F, et al. PubMed
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Ancestry and pharmacogenetics of antileukemic drug toxicity. Blood. 2007. Kishi Shinji, et al. PubMed
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Effects of green tea compounds on irinotecan metabolism. Drug metabolism and disposition: the biological fate of chemicals. 2007. Mirkov Snezana, et al. PubMed
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Irinotecan-induced diarrhea: functional significance of the polymorphic ABCC2 transporter protein. Clinical pharmacology and therapeutics. 2007. de Jong F A, et al. PubMed
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The role of SN-38 exposure, UGT1A1*28 polymorphism, and baseline bilirubin level in predicting severe irinotecan toxicity. Journal of clinical pharmacology. 2007. Ramchandani Roshni P, et al. PubMed
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Pharmacogenetics of irinotecan: clinical perspectives on the utility of genotyping. Pharmacogenomics. 2006. Innocenti Federico, et al. PubMed
Gilbert's disease and atazanavir: from phenotype to UDP-glucuronosyltransferase haplotype. Hepatology (Baltimore, Md.). 2006. Lankisch Tim O, et al. PubMed
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A phase II study of irinotecan and carboplatin in advanced non-small cell lung cancer with pharmacogenomic analysis: final report. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2006. Pillot Giancarlo A, et al. PubMed
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Association between the UGT1A1*28 allele, bilirubin levels, and coronary heart disease in the Framingham Heart Study. Circulation. 2006. Lin Jing-Ping, et al. PubMed
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Estrogen sulfation genes, hormone replacement therapy, and endometrial cancer risk. Journal of the National Cancer Institute. 2006. Rebbeck Timothy R, et al. PubMed
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Prophylaxis of irinotecan-induced diarrhea with neomycin and potential role for UGT1A1*28 genotype screening: a double-blind, randomized, placebo-controlled study. The oncologist. 2006. de Jong Floris A, et al. PubMed
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Genetic variability, haplotypes, and htSNPs for exons 1 at the human UGT1A locus. Human mutation. 2006. Thomas Sushma S, et al. PubMed
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The role of UGT1A1*28 polymorphism in the pharmacodynamics and pharmacokinetics of irinotecan in patients with metastatic colorectal cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2006. Toffoli Giuseppe, et al. PubMed
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Ketoconazole and miconazole are antagonists of the human glucocorticoid receptor: consequences on the expression and function of the constitutive androstane receptor and the pregnane X receptor. Molecular pharmacology. 2006. Duret Cedric, et al. PubMed
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Cancer and leukemia group B gastrointestinal cancer committee. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Goldberg Richard M, et al. PubMed
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N-Glucuronidation of the antiepileptic drug retigabine: results from studies with human volunteers, heterologously expressed human UGTs, human liver, kidney, and liver microsomal membranes of Crigler-Najjar type II. Metabolism: clinical and experimental. 2006. Borlak Jürgen, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Expression of drug pathway proteins is independent of tumour type. The Journal of pathology. 2006. Zhang W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity. Chemical research in toxicology. 2006. Mutlib Abdul E, et al. PubMed
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Comprehensive analysis of UGT1A polymorphisms predictive for pharmacokinetics and treatment outcome in patients with non-small-cell lung cancer treated with irinotecan and cisplatin. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2006. Han Ji-Youn, et al. PubMed
Relationship between hyperbilirubinaemia and UDP-glucuronosyltransferase 1A1 (UGT1A1) polymorphism in adult HIV-infected Thai patients treated with indinavir. Pharmacogenetics and genomics. 2006. Boyd Mark A, et al. PubMed
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Uridine diphosphate glucuronosyl transferase 1A1 promoter polymorphism predicts the risk of gastrointestinal toxicity and fatigue induced by irinotecan-based chemotherapy. Cancer. 2006. Massacesi Cristian, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Irinotecan inactivation is modulated by epigenetic silencing of UGT1A1 in colon cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Gagnon Jean-François, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Expression of UDP-glucuronosyltransferase isoform mRNAs during inflammation and infection in mouse liver and kidney. Drug metabolism and disposition: the biological fate of chemicals. 2006. Richardson Terrilyn A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Study of the genetic determinants of UGT1A1 inducibility by phenobarbital in cultured human hepatocytes. Pharmacogenetics and genomics. 2006. Ramírez Jacqueline, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Contribution of polymorphisms in UDP-glucuronosyltransferase and CYP2D6 to the individual variation in disposition of carvedilol. Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Société canadienne des sciences pharmaceutiques. 2006. Takekuma Yoh, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Overview of the pharmacogenetics of HIV therapy. The pharmacogenomics journal. 2006. Rodríguez-Nóvoa S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug metabolism and disposition: the biological fate of chemicals. 2005. Zhang Donglu, et al. PubMed
Gilbert syndrome and the development of antiretroviral therapy-associated hyperbilirubinemia. The Journal of infectious diseases. 2005. Rotger Margalida, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of ketoconazole on glucuronidation by UDP-glucuronosyltransferase enzymes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2005. Yong Wei Peng, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Alternate pathways of thyroid hormone metabolism. Thyroid : official journal of the American Thyroid Association. 2005. Wu Sing-Yung, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug metabolism and disposition: the biological fate of chemicals. 2005. Kuehl Gwendolyn E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of outcome in children with acute lymphoblastic leukemia. Blood. 2005. Rocha Jose Claudio C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional analysis of six human aryl hydrocarbon receptor variants in a Japanese population. Drug metabolism and disposition: the biological fate of chemicals. 2005. Koyano Satoru, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Haplotypes of variants in the UDP-glucuronosyltransferase1A9 and 1A1 genes. Pharmacogenetics and genomics. 2005. Innocenti Federico, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Racial variability in haplotype frequencies of UGT1A1 and glucuronidation activity of a novel single nucleotide polymorphism 686C> T (P229L) found in an African-American. Drug metabolism and disposition: the biological fate of chemicals. 2005. Kaniwa Nahoko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
UGT1A1 variation and gallstone formation in sickle cell disease. Blood. 2005. Haverfield Eden V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clinical pharmacokinetics. 2005. Kosoglou Teddy, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Breast cancer risk associated with genotype polymorphism of the catechol estrogen-metabolizing genes: a multigenic study on cancer susceptibility. International journal of cancer. Journal international du cancer. 2005. Cheng Ting-Chih, et al. PubMed
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UGT1A1 gene variations and irinotecan treatment in patients with metastatic colorectal cancer. British journal of cancer. 2004. Marcuello E, et al. PubMed
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Relevance of different UGT1A1 polymorphisms in irinotecan-induced toxicity: a molecular and clinical study of 75 patients. Clinical cancer research : an official journal of the American Association for Cancer Research. 2004. Rouits Elisabeth, et al. PubMed
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Pharmacogenetics of tipifarnib (R115777) transport and metabolism in cancer patients. Investigational new drugs. 2004. Sparreboom Alex, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
UGT1A1 haplotypes associated with reduced glucuronidation and increased serum bilirubin in irinotecan-administered Japanese patients with cancer. Clinical pharmacology and therapeutics. 2004. Sai Kimie, et al. PubMed
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Genetic variants in the UDP-glucuronosyltransferase 1A1 gene predict the risk of severe neutropenia of irinotecan. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2004. Innocenti Federico, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Irinotecan pharmacogenetics: is it time to intervene?. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2004. McLeod Howard L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of prednisone and genetic polymorphisms on etoposide disposition in children with acute lymphoblastic leukemia. Blood. 2004. Kishi Shinji, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cancer pharmacogenetics: polymorphisms, pathways and beyond. Nature reviews. Cancer. 2003. Ulrich Cornelia M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A Gilbert's syndrome UGT1A1 variant confers susceptibility to tranilast-induced hyperbilirubinemia. The pharmacogenomics journal. 2004. Danoff T M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Identification of a pharmacogenetic effect by linkage disequilibrium mapping. The pharmacogenomics journal. 2004. Xu C-F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Glucuronidation of etoposide in human liver microsomes is specifically catalyzed by UDP-glucuronosyltransferase 1A1. Drug metabolism and disposition: the biological fate of chemicals. 2003. Watanabe Yuichiro, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Characterization of nicotine and cotinine N-glucuronidations in human liver microsomes. Drug metabolism and disposition: the biological fate of chemicals. 2002. Nakajima Miki, et al. PubMed
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Haplotype structure of the UDP-glucuronosyltransferase 1A1 promoter in different ethnic groups. Pharmacogenetics. 2002. Innocenti Federico, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Involvement of multiple UDP-glucuronosyltransferase 1A isoforms in glucuronidation of 5-(4'-hydroxyphenyl)-5-phenylhydantoin in human liver microsomes. Drug metabolism and disposition: the biological fate of chemicals. 2002. Nakajima Miki, et al. PubMed
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Common human UGT1A polymorphisms and the altered metabolism of irinotecan active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38). Molecular pharmacology. 2002. Gagné Jean-François, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Nuclear pregnane x receptor and constitutive androstane receptor regulate overlapping but distinct sets of genes involved in xenobiotic detoxification. Molecular pharmacology. 2002. Maglich Jodi M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Identification of a defect in the UGT1A1 gene promoter and its association with hyperbilirubinemia. Biochemical and biophysical research communications. 2002. Sugatani Junko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
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UGT1A1*28 polymorphism as a determinant of irinotecan disposition and toxicity. The pharmacogenomics journal. 2002. Iyer L, et al. PubMed
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Human liver UDP-glucuronosyltransferase isoforms involved in the glucuronidation of 7-ethyl-10-hydroxycamptothecin. Xenobiotica; the fate of foreign compounds in biological systems. 2001. Hanioka N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of anticancer agents: lessons from amonafide and irinotecan. Drug metabolism and disposition: the biological fate of chemicals. 2001. Innocenti F, et al. PubMed
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Polymorphisms of UDP-glucuronosyltransferase gene and irinotecan toxicity: a pharmacogenetic analysis. Cancer research. 2000. Ando Y, et al. PubMed
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Genetic lesions of bilirubin uridine-diphosphoglucuronate glucuronosyltransferase (UGT1A1) causing Crigler-Najjar and Gilbert syndromes: correlation of genotype to phenotype. Human mutation. 2000. Kadakol A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Variations of the bilirubin uridine-diphosphoglucuronosyl transferase 1A1 gene in healthy Taiwanese. Pharmacogenetics. 2000. Huang C S, et al. PubMed
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Characterization of the uridine diphosphate-glucuronosyltransferase-catalyzing thyroid hormone glucuronidation in man. The Journal of clinical endocrinology and metabolism. 2000. Findlay K A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Variability at the uridine diphosphate glucuronosyltransferase 1A1 promoter in human populations and primates. Pharmacogenetics. 1999. Hall D, et al. PubMed
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Gilbert's syndrome is a contributory factor in prolonged unconjugated hyperbilirubinemia of the newborn. The Journal of pediatrics. 1999. Monaghan G, et al. PubMed
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(TA)8 allele in the UGT1A1 gene promoter of a Caucasian with Gilbert's syndrome. Haematologica. 1999. Iolascon A, et al. PubMed
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Neonatal hyperbilirubinemia and a common mutation of the bilirubin uridine diphosphate-glucuronosyltransferase gene in Japanese. Journal of human genetics. 1999. Akaba K, et al. PubMed
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Patellar metastasis from a lung epidermoid carcinoma. Yonsei medical journal. 1998. Aktas S, et al. PubMed
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Neonatal hyperbilirubinemia and mutation of the bilirubin uridine diphosphate-glucuronosyltransferase gene: a common missense mutation among Japanese, Koreans and Chinese. Biochemistry and molecular biology international. 1998. Akaba K, et al. PubMed
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Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7. Toxicological sciences : an official journal of the Society of Toxicology. 1998. Cheng Z, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
UGT1A1 genotypes and glucuronidation of SN-38, the active metabolite of irinotecan. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO. 1998. Ando Y, et al. PubMed
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The UGT1A1*28 allele is relatively rare in a Japanese population. Pharmacogenetics. 1998. Ando Y, et al. PubMed
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Racial variability in the UDP-glucuronosyltransferase 1 (UGT1A1) promoter: a balanced polymorphism for regulation of bilirubin metabolism?. Proceedings of the National Academy of Sciences of the United States of America. 1998. Beutler E, et al. PubMed
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Contribution of two missense mutations (G71R and Y486D) of the bilirubin UDP glycosyltransferase (UGT1A1) gene to phenotypes of Gilbert's syndrome and Crigler-Najjar syndrome type II. Biochimica et biophysica acta. 1998. Yamamoto K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic predisposition to the metabolism of irinotecan (CPT-11). Role of uridine diphosphate glucuronosyltransferase isoform 1A1 in the glucuronidation of its active metabolite (SN-38) in human liver microsomes. The Journal of clinical investigation. 1998. Iyer L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic variation in bilirubin UPD-glucuronosyltransferase gene promoter and Gilbert's syndrome. Lancet. 1996. Monaghan G, et al. PubMed
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Preclinical evaluation of CPT-11 and its active metabolite SN-38. Seminars in oncology. 1996. Lavelle F, et al. PubMed
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The genetic basis of the reduced expression of bilirubin UDP-glucuronosyltransferase 1 in Gilbert's syndrome. The New England journal of medicine. 1995. Bosma P J, et al. PubMed
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Gilbert's syndrome is caused by a heterozygous missense mutation in the gene for bilirubin UDP-glucuronosyltransferase. Human molecular genetics. 1995. Koiwai O, et al. PubMed
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Genetic heterogeneity of Crigler-Najjar syndrome type I: a study of 14 cases. Human genetics. 1994. Labrune P, et al. PubMed
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Discrimination between Crigler-Najjar type I and II by expression of mutant bilirubin uridine diphosphate-glucuronosyltransferase. The Journal of clinical investigation. 1994. Seppen J, et al. PubMed
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Identification of defect in the genes for bilirubin UDP-glucuronosyl-transferase in a patient with Crigler-Najjar syndrome type II. Biochemical and biophysical research communications. 1993. Aono S, et al. PubMed
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Identification of an A-to-G missense mutation in exon 2 of the UGT1 gene complex that causes Crigler-Najjar syndrome type 2. Genomics. 1993. Moghrabi N, et al. PubMed
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Cosegregation of intragenic markers with a novel mutation that causes Crigler-Najjar syndrome type I: implication in carrier detection and prenatal diagnosis. American journal of human genetics. 1993. Moghrabi N, et al. PubMed
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A mutation in bilirubin uridine 5'-diphosphate-glucuronosyltransferase isoform 1 causing Crigler-Najjar syndrome type II. Gastroenterology. 1993. Bosma P J, et al. PubMed
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Paracetamol glucuronidation by recombinant rat and human phenol UDP-glucuronosyltransferases. Biochemical pharmacology. 1993. Bock K W, et al. PubMed
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Mechanisms of inherited deficiencies of multiple UDP-glucuronosyltransferase isoforms in two patients with Crigler-Najjar syndrome, type I. The FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 1992. Bosma P J, et al. PubMed
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Sequence of exons and the flanking regions of human bilirubin-UDP-glucuronosyltransferase gene complex and identification of a genetic mutation in a patient with Crigler-Najjar syndrome, type I. Hepatology (Baltimore, Md.). 1992. Bosma P J, et al. PubMed

LinkOuts

Entrez Gene:
54658
OMIM:
143500
191740
218800
237900
601816
606785
UCSC Genome Browser:
NM_000463
RefSeq RNA:
NM_000463
RefSeq Protein:
NP_000454
MutDB:
UGT1A1
ALFRED:
LO000317L
HuGE:
UGT1A1
Comparative Toxicogenomics Database:
54658
ModBase:
P22309
HGNC:
12530

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