Drug/Small Molecule:
lovastatin

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with lovastatin that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105183

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 page.

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.

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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 Gene?

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.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA CYP2D6 *1 N/A N/A N/A
No VIP available CA VA CYP2D6 *5 N/A N/A N/A
No VIP available CA VA CYP2D6 *10 N/A N/A N/A
rs17238540 2298+117T>G, 2457+117T>G, 25249857T>G, 27506T>G, 74655498T>G, HMGCR:SNP 29
T > G
Intronic
No VIP available No Clinical Annotations available VA
rs2291073 14085938T>G, 21325814T>G, 226+89T>G, 46687T>G
T > G
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs2306283 14089862A>G, 21329738A>G, 388A>G, 50611A>G, Asn130Asp, SLCO1B1*1B
A > G
Missense
Asn130Asp
No VIP available No Clinical Annotations available VA
rs35599367 20493C>T, 37399159G>A, 522-191C>T, 99366316G>A, CYP3A4*22
G > A
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs3846662 1564-106A>G, 1722+45A>G, 23092A>G, 25245443A>G, 74651084A>G
A > G
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs4149015 -910G>A, 14043446G>A, 21283322G>A, 4195G>A, SLCO1B1:11187G>A, SLCO1B1:G-11187A
G > A
5' Flanking
VIP No Clinical Annotations available No Variant Annotations available
rs4149056 14091673T>C, 21331549T>C, 521T>C, 52422T>C, SLCO1B1*5, Val174Ala
T > C
Missense
Val174Ala
No VIP available No Clinical Annotations available VA
rs429358 17680159T>C, 388T>C, 45411941T>C, 7903T>C, APOE:Cys112Arg, ApoE epsilon 4, ApoE4, Cys130Arg
T > C
Missense
Cys130Arg
No VIP available No Clinical Annotations available VA
rs5925 11230881T>C, 1455T>C, 1578T>C, 1596T>C, 1836T>C, 1959T>C, 2493683T>C, 35825T>C, Val485=, Val526=, Val532=, Val612=, Val653=
T > C
Synonymous
Val526Val
No VIP available CA VA
rs662799 -620C>T, -644C>T, 116663707G>A, 20226123G>A, 4430C>T
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs688 11227602C>T, 1269C>T, 1392C>T, 1410C>T, 1650C>T, 1773C>T, 2490404C>T, 32546C>T, Asn423=, Asn464=, Asn470=, Asn550=, Asn591=, LDLR: 16730C>T
C > T
Synonymous
Asn464Asn
No VIP available CA VA
rs708272 10610487G>A, 118+279G>A, 5454G>A, 56996288G>A, A allele = B2 = not cut by TaqI, CETP:Taq1B, G allele = B1 = cut by TaqI
G > A
Intronic
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • 6 alpha-Methylcompactin
  • Lovastatina [Spanish]
  • Lovastatine [French]
  • Lovastatinum [Latin]
  • lovastatin
Trade Names
  • Altocor
  • Altoprev
  • Artein
  • Belvas
  • Cholestra
  • Closterol
  • Colevix
  • Hipolip
  • Hipovastin
  • Lestatin
  • Lipdip
  • Lipivas
  • Lipofren
  • Lovalip
  • Lovalord
  • Lovasterol
  • Lovastin
  • Lozutin
  • Mevacor
  • Mevinacor
  • Mevlor
  • Monacolin K
  • Nergadan
  • Paschol
  • Rodatin
  • Rovacor
  • Sivlor
  • Taucor
  • Tecnolip
  • Teroltrat
Brand Mixture Names

PharmGKB Accession Id:
PA450272

Description

Lovastatin is a cholesterol-lowering agent that belongs to the class of medications called statins. It was the second agent of this class discovered. It was discovered by Alfred Alberts and his team at Merck in 1978 after screening only 18 compounds over 2 weeks. The agent, also known as mevinolin, was isolated from the fungi Aspergillus terreus. Research on this compound was suddenly shut down in 1980 and the drug was not approved until 1987. Interesting, Akira Endo at Sankyo Co. (Japan) patented lovastatin isolated from Monascus ruber four months before Merck. Lovastatin was found to be 2 times more potent than its predecessor, mevastatin, the first discovered statin. Like mevastatin, lovastatin is structurally similar to hydroxymethylglutarate (HMG), a substituent of HMG-Coenzyme A (HMG-CoA), a substrate of the cholesterol biosynthesis pathway via the mevalonic acid pathway. Lovastatin is a competitive inhibitor of HMG-CoA reductase with a binding affinity 20,000 times greater than HMG-CoA. Lovastatin differs structurally from mevastatin by a single methyl group at the 6' position. Lovastatin is a prodrug that is activated by in vivo hydrolysis of the lactone ring. It, along with mevastatin, has served as one of the lead compounds for the development of the synthetic compounds used today.

Source: Drug Bank

Indication

For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia. For primary prevention of coronary heart disease and to slow progression of coronary atherosclerosis in patients with coronary heart disease.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Lovastatin is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Lovastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind with 20,000 times greater affinity than its natural substrate. The bicyclic portion of lovastatin binds to the coenzyme A portion of the active site.

Source: Drug Bank

Pharmacology

The primary cause of cardiovascular disease is atherosclerotic plaque formation. Sustained elevations of cholesterol in the blood increase the risk of cardiovascular disease. Lovastatin lowers hepatic cholesterol synthesis by competitively inhibiting HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step in the cholesterol biosynthesis pathway via the mevalonic acid pathway. Decreased hepatic cholesterol levels causes increased uptake of low density lipoprotein (LDL) cholesterol and reduces cholesterol levels in the circulation. At therapeutic doses, lovastatin decreases serum LDL cholesterol by 29-32%, increases high density lipoprotein (HDL) cholesterol by 4.6-7.3%, and decrease triglyceride levels by 2-12%. HDL cholesterol is thought to confer protective effects against CV disease, whereas high LDL and triglyceride levels are associated with higher risk of disease.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Avoid taking with grapefruit juice.|Avoid drastic changes in dietary habit.|Take with food, 50% increase in bioavailability when taken with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Undergoes first pass hydrolysis to active metabolites beta-hydroxyacid and 6'-hydroxy dervative.

Source: Drug Bank

Protein Binding

> 95%

Source: Drug Bank

Absorption

< 5%. Time to peak serum concentration is 2-4 hours.

Source: Drug Bank

Half-Life

5.3 hours

Source: Drug Bank

Toxicity

LD 50>1000 mg/kg (orally in mice)

Source: Drug Bank

Route of Elimination

Lovastatin undergoes extensive first-pass extraction in the liver, its primary site of action, with subsequent excretion of drug equivalents in the bile. 83% of the orally administered dose is excreted in bile and 10% is excreted in urine.

Source: Drug Bank

Chemical Properties

Chemical Formula

C24H36O5

Source: Drug Bank

Isomeric SMILES

CC[C@H](C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@@H]3C[C@H](CC(=O)O3)O)C

Source: OpenEye

Canonical SMILES

CC[C@H](C)C(=O)O[C@H]

Source: Drug Bank

Average Molecular Weight

404.5396

Source: Drug Bank

Monoisotopic Molecular Weight

404.256274262

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Atorvastatin/Lovastatin/Simvastatin Pathway, Pharmacokinetics
    Drug-specific representation of the candidate genes involved in transport, metabolism and clearance.

External Pathways

Links to non-PharmGKB pathways.

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

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
HDAC2 (source: Drug Bank)
HMGCR (source: Drug Bank)
ITGAL (source: Drug Bank)

Drug Interactions

Drug Description
lovastatin Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
lovastatin Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Azithromycin can possibly increase the statin toxicity (source: Drug Bank)
lovastatin Azithromycin can possibly increase the statin toxicity (source: Drug Bank)
lovastatin Bosentan could decrease the statin effect (source: Drug Bank)
lovastatin Bosentan could decrease the statin effect (source: Drug Bank)
lovastatin Decreases the effect of the statin (source: Drug Bank)
lovastatin Decreases the effect of the statin (source: Drug Bank)
lovastatin The macrolide possibly increases the statin toxicity (source: Drug Bank)
lovastatin The macrolide, clarithromycin, may increase the toxicity of the statin, lovastatin. (source: Drug Bank)
lovastatin Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
lovastatin Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
lovastatin Possible myopathy and rhabdomyolysis (source: Drug Bank)
lovastatin Possible myopathy and rhabdomyolysis (source: Drug Bank)
lovastatin Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
lovastatin The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin Increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin Increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin The macrolide possibly increases the statin toxicity (source: Drug Bank)
lovastatin The macrolide, erythromycin, may increase the toxicity of the statin, lovastatin. (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
lovastatin Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Imatinib increases the effect and toxicity of statin (source: Drug Bank)
lovastatin Imatinib increases the effect and toxicity of statin (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
acenocoumarol The statin increases the anticoagulant effect (source: Drug Bank)
acenocoumarol The statin increases the anticoagulant effect (source: Drug Bank)
amprenavir Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
amprenavir Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
anisindione The statin increases the anticoagulant effect (source: Drug Bank)
atazanavir Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
atazanavir Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
azithromycin Azithromycin can possibly increase the statin toxicity (source: Drug Bank)
azithromycin Azithromycin can possibly increase the statin toxicity (source: Drug Bank)
bezafibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
bezafibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
bosentan Bosentan could decrease the statin effect (source: Drug Bank)
bosentan Bosentan could decrease the statin effect (source: Drug Bank)
carbamazepine Carbamazepine decreases the effect of the statin (source: Drug Bank)
carbamazepine Carbamazepine decreases the effect of the statin (source: Drug Bank)
clarithromycin The macrolide possibly increases the statin toxicity (source: Drug Bank)
clarithromycin The macrolide, clarithromycin, may increase the toxicity of the statin, lovastatin. (source: Drug Bank)
colchicine Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
colchicine Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
cyclosporine Possible myopathy and rhabdomyolysis (source: Drug Bank)
cyclosporine Possible myopathy and rhabdomyolysis (source: Drug Bank)
danazol Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
darunavir Darunavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated. (source: Drug Bank)
delavirdine The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
delavirdine The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
dicumarol The statin increases the anticoagulant effect (source: Drug Bank)
dicumarol The statin increases the anticoagulant effect (source: Drug Bank)
diltiazem Diltiazem increases the effect and toxicity of the statin (source: Drug Bank)
diltiazem Diltiazem increases the effect and toxicity of the statin (source: Drug Bank)
efavirenz The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
efavirenz The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
erythromycin The macrolide possibly increases the statin toxicity (source: Drug Bank)
erythromycin The macrolide, erythromycin, may increase the toxicity of the statin, lovastatin. (source: Drug Bank)
fenofibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fenofibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fluconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fluconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fosamprenavir Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
fosamprenavir Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
gemfibrozil Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
gemfibrozil Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
imatinib Imatinib increases the effect and toxicity of statin (source: Drug Bank)
imatinib Imatinib increases the effect and toxicity of statin (source: Drug Bank)
indinavir Indinavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated. (source: Drug Bank)
itraconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
itraconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
josamycin The macrolide, josamycin, may increase the toxicity of the statin, lovastatin. (source: Drug Bank)
ketoconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
ketoconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
nefazodone Nefazodone increases the effect and toxicity of the statin (source: Drug Bank)
nefazodone Nefazodone increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nevirapine The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
nevirapine The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
niacin Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
niacin Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
rifabutin The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifabutin The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifampin The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifampin The rifamycin decreases the effect of statin drug (source: Drug Bank)
ritonavir Ritonavir increases the effect and toxicity of the statin (source: Drug Bank)
ritonavir Ritonavir increases the effect and toxicity of the statin (source: Drug Bank)
saquinavir Saquinavir may increase the effect and toxicity of lovastatin. Concomitant therapy is contraindicated. (source: Drug Bank)
tacrolimus Tacrolimus increases the effect and toxicity of the statin (source: Drug Bank)
telithromycin Telithromycin may possibly increase statin toxicity (source: Drug Bank)
telithromycin Telithromycin may possibly increase statin toxicity (source: Drug Bank)
verapamil Verapamil increases the effect and toxicity of statin (source: Drug Bank)
verapamil Verapamil increases the effect and toxicity of statin (source: Drug Bank)
warfarin The statin increases the anticoagulant effect (source: Drug Bank)
warfarin The statin increases the anticoagulant effect (source: Drug Bank)
lovastatin Nefazodone increases the effect and toxicity of the statin drug (source: Drug Bank)
lovastatin Nefazodone increases the effect and toxicity of the statin drug (source: Drug Bank)
lovastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
lovastatin Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
lovastatin This combination presents an increased risk of toxicity (source: Drug Bank)
lovastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
lovastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
lovastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
lovastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
lovastatin Telithromycin may possibly increase statin toxicity (source: Drug Bank)
lovastatin Telithromycin may reduce clearance of Lovastatin. Concomitant therapy is contraindicated. (source: Drug Bank)
lovastatin Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Lovastatin. Concomitant therapy is contraindicated. (source: Drug Bank)
lovastatin Verapamil, a moderate CYP3A4 inhibitor, may increase the serum concentration of Lovastatin by decreasing its metabolism. Avoid concurrent use if possible or reduce lovastatin dose during concomitant therapy. Monitor for changes in the therapeutic/adverse effects of Lovastatin if Verapamil is initiated, discontinued or dose changed. (source: Drug Bank)
lovastatin Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of lovastatin by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of lovastatin if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to lovastatin: 61

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP4F2. Pharmacogenetics and genomics. 2014. Alvarellos Maria 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
CYP3A4/5 combined genotype analysis for predicting statin dose requirement for optimal lipid control. Drug metabolism and drug interactions. 2013. Kitzmiller Joseph Paul, 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
CYP3A4*22: promising newly identified CYP3A4 variant allele for personalizing pharmacotherapy. Pharmacogenomics. 2013. Elens Laure, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of CYP2D6 polymorphisms on the pharmacokinetics of lovastatin in Chinese subjects. European journal of clinical pharmacology. 2012. Yin Ophelia Qi Ping, 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
Pharmacogenomics: the genetics of variable drug responses. Circulation. 2011. Roden Dan M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura 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
PharmGKB summary: methotrexate pathway. Pharmacogenetics and genomics. 2011. Mikkelsen Torben S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB: very important pharmacogene--HMGCR. Pharmacogenetics and genomics. 2011. Medina Marisa Wong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
KCNH2 pharmacogenomics summary. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Intronic polymorphism in CYP3A4 affects hepatic expression and response to statin drugs. The pharmacogenomics journal. 2010. Wang D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB very important pharmacogene: SLCO1B1. Pharmacogenetics and genomics. 2010. Oshiro Connie, 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
Common sequence variants in pharmacodynamic and pharmacokinetic pathway-related genes conferring LDL cholesterol response to statins. Pharmacogenomics. 2010. Chien Kuo-Liong, 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
Transporter pharmacogenetics and statin toxicity. Clinical pharmacology and therapeutics. 2010. Niemi M. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Warfarin interactions with substances listed in drug information compendia and in the FDA-approved label for warfarin sodium. Clinical pharmacology and therapeutics. 2009. Anthony 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
The pharmacogenetics of statin therapy: when the body aches, the mind will follow. Journal of the American College of Cardiology. 2009. Rossi Joseph 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
Drug discovery and natural products: end of an era or an endless frontier?. Science (New York, N.Y.). 2009. Li Jesse W-H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, 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
Statin regulation of CYP3A4 and CYP3A5 expression. Pharmacogenomics. 2009. Willrich Maria Alice Vieira, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of apolipoprotein A5 variants on statin treatment efficacy. Pharmacogenomics. 2009. Hubacek Jaroslav A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
A paucimorphic variant in the HMG-CoA reductase gene is associated with lipid-lowering response to statin treatment in diabetes: a GoDARTS study. Pharmacogenetics and genomics. 2008. Donnelly Louise 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
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Genetic variation at the LDL receptor and HMG-CoA reductase gene loci, lipid levels, statin response, and cardiovascular disease incidence in PROSPER. Atherosclerosis. 2008. Polisecki Eliana, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Over-the-counter sales of statins and other drugs for asymptomatic conditions. The New England journal of medicine. 2008. Tinetti Mary E. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Variation in the 3-hydroxyl-3-methylglutaryl coenzyme a reductase gene is associated with racial differences in low-density lipoprotein cholesterol response to simvastatin treatment. Circulation. 2008. Krauss Ronald M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Genetic analysis of fluvastatin response and dyslipidemia in renal transplant recipients. Journal of lipid research. 2007. Singer Jonathan B, 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
Zetia: inhibition of Niemann-Pick C1 Like 1 (NPC1L1) to reduce intestinal cholesterol absorption and treat hyperlipidemia. Journal of atherosclerosis and thrombosis. 2007. Davis Harry R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Effect of HMGCoA reductase inhibitors on cytochrome P450 expression in endothelial cell line. Journal of cardiovascular pharmacology. 2007. Bertrand-Thiebault Céline, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Regulation of human cytochrome P450 4F2 expression by sterol regulatory element-binding protein and lovastatin. The Journal of biological chemistry. 2007. Hsu Mei-Hui, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. The Journal of pharmacology and experimental therapeutics. 2007. Faucette Stephanie R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, 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
Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clinical pharmacology and therapeutics. 2006. Neuvonen Pertti J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs. The Journal of pharmacology and experimental therapeutics. 2006. Katchman Alexander N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug metabolism and disposition: the biological fate of chemicals. 2005. Chen Cuiping, et al. PubMed
An association study of 43 SNPs in 16 candidate genes with atorvastatin response. The pharmacogenomics journal. 2005. Thompson J F, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Pharmacogenetic study of statin therapy and cholesterol reduction. JAMA : the journal of the American Medical Association. 2004. Chasman Daniel I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Lipid-lowering response to statins is affected by CYP3A5 polymorphism. Pharmacogenetics. 2004. Kivistö Kari T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, 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
The discovery of ezetimibe: a view from outside the receptor. Journal of medicinal chemistry. 2004. Clader John W. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus 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
Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharmaceutics & drug disposition. 2000. Cohen L H, 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
Inhibition of small G proteins of the rho family by statins or clostridium difficile toxin B enhances cytokine-mediated induction of NO synthase II. British journal of pharmacology. 2000. Hausding M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. The Journal of biological chemistry. 1999. Hsiang B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. The Journal of clinical investigation. 1998. Lehmann J M, et al. PubMed
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Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0378-6510-91
DrugBank:
DB00227
PDB:
803
ChEBI:
40303
KEGG Compound:
C07074
KEGG Drug:
D00359
PubChem Compound:
53232
PubChem Substance:
191104
46508223
Drugs Product Database (DPD):
2243127
ChemSpider:
48085
HET:
803
Therapeutic Targets Database:
DAP000551
FDA Drug Label at DailyMed:
73f92f9b-3715-4699-ba60-1ffecd677e23

Clinical Trials

These are trials that mention lovastatin and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.