Chemical: Prodrug
lamivudine

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



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 lamivudine

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 HLA-B *35:05:01 N/A N/A N/A
No VIP available No VIP available VA HLA-B *40:01:01 N/A N/A N/A
No VIP available CA VA
rs1045642 NC_000007.13:g.87138645A>G, NC_000007.14:g.87509329A>G, NG_011513.1:g.208920T>C, NM_000927.4:c.3435T>C, NP_000918.2:p.Ile1145=, rs10239679, rs11568726, rs117328163, rs17210003, rs2229108, rs386513066, rs60023214, rs9690664
A > G
SNP
I1145I
No VIP available No Clinical Annotations available VA
rs11568695 NC_000013.10:g.95696540C>T, NC_000013.11:g.95044286C>T, NM_001301829.1:c.3468G>A, NM_005845.4:c.3609G>A, NP_001288758.1:p.Ala1156=, NP_005836.2:p.Ala1203=, XM_005254025.1:c.3480G>A, XM_005254025.2:c.3480G>A, XM_005254026.1:c.3468G>A, XM_005254027.1:c.3384G>A, XM_006719914.1:c.3519G>A, XM_011521047.1:c.3060G>A, XP_005254082.1:p.Ala1160=, XP_005254083.1:p.Ala1156=, XP_005254084.1:p.Ala1128=, XP_006719977.1:p.Ala1173=, XP_011519349.1:p.Ala1020=, rs57205843
C > T
SNP
A1156A
No VIP available No Clinical Annotations available VA
rs145450955 NC_000006.11:g.160671651G>A, NC_000006.12:g.160250619G>A, NM_003058.3:c.602C>T, NP_003049.2:p.Thr201Met
G > A
SNP
T201M
No VIP available No Clinical Annotations available VA
rs1517618 NC_000015.10:g.92104415G>C, NC_000015.9:g.92647645G>C, NM_001145044.1:c.882G>C, NM_013272.3:c.882G>C, NP_001138516.1:p.Glu294Asp, NP_037404.2:p.Glu294Asp, XM_005254889.1:c.882G>C, XM_005254890.1:c.708G>C, XM_005254891.1:c.537G>C, XM_011521456.1:c.708G>C, XM_011521457.1:c.882G>C, XP_005254946.1:p.Glu294Asp, XP_005254947.1:p.Glu236Asp, XP_005254948.1:p.Glu179Asp, XP_011519758.1:p.Glu236Asp, XP_011519759.1:p.Glu294Asp, XR_429450.2:n.802G>C, XR_931795.1:n.972G>C, XR_931796.1:n.972G>C, rs17519193, rs17844850, rs17857564, rs52834221, rs60307785
G > C
SNP
E294D
No VIP available No Clinical Annotations available VA
rs2032582 NC_000007.13:g.87160618A>C, NC_000007.13:g.87160618A>T, NC_000007.14:g.87531302A>C, NC_000007.14:g.87531302A>T, NG_011513.1:g.186947T>A, NG_011513.1:g.186947T>G, NM_000927.4:c.2677T>A, NM_000927.4:c.2677T>G, NP_000918.2:p.Ser893Ala, NP_000918.2:p.Ser893Thr, rs10228331, rs2229106, rs386553610, rs57135550, rs9641018
A > C
SNP
S893A
No VIP available CA VA
rs212091 NC_000016.10:g.16142793T>C, NC_000016.9:g.16236650T>C, NG_028268.1:g.198217T>C, NM_004996.3:c.*1512T>C, NT_187607.1:g.1800685T>C, XM_005255326.1:c.*1512T>C, XM_005255327.1:c.*1512T>C, XM_005255328.1:c.*1512T>C, XM_005255329.1:c.*1512T>C, XM_011522497.1:c.*1512T>C, XM_011522498.1:c.*1512T>C, XR_933134.1:n.-960T>C, XR_951923.1:n.-989T>C, rs16967633, rs212647, rs3186999, rs58366070
T > C
SNP
No VIP available No Clinical Annotations available VA
rs2740574 NC_000007.13:g.99382096C>T, NC_000007.14:g.99784473C>T, NG_008421.1:g.4713G>A, NM_001202855.2:c.-392G>A, NM_017460.5:c.-392G>A, XM_011515841.1:c.-392G>A, XM_011515842.1:c.-392G>A, rs3176920, rs36231114, rs59393892
C > T
SNP
No VIP available No Clinical Annotations available VA
rs28399433 NC_000019.10:g.40850474A>C, NC_000019.9:g.41356379A>C, NG_008377.1:g.4974T>G, NM_000762.5:c.-48T>G, XM_005258568.1:c.-48T>G, rs386508632, rs58538938
A > C
SNP
No VIP available No Clinical Annotations available VA
rs28399499 NC_000019.10:g.41012316T>C, NC_000019.9:g.41518221T>C, NG_007929.1:g.26018T>C, NM_000767.4:c.983T>C, NP_000758.1:p.Ile328Thr, XM_005258569.1:c.983T>C, XM_005258569.3:c.983T>C, XM_005258570.1:c.983T>C, XM_005258571.1:c.383T>C, XM_006723050.2:c.983T>C, XM_011526546.1:c.983T>C, XM_011526547.1:c.983T>C, XM_011526548.1:c.503T>C, XM_011526549.1:c.392T>C, XM_011526550.1:c.383T>C, XP_005258626.1:p.Ile328Thr, XP_005258627.1:p.Ile328Thr, XP_005258628.1:p.Ile128Thr, XP_006723113.1:p.Ile328Thr, XP_011524848.1:p.Ile328Thr, XP_011524849.1:p.Ile328Thr, XP_011524850.1:p.Ile168Thr, XP_011524851.1:p.Ile131Thr, XP_011524852.1:p.Ile128Thr
T > C
SNP
I328T
No VIP available No Clinical Annotations available VA
rs3743527 NC_000016.10:g.16141824C>T, NC_000016.9:g.16235681C>T, NG_028268.1:g.197248C>T, NM_004996.3:c.*543C>T, NT_187607.1:g.1799715C>T, XM_005255326.1:c.*543C>T, XM_005255327.1:c.*543C>T, XM_005255328.1:c.*543C>T, XM_005255329.1:c.*543C>T, XM_011522497.1:c.*543C>T, XM_011522498.1:c.*543C>T, XR_933134.1:n.-1929C>T, XR_951923.1:n.-1959C>T, rs386585277, rs57742638
C > T
SNP
No VIP available No Clinical Annotations available VA
rs3745274 NC_000019.10:g.41006936G>T, NC_000019.9:g.41512841G>T, NG_007929.1:g.20638G>T, NM_000767.4:c.516G>T, NP_000758.1:p.Gln172His, XM_005258569.1:c.516G>T, XM_005258569.3:c.516G>T, XM_005258570.1:c.516G>T, XM_005258571.1:c.364+2490G>T, XM_006723050.2:c.516G>T, XM_011526546.1:c.516G>T, XM_011526547.1:c.516G>T, XM_011526548.1:c.484+2490G>T, XM_011526549.1:c.-75-1G>T, XM_011526550.1:c.364+2490G>T, XP_005258626.1:p.Gln172His, XP_005258627.1:p.Gln172His, XP_006723113.1:p.Gln172His, XP_011524848.1:p.Gln172His, XP_011524849.1:p.Gln172His, rs56308434, rs57685583
G > T
SNP
Q172H
No VIP available No Clinical Annotations available VA
rs3842 NC_000007.13:g.87133366T>C, NC_000007.14:g.87504050T>C, NG_011513.1:g.214199A>G, NM_000927.4:c.*193A>G, rs3747805, rs60395104
T > C
SNP
No VIP available No Clinical Annotations available VA
rs4803419 NC_000019.10:g.41006887C>T, NC_000019.9:g.41512792C>T, NG_007929.1:g.20589C>T, NM_000767.4:c.485-18C>T, XM_005258569.1:c.485-18C>T, XM_005258569.3:c.485-18C>T, XM_005258570.1:c.485-18C>T, XM_005258571.1:c.364+2441C>T, XM_006723050.2:c.485-18C>T, XM_011526546.1:c.485-18C>T, XM_011526547.1:c.485-18C>T, XM_011526548.1:c.484+2441C>T, XM_011526549.1:c.-75-50C>T, XM_011526550.1:c.364+2441C>T, rs60830962
C > T
SNP
No VIP available No Clinical Annotations available VA
rs628031 NC_000006.11:g.160560845A>G, NC_000006.12:g.160139813A>G, NM_003057.2:c.1222A>G, NM_153187.1:c.1222A>G, NP_003048.1:p.Met408Val, NP_694857.1:p.Met408Val, XM_005267102.1:c.1222A>G, XM_005267102.3:c.1222A>G, XM_005267103.1:c.1222A>G, XM_005267104.1:c.646A>G, XM_005267104.3:c.646A>G, XM_005267105.1:c.646A>G, XM_005267105.3:c.646A>G, XM_006715552.1:c.1222A>G, XM_011536074.1:c.646A>G, XP_005267159.1:p.Met408Val, XP_005267160.1:p.Met408Val, XP_005267161.1:p.Met216Val, XP_005267162.1:p.Met216Val, XP_006715615.1:p.Met408Val, XP_011534376.1:p.Met216Val, rs1086277, rs17202481, rs60990824
A > G
SNP
M408V
No VIP available No Clinical Annotations available VA
rs8175347
(TA)6 > (TA)5
(TA)6 > (TA)7
(TA)6 > (TA)8
microsatellite
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Lamivudine [Usan:Ban:Inn]
  • lamivudine
Trade Names
  • 3TC
  • Epivir
  • Epivir-HBV
  • Epzicom
  • Hepitec
  • Heptovir
  • Zeffix
Brand Mixture Names
  • Combivir (Lamivudine + Zidovudine)
  • Kivexa (Abacavir (Abacavir Sulfate) + Lamivudine)
  • Trizivir (Abacavir (Abacavir Sulfate) + Lamivudine + Zidovudine)

PharmGKB Accession Id

PA450163

Type(s):

Prodrug

Description

A reverse transcriptase inhibitor and zalcitabine analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV).

Source: Drug Bank

Indication

For the treatment of HIV infection and chronic hepatitis B (HBV).

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Lamivudine is a synthetic nucleoside analogue and is phosphorylated intracellularly to its active 5'-triphosphate metabolite, lamivudine triphosphate (L-TP). This nucleoside analogue is incorporated into viral DNA by HIV reverse transcriptase and HBV polymerase, resulting in DNA chain termination.

Source: Drug Bank

Pharmacology

Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV). Lamivudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.

Source: Drug Bank

Food Interaction

Take without regard to meals. Food does not decrease the extent of absorption, but it decreases the Cmax by slowing the rate of absorption.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

The only detected metabolite of lamivudine is trans-sulfoxide.

Source: Drug Bank

Protein Binding

36%

Source: Drug Bank

Absorption

Lamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in adults is 86% +/- 16% for the tablet and 87% +/- 13% for the oral solution.

Source: Drug Bank

Half-Life

5 to 7 hours

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

The primary routes of elimination of abacavir are metabolism by alcohol dehydrogenase to form the 5'-carboxylic acid and glucuronyl transferase to form the 5'-glucuronide. Lamivudine is excreted in human breast milk and into the milk of lactating rats.

Source: Drug Bank

Chemical Properties

Chemical Formula

C8H11N3O3S

Source: Drug Bank

Canonical SMILES

NC1=NC(=O)N(C=C1)[C@@H]1CS[C@H]

Source: Drug Bank

Average Molecular Weight

229.256

Source: Drug Bank

Monoisotopic Molecular Weight

229.052111923

Source: Drug Bank

SMILES

NC1=NC(=O)N(C=C1)[C@@H]1CS[C@H](CO)O1

Source: Drug Bank

InChI String

InChI=1S/C8H11N3O3S/c9-5-1-2-11(8(13)10-5)6-4-15-7(3-12)14-6/h1-2,6-7,12H,3-4H2,(H2,9,10,13)/t6-,7+/m0/s1

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Lamivudine Pathway, Pharmacokinetics/Pharmacodynamics
    Representation of candidate genes involved in the metabolism of lamivudine and its mechanism of antiviral action.

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 Interactions

Interaction Description
valganciclovir - lamivudine The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Lamivudine, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended. (source: Drug Bank)
valganciclovir - lamivudine The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Lamivudine, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended. (source: Drug Bank)
zalcitabine - lamivudine Lamivudine may reduce the efficacy of zalcitabine. Combination therapy is not recommended. (source: Drug Bank)

Curated Information ?

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

May Treat
Contraindicated With

Publications related to lamivudine: 20

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Incidence and predictors of regimen-modification from first-line antiretroviral therapy in Thailand: a cohort study. BMC infectious diseases. 2014. Tsuchiya Naho, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Functional CYP2B6 variants and virologic response to an efavirenz-containing regimen in Port-au-Prince, Haiti. The Journal of antimicrobial chemotherapy. 2014. Haas David 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
Dependence of efavirenz- and rifampicin-isoniazid-based antituberculosis treatment drug-drug interaction on CYP2B6 and NAT2 genetic polymorphisms: ANRS 12154 study in Cambodia. The Journal of infectious diseases. 2014. Bertrand Julie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
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
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mitochondrial DNA Variation and Changes in Adiponectin and Endothelial Function in HIV-Infected Adults After Antiretroviral Therapy Initiation. AIDS research and human retroviruses. 2013. Hulgan Todd, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
ABCB1 and ABCC1 variants associated with virological failure of first-line protease inhibitors antiretroviral regimens in Northeast Brazil patients. Journal of clinical pharmacology. 2013. Coelho Antonio V C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Effects of OCT2 c.602C > T genetic variant on the pharmacokinetics of lamivudine. Xenobiotica; the fate of foreign compounds in biological systems. 2013. Choi Chang-Ik, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
ABCB1 variation and treatment response in AIDS patients: initial results of the Henan cohort. PloS one. 2013. Zhu 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
Potential effect of pharmacogenetics on maternal, fetal and infant antiretroviral drug exposure during pregnancy and breastfeeding. Pharmacogenomics. 2012. Olagunju Adeniyi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Pharmacogenetic and pharmacokinetic aspects of CYP3A induction by efavirenz in HIV patients. The pharmacogenomics journal. 2012. Habtewold 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 Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological reviews. 2012. Michaud Veronique, 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
HIV-1 antiretroviral drug therapy. Cold Spring Harbor perspectives in medicine. 2012. Arts 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
Nuclear receptor-mediated induction of CYP450 by antiretrovirals: functional consequences of NR1I2 (PXR) polymorphisms and differential prevalence in whites and sub-Saharan Africans. Journal of acquired immune deficiency syndromes (1999). 2010. Svärd Jenny, 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 VA No VIP available No VIP available
Presence of the CYP2B6 516G> T polymorphism, increased plasma Efavirenz concentrations and early neuropsychiatric side effects in South African HIV-infected patients. AIDS research and therapy. 2010. Gounden Verena, 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
Whole genome expression profiling of hepatitis B virus-transfected cell line reveals the potential targets of anti-HBV drugs. The pharmacogenomics journal. 2008. Ding X R, 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
Age-dependent pharmacokinetics of lamivudine in HIV-infected children. Clinical pharmacology and therapeutics. 2007. Burger D M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Pharmacogenetic characteristics of indinavir, zidovudine, and lamivudine therapy in HIV-infected adults: a pilot study. Journal of acquired immune deficiency syndromes (1999). 2006. Anderson Peter 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
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
Efavirenz. Drugs. 1998. Adkins J C, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0173-0742-00
DrugBank:
DB00709
KEGG Compound:
C07065
KEGG Drug:
D00353
PubChem Compound:
60825
PubChem Substance:
197069
46507855
Drugs Product Database (DPD):
2239194
BindingDB:
50046287
ChemSpider:
54812
Therapeutic Targets Database:
DAP000167
FDA Drug Label at DailyMed:
6a821a47-e1c1-4291-ac8f-1c2a0f58142a

Clinical Trials

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

No trials found.

Common Searches

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Sources for PharmGKB drug information: DrugBank, PubChem.