Chemical: Drug
fludarabine

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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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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.

List of all variant annotations for fludarabine

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2B6 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *6 N/A N/A N/A
No VIP available No VIP available VA CYP2B6 *6A N/A N/A N/A
No VIP available CA VA
rs11231825 NC_000011.10:g.64592802T>C, NC_000011.9:g.64360274T>C, NG_008110.1:g.6993T>C, NM_001276326.1:c.426T>C, NM_001276327.1:c.426T>C, NM_144585.3:c.426T>C, NM_153378.2:c.-83T>C, NP_001263255.1:p.His142=, NP_001263256.1:p.His142=, NP_653186.2:p.His142=, XM_005273740.1:c.426T>C, XM_005273741.1:c.426T>C, XM_005273742.1:c.426T>C, XM_005273743.1:c.426T>C, XM_005273744.1:c.426T>C, XM_005273745.1:c.426T>C, XM_005273746.1:c.426T>C, XM_005273747.1:c.-764T>C, XM_006718430.2:c.426T>C, XM_006718431.2:c.321T>C, XP_005273797.1:p.His142=, XP_005273798.1:p.His142=, XP_005273799.1:p.His142=, XP_005273800.1:p.His142=, XP_005273801.1:p.His142=, XP_005273802.1:p.His142=, XP_005273803.1:p.His142=, XP_006718493.1:p.His142=, XP_006718494.1:p.His107=, rs17846504, rs17859573, rs60376821
T > C
SNP
H142H
No VIP available CA VA
rs1801157
C > T
SNP
No VIP available No Clinical Annotations available VA
rs1826909 NC_000004.11:g.100217743C>T, NC_000004.12:g.99296586C>T, NR_037884.1:n.4161-3713C>T, rs17512416, rs4525982, rs61683245
C > T
SNP
No VIP available CA VA
rs2070673 NC_000010.10:g.135340567A>T, NC_000010.11:g.133527063A>T, NG_008383.1:g.4701A>T, NM_000773.3:c.-333A>T, XM_005252665.1:c.21+190A>T
A > T
SNP
No VIP available CA VA
rs2302948 NC_000019.10:g.48592808C>T, NC_000019.9:g.49096065C>T, NG_029063.1:g.45637C>T, NM_004605.2:c.592C>T, NM_177973.1:c.637C>T, NP_004596.2:p.Leu198=, NP_814444.1:p.Leu213=, XM_005259182.1:c.205C>T, XM_005259182.2:c.205C>T, XP_005259239.1:p.Leu69=, rs59383755
C > T
SNP
L198L
No VIP available CA VA
rs2515641 NC_000010.10:g.135351362T>C, NC_000010.11:g.133537858C>T, NG_008383.1:g.15496C=, NG_008383.1:g.15496C>T, NM_000773.3:c.1263C=, NM_000773.3:c.1263C>T, NP_000764.1:p.Phe421=, XM_005252665.1:c.1323T>C, XP_005252722.1:p.Phe441=, rs17012766, rs60244712
T > C
SNP
F421F
No VIP available CA VA
rs4149056 NC_000012.11:g.21331549T>C, NC_000012.12:g.21178615T>C, NG_011745.1:g.52422T>C, NM_006446.4:c.521T>C, NP_006437.3:p.Val174Ala, rs52816141, rs60037639
T > C
SNP
V174A
No VIP available No Clinical Annotations available VA
rs6811453 NC_000004.11:g.100194977G>A, NC_000004.12:g.99273820G>A, NR_037884.1:n.3790-12975G>A, XR_244675.1:n.691-305G>A
G > A
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • FAMP
  • Fludarabine 5'-monophosphate
  • Fludarabine monophosphate
  • Fludarabine phosphate
Trade Names
  • Fludara
  • Fludura
Brand Mixture Names

PharmGKB Accession Id

PA449655

Type(s):

Drug

Description

Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a chemotherapy drug used in the treatment of hematological malignancies. Wikipedia

Source: Drug Bank

Indication

For the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to or whose disease has progressed during treatment with at least one standard alkylating-agent containing regimen

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis. The mechanism of action of this antimetabolite is not completely characterized and may be multi-faceted.

Source: Drug Bank

Pharmacology

Fludarabine is a chemotherapy drug used in the treatment of chronic lymphocytic leukemia. It acts at DNA polymerase alpha, ribonucleotide reductase and DNA primase, results in the inhibition of DNA synthesis, and destroys the cancer cells.

Source: Drug Bank

Food Interaction

Food slightly increases product bioavailability.|Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Protein Binding

19-29%

Source: Drug Bank

Absorption

Bioavailability is 55% following oral administration.

Source: Drug Bank

Half-Life

20 hours

Source: Drug Bank

Chemical Properties

Chemical Formula

C10H13FN5O7P

Source: Drug Bank

Isomeric SMILES

c1nc2c(nc(nc2n1[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)F)N

Source: OpenEye

Canonical SMILES

NC1=C2N=CN([C@@H]3O[C@H]

Source: Drug Bank

Average Molecular Weight

365.2117

Source: Drug Bank

Monoisotopic Molecular Weight

365.053662512

Source: Drug Bank

SMILES

NC1=C2N=CN([C@@H]3O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]3O)C2=NC(F)=N1

Source: Drug Bank

InChI String

InChI=1S/C10H13FN5O7P/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(18)5(17)3(23-9)1-22-24(19,20)21/h2-3,5-6,9,17-18H,1H2,(H2,12,14,15)(H2,19,20,21)/t3-,5-,6+,9-/m1/s1

Source: Drug Bank

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
ADA (source: Drug Bank )
BCL2 (source: Drug Bank )
DCK (source: Drug Bank )
POLA1 (source: Drug Bank )
RRM1 (source: Drug Bank )
STAT1 (source: Drug Bank )

Drug Interactions

Interaction Description
dipyridamole - fludarabine Decreases the effect of fludarabine (source: Drug Bank )
dipyridamole - fludarabine Decreases the effect of fludarabine (source: Drug Bank )
fludarabine - dipyridamole Dipyridamole decreases the effect of fludarabine (source: Drug Bank )
fludarabine - dipyridamole Dipyridamole decreases the effect of fludarabine (source: Drug Bank )
fludarabine - pentostatin Unacceptable pulmonary toxicity (source: Drug Bank )
fludarabine - pentostatin Unacceptable pulmonary toxicity (source: Drug Bank )
trastuzumab - fludarabine Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank )

Curated Information ?

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

May Treat
Contraindicated With

Publications related to fludarabine: 10

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Dual role of the CXCL12 polymorphism in patients with chronic lymphocytic leukemia. HLA. 2016. Butrym 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
The rate of in vitro fludarabine-induced peripheral blood and bone marrow cell apoptosis may predict the chemotherapy outcome in patients with chronic lymphocytic leukemia. European journal of clinical pharmacology. 2015. Podhorecka Monika, 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
Pharmacokinetics and safety of subcutaneous rituximab plus fludarabine and cyclophosphamide for patients with chronic lymphocytic leukaemia. British journal of clinical pharmacology. 2015. Assouline Sarit, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
CYP2B6*6 is an independent determinant of inferior response to fludarabine plus cyclophosphamide in chronic lymphocytic leukemia. Blood. 2013. Johnson Gillian G, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Profiling of drug-metabolizing enzymes/transporters in CD33+ acute myeloid leukemia patients treated with Gemtuzumab-Ozogamicin and Fludarabine, Cytarabine and Idarubicin. The pharmacogenomics journal. 2012. Iacobucci I, 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
Pharmacogenomic characterization of US FDA-approved cytotoxic drugs. Pharmacogenomics. 2011. Peters Eric J, 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 transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010. Errasti-Murugarren Ekaitz, 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
Ofatumumab. Nature reviews. Drug discovery. 2010. Keating Michael J, 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
Chronic lymphocytic leukaemia. Lancet. 2008. Dighiero G, 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 genetic variants in the human concentrative nucleoside transporter 3 (CNT3; SLC28A3). The pharmacogenomics journal. 2005. Badagnani I, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0024-5820-15
DrugBank:
DB01073
KEGG Drug:
D01907
PubChem Compound:
30751
PubChem Substance:
46507525
7848969
Drugs Product Database (DPD):
2246226
ChemSpider:
28532
Therapeutic Targets Database:
DAP000567
FDA Drug Label at DailyMed:
30bac07f-86bd-4a03-8ea1-7ab2d42d3ea3

Clinical Trials

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

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

Common Searches

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Sources for PharmGKB drug information: DrugBank, PubChem.