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Identification
NameLamivudine
Accession NumberDB00709  (APRD00681)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionA 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).
Structure
Thumb
Synonyms
(-)-1-((2R,5S)-2-(Hydroxymethyl)-1,3-oxathiolan-5-yl)cytosine
(-)-2'-Deoxy-3'-thiacytidine
2',3'-Dideoxy-3'-thiacytidine
3'-Thia-2',3'-dideoxycytidine
3TC
beta-L-2',3'-Dideoxy-3'-thiacytidine
beta-L-3'-Thia-2',3'-dideoxycytidine
Epivir
Lamivudin
Lamivudina
Lamivudine
Lamivudinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
3tctablet150 mgoralViiv Healthcare Ulc1995-12-31Not applicableCanada
3tctablet300 mgoralViiv Healthcare Ulc2003-09-09Not applicableCanada
3tcsolution10 mgoralViiv Healthcare Ulc1995-12-31Not applicableCanada
Auro-lamivudinetablet300 mgoralAuro Pharma Inc2013-10-16Not applicableCanada
Auro-lamivudinetablet150 mgoralAuro Pharma Inc2013-10-16Not applicableCanada
Epivirtablet, film coated150 mg/1oralVii V Healthcare Company2010-10-04Not applicableUs
EpivirFilm-coated tablet300 mgOral useVii V Healthcare Uk Limited 1996-08-08Not applicableEu
Epivirtablet, film coated300 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Epivirtablet, film coated150 mg/1oralREMEDYREPACK INC.2013-03-15Not applicableUs
Epivirtablet, film coated300 mg/1oralVii V Healthcare Company2010-10-04Not applicableUs
Epivirtablet, film coated150 mg/1oralA S Medication Solutions2010-10-04Not applicableUs
EpivirFilm-coated tablet150 mgOral useVii V Healthcare Uk Limited 1996-08-08Not applicableEu
Epivirtablet, film coated150 mg/1oralREMEDYREPACK INC.2011-07-13Not applicableUs
EpivirFilm-coated tablet150 mgOral useVii V Healthcare Uk Limited 1996-08-08Not applicableEu
Epivirsolution10 mg/mLoralVii V Healthcare Company2010-10-04Not applicableUs
Epivirtablet, film coated150 mg/1oralKAISER FOUNDATION HOSPITALS2011-03-15Not applicableUs
Epivirtablet, film coated150 mg/1oralPhysicians Total Care, Inc.1995-12-01Not applicableUs
EpivirFilm-coated tablet300 mgOral useVii V Healthcare Uk Limited 1996-08-08Not applicableEu
Epivirtablet300 mg/1oralREMEDYREPACK INC.2011-08-30Not applicableUs
EpivirOral solution10 mg/mlOral useVii V Healthcare Uk Limited 1996-08-08Not applicableEu
Epivirtablet, film coated150 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Epivirtablet, film coated150 mg/1oralRebel Distributors Corp1995-11-21Not applicableUs
Epivirtablet, film coated300 mg/1oralPhysicians Total Care, Inc.2007-09-28Not applicableUs
Epivir Hbvtablet, film coated100 mg/1oralGlaxo Smith Kline Llc1998-12-17Not applicableUs
Epivir Hbvsolution5 mg/mLoralGlaxo Smith Kline Llc1998-12-23Not applicableUs
Epivir Hbvtablet, film coated100 mg/1oralState of Florida DOH Central Pharmacy2014-01-01Not applicableUs
Heptovirsolution5 mgoralGlaxosmithkline Inc1999-03-30Not applicableCanada
Heptovirtablet100 mgoralGlaxosmithkline Inc1998-12-02Not applicableCanada
Lamivudinetablet, film coated100 mg/1oralPrasco Laboratories2014-09-05Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-lamivudinetablet150 mgoralApotex Inc2012-05-18Not applicableCanada
Apo-lamivudinetablet300 mgoralApotex Inc2012-05-18Not applicableCanada
Apo-lamivudine Hbvtablet100 mgoralApotex Inc2012-09-21Not applicableCanada
Lamivudinetablet, film coated150 mg/1oralAv Pak2015-07-30Not applicableUs
Lamivudinetablet, film coated150 mg/1oralLupin Pharmaceuticals, Inc.2015-03-25Not applicableUs
Lamivudinetablet, film coated100 mg/1oralKAISER FOUNDATION HOSPITALS2014-05-29Not applicableUs
Lamivudinetablet, film coated150 mg/1oralApotex Corp.2011-12-02Not applicableUs
Lamivudinetablet, film coated150 mg/1oralMylan Pharmaceuticals Inc.2016-03-28Not applicableUs
Lamivudinetablet, film coated300 mg/1oralREMEDYREPACK INC.2016-01-19Not applicableUs
Lamivudinetablet, film coated300 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Lamivudinetablet, film coated150 mg/1oralCamber Pharmaceuticals, Inc.2014-01-06Not applicableUs
Lamivudinetablet, film coated150 mg/1oralAurobindo Pharma Limited2011-11-17Not applicableUs
Lamivudinetablet, film coated300 mg/1oralAv Pak2015-07-30Not applicableUs
Lamivudinetablet, film coated300 mg/1oralLupin Pharmaceuticals, Inc.2015-03-25Not applicableUs
Lamivudinetablet, film coated300 mg/1oralMylan Pharmaceuticals Inc.2016-03-28Not applicableUs
Lamivudinetablet, film coated100 mg/1oralKAISER FOUNDATION HOSPITALS2015-03-20Not applicableUs
Lamivudinetablet, film coated300 mg/1oralApotex Corp.2011-12-02Not applicableUs
Lamivudinetablet, film coated150 mg/1oralGolden State Medical Supply, Inc.2011-12-02Not applicableUs
Lamivudinesolution10 mg/mLoralMarlex Pharmaceuticals Inc2016-02-01Not applicableUs
Lamivudinetablet, film coated300 mg/1oralCamber Pharmaceuticals, Inc.2014-01-06Not applicableUs
Lamivudinetablet, film coated300 mg/1oralAurobindo Pharma Limited2011-11-17Not applicableUs
Lamivudinetablet, film coated300 mg/1oralREMEDYREPACK INC.2013-03-28Not applicableUs
Lamivudinetablet, film coated150 mg/1oralREMEDYREPACK INC.2015-05-30Not applicableUs
Lamivudinetablet, film coated100 mg/1oralMylan Pharmaceuticals Inc.2015-01-09Not applicableUs
Lamivudinetablet, film coated300 mg/1oralGolden State Medical Supply, Inc.2011-12-02Not applicableUs
Lamivudinetablet, film coated150 mg/1oralREMEDYREPACK INC.2013-04-11Not applicableUs
Lamivudinetablet, film coated150 mg/1oralAmerican Health Packaging2012-02-01Not applicableUs
Lamivudinetablet, film coated150 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Lamivudinetablet, film coated150 mg/1oralbryant ranch prepack2011-11-17Not applicableUs
Lamivudinetablet, film coated100 mg/1oralCamber Pharmaceuticals, Inc.2014-01-02Not applicableUs
Lamivudinetablet, film coated100 mg/1oralApotex Corp.2014-01-03Not applicableUs
Lamivudinesolution10 mg/mLoralSilarx Pharmaceuticals, Inc.2014-01-30Not applicableUs
Lamivudine and Zidovudinetablet, film coated150 mg/1oralREMEDYREPACK INC.2013-04-11Not applicableUs
Lamivudine TevaFilm-coated tablet100 mgOral useTeva B.V.2009-10-23Not applicableEu
Lamivudine TevaFilm-coated tablet100 mgOral useTeva B.V.2009-10-23Not applicableEu
Lamivudine TevaFilm-coated tablet100 mgOral useTeva B.V.2009-10-23Not applicableEu
Lamivudine TevaFilm-coated tablet100 mgOral useTeva B.V.2009-10-23Not applicableEu
Lamivudine TevaFilm-coated tablet100 mgOral useTeva B.V.2009-10-23Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet300 mgOral useTeva B.V.  2009-12-10Not applicableEu
Lamivudine Teva Pharma B.V.Film-coated tablet150 mgOral useTeva B.V.  2009-12-10Not applicableEu
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AmilitrapDosa
AntihebMebiphar
AvilamBeximco
AvolamRanbaxy Laboratories
Epivir-HBVGlaxoSmithKline
FlamivudFlamingo Pharmacueticals
GanvirelIvax
HepavirSquare
HepitecGlaxoSmithKline
HeptavirHetero
HeptodinGlaxoSmithKline
HeptodineGlaxoSmithKline
LamdaCadila
LamibergenPaylos
LamidacZydus
LamitecZifam India
LamivirIncepta
ZeffixGlaxoSmithKline
Brand mixtures
NameLabellerIngredients
Abacavir Sulfate, Lamivudine and ZidovudineLupin Pharmaceuticals, Inc.
Apo-abacavir-lamivudineApotex Inc
Apo-abacavir-lamivudine-zidovudineApotex Inc
Apo-lamivudine-zidovudineApotex Inc
Apo-zidovudine-lamivudine-nevirapineApotex Inc
Auro-abacavir/lamivudineAuro Pharma Inc
Auro-lamivudine/zidovudineAuro Pharma Inc
CombivirStat Rx USA
Direct RxDIRECT RX
EpzicomREMEDYREPACK INC.
KivexaViiv Healthcare Ulc
Lamivudine and ZidovudineTeva Pharmaceuticals USA Inc
Mylan-abacavir/lamivudineMylan Pharmaceuticals Ulc
Teva-abacavir/lamivudineTeva Canada Limited
Teva-lamivudine/zidovudineTeva Canada Limited
TriumeqVii V Healthcare Company
TrizivirVii V Healthcare Company
Salts
Name/CASStructureProperties
3-TC
ThumbNot applicableDBSALT000976
GR 109714 X
ThumbNot applicableDBSALT000977
Categories
UNII2T8Q726O95
CAS number134678-17-4
WeightAverage: 229.256
Monoisotopic: 229.052111923
Chemical FormulaC8H11N3O3S
InChI KeyInChIKey=JTEGQNOMFQHVDC-NKWVEPMBSA-N
InChI
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
IUPAC Name
4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-dihydropyrimidin-2-one
SMILES
NC1=NC(=O)N(C=C1)[C@@H]1CS[[email protected]](CO)O1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 3'-thia pyrimidine nucleosides. These are nucleoside analogues with a structure that consists of a pyrimidine base, which is N-substituted at the 1-position with a 3'-thia derivative (1,3-oxazolidine) of the ribose moiety that is characteristic of nucleosides.
KingdomOrganic compounds
Super ClassNucleosides, nucleotides, and analogues
ClassNucleoside and nucleotide analogues
Sub Class3'-thia pyrimidine nucleosides
Direct Parent3'-thia pyrimidine nucleosides
Alternative Parents
Substituents
  • 3'-thia pyrimidine nucleoside
  • Pyrimidone
  • Aminopyrimidine
  • Imidolactam
  • Pyrimidine
  • Primary aromatic amine
  • Hydropyrimidine
  • Heteroaromatic compound
  • Oxathiolane
  • Monothioacetal
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Thioether
  • Hydrocarbon derivative
  • Primary amine
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of HIV infection and chronic hepatitis B (HBV).
PharmacodynamicsLamivudine 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.
Mechanism of actionLamivudine 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.
Related Articles
AbsorptionLamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in 12 adult patients was 86% ± 16% (mean ± SD) for the 150-mg tablet and 87% ± 13% for the oral solution. The peak serum lamivudine concentration (Cmax) was 1.5 ± 0.5 mcg/mL when an oral dose of 2 mg/kg twice a day was given to HIV-1 patients. When given with food, absorption is slower, compared to the fasted state.
Volume of distribution

Apparent volume of distribution, IV administration = 1.3 ± 0.4 L/kg. Volume of distribution was independent of dose and did not correlate with body weight.

Protein binding<36% bound to plasma protein.
Metabolism

Metabolism of lamivudine is a minor route of elimination. In man, the only known metabolite of lamivudine is the trans-sulfoxide metabolite. This biotransformation is catalyzed by sulfotransferases.

SubstrateEnzymesProduct
Lamivudine
Lamivudine sulfoxideDetails
Lamivudine
Lamivudine-diphosphate-cholineDetails
Lamivudine
Not Available
Lamivudine-diphosphate-ethanolamineDetails
Lamivudine
Not Available
Lamivudine-monophosphateDetails
Lamivudine
Not Available
Lamivudine-triphosphateDetails
Route of eliminationThe majority of lamivudine is eliminated unchanged in urine by active organic cationic secretion. 5.2% ± 1.4% (mean ± SD) of the dose was excreted as the trans-sulfoxide metabolite in the urine. Lamivudine is excreted in human breast milk and into the milk of lactating rats.
Half life5 to 7 hours (healthy or HBV-infected patients)
Clearance
  • Renal clearance = 199.7 ± 56.9 mL/min [300 mg oral dose, healthy subjects]
  • Renal clearance = 280.4 ± 75.2 mL/min [single IV dose, HIV-1-infected patients]
  • Total clearance = 398.5 ± 69.1 mL/min [HIV-1-infected patients]
ToxicityThe most common reported adverse reactions (incidence ≥15%) in adults were headache, nausea, malaise and fatigue, nasal signs and symptoms, diarrhea, and cough.
Affected organisms
  • Human Immunodeficiency Virus
  • Hepatitis B virus
Pathways
PathwayCategorySMPDB ID
Lamivudine Metabolism PathwayDrug metabolismSMP00649
Lamivudine Action PathwayDrug actionSMP00742
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9932
Blood Brain Barrier+0.9792
Caco-2 permeable-0.7147
P-glycoprotein substrateNon-substrate0.7523
P-glycoprotein inhibitor INon-inhibitor0.9561
P-glycoprotein inhibitor IINon-inhibitor0.9803
Renal organic cation transporterNon-inhibitor0.8646
CYP450 2C9 substrateNon-substrate0.7476
CYP450 2D6 substrateNon-substrate0.8393
CYP450 3A4 substrateNon-substrate0.6393
CYP450 1A2 substrateNon-inhibitor0.8687
CYP450 2C9 inhibitorNon-inhibitor0.7933
CYP450 2D6 inhibitorNon-inhibitor0.9206
CYP450 2C19 inhibitorNon-inhibitor0.8282
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.887
Ames testAMES toxic0.6341
CarcinogenicityNon-carcinogens0.782
BiodegradationNot ready biodegradable0.9698
Rat acute toxicity2.1348 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9834
hERG inhibition (predictor II)Non-inhibitor0.8735
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Viiv healthcare co
  • Glaxosmithkline
Packagers
Dosage forms
FormRouteStrength
Solutionoral10 mg
Tabletoral150 mg
Tabletoral300 mg
Tabletoral
Film-coated tabletOral use150 mg
Film-coated tabletOral use300 mg
Oral solutionOral use10 mg/ml
Solutionoral10 mg/mL
Tabletoral300 mg/1
Tablet, film coatedoral150 mg/1
Solutionoral5 mg/mL
Tablet, film coatedoral100 mg/1
Solutionoral5 mg
Tabletoral100 mg
Tablet, film coatedoral300 mg/1
Tablet, film coatedoral
Film-coated tabletOral use100 mg
Prices
Unit descriptionCostUnit
Epzicom 600-300 mg tablet37.21USD tablet
Epzicom tablet35.78USD tablet
Epivir 300 mg tablet15.57USD tablet
Epivir hbv 100 mg tablet13.94USD tablet
Epivir 150 mg tablet7.79USD tablet
Epivir 10 mg/ml Solution0.53USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2070230 No2004-08-032012-06-02Canada
CA2100269 No1999-02-232012-01-03Canada
US5905082 Yes1996-11-182016-11-18Us
US6004968 Yes1998-09-202018-09-20Us
US6294540 Yes1998-11-142018-11-14Us
US6417191 Yes1996-09-282016-09-28Us
US7119202 No1992-08-082009-08-08Us
US7169780 No2003-10-032023-10-03Us
US7217713 No2002-10-212022-10-21Us
US7435734 No2002-10-212022-10-21Us
US7754731 No2009-03-112029-03-11Us
US7820660 No2003-04-252023-04-25Us
US8129385 No2007-10-052027-10-05Us
US9242986 No2009-10-082029-10-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point160-162 °CNot Available
water solubility70 mg/mlNot Available
logP-1.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.76 mg/mLALOGPS
logP-1.3ALOGPS
logP-1.1ChemAxon
logS-1.9ALOGPS
pKa (Strongest Acidic)14.29ChemAxon
pKa (Strongest Basic)-0.16ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area88.15 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity55.16 m3·mol-1ChemAxon
Polarizability21.7 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Jinliang LI, Feng LV, “PROCESS FOR STEREOSELECTIVE SYNTHESIS OF LAMIVUDINE.” U.S. Patent US20100249409, issued September 30, 2010.

US20100249409
General References
  1. Fox Z, Dragsted UB, Gerstoft J, Phillips AN, Kjaer J, Mathiesen L, Youle M, Katlama C, Hill A, Bruun JN, Clumeck N, Dellamonica P, Lundgren JD: A randomized trial to evaluate continuation versus discontinuation of lamivudine in individuals failing a lamivudine-containing regimen: the COLATE trial. Antivir Ther. 2006;11(6):761-70. [PubMed:17310820 ]
External Links
ATC CodesJ05AR13J05AR02J05AR12J05AR01J05AR05J05AR07J05AR04J05AR16J05AF05J05AR11
AHFS Codes
  • 08:18.08.20
PDB EntriesNot Available
FDA labelDownload (310 KB)
MSDSDownload (57.6 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe serum concentration of Lamivudine can be increased when it is combined with Acetaminophen.
AfatinibThe serum concentration of Lamivudine can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Lamivudine can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Lamivudine can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Lamivudine can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Lamivudine can be increased when it is combined with Alfentanil.
AmantadineThe serum concentration of Lamivudine can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Lamivudine can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Lamivudine can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Lamivudine can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Lamivudine can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Lamivudine can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Lamivudine can be increased when it is combined with Amsacrine.
AstemizoleThe serum concentration of Lamivudine can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Lamivudine can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Lamivudine can be increased when it is combined with Atenolol.
AtorvastatinThe serum concentration of Lamivudine can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Lamivudine can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Lamivudine can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Lamivudine can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Lamivudine can be increased when it is combined with Bepridil.
BiperidenThe serum concentration of Lamivudine can be increased when it is combined with Biperiden.
BosutinibThe serum concentration of Lamivudine can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Lamivudine can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Lamivudine can be increased when it is combined with Buprenorphine.
BupropionThe serum concentration of Lamivudine can be increased when it is combined with Bupropion.
BuspironeThe serum concentration of Lamivudine can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Lamivudine can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Lamivudine can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Lamivudine can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Lamivudine can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Lamivudine can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Lamivudine can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Lamivudine can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Lamivudine can be increased when it is combined with Caspofungin.
ChloroquineThe serum concentration of Lamivudine can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Lamivudine can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Lamivudine can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Lamivudine can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Lamivudine can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Lamivudine can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Lamivudine can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Lamivudine can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Lamivudine can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Lamivudine can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Lamivudine can be increased when it is combined with Clarithromycin.
ClofazimineThe serum concentration of Lamivudine can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Lamivudine can be increased when it is combined with Clomipramine.
ClotrimazoleThe serum concentration of Lamivudine can be decreased when it is combined with Clotrimazole.
CobicistatThe serum concentration of Lamivudine can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Lamivudine can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Lamivudine can be increased when it is combined with Colforsin.
CrizotinibThe serum concentration of Lamivudine can be increased when it is combined with Crizotinib.
CyclophosphamideThe serum concentration of Lamivudine can be increased when it is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Lamivudine can be decreased when it is combined with Cyclosporine.
DaclatasvirThe serum concentration of Lamivudine can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Lamivudine can be increased when it is combined with Dactinomycin.
DasatinibThe serum concentration of Lamivudine can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Lamivudine can be decreased when it is combined with Daunorubicin.
DesipramineThe serum concentration of Lamivudine can be increased when it is combined with Desipramine.
DesloratadineThe serum concentration of Lamivudine can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Lamivudine can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Lamivudine can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Lamivudine can be increased when it is combined with Diclofenac.
DigoxinThe serum concentration of Lamivudine can be decreased when it is combined with Digoxin.
DihydroergotamineThe serum concentration of Lamivudine can be increased when it is combined with Dihydroergotamine.
DiltiazemThe serum concentration of Lamivudine can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Lamivudine can be increased when it is combined with Dipyridamole.
DoxazosinThe serum concentration of Lamivudine can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Lamivudine can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Lamivudine can be decreased when it is combined with Doxorubicin.
DronabinolThe serum concentration of Lamivudine can be increased when it is combined with Dronabinol.
DronedaroneThe serum concentration of Lamivudine can be increased when it is combined with Dronedarone.
ElbasvirThe serum concentration of Lamivudine can be increased when it is combined with Elbasvir.
EltrombopagThe serum concentration of Lamivudine can be increased when it is combined with Eltrombopag.
EmtricitabineThe risk or severity of adverse effects can be increased when Lamivudine is combined with Emtricitabine.
EnalaprilThe serum concentration of Lamivudine can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Lamivudine can be increased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Lamivudine can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Lamivudine can be increased when it is combined with Ergotamine.
ErythromycinThe serum concentration of Lamivudine can be decreased when it is combined with Erythromycin.
EstramustineThe serum concentration of Lamivudine can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Lamivudine can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Lamivudine can be decreased when it is combined with Estrone.
EtoposideThe serum concentration of Lamivudine can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Lamivudine can be increased when it is combined with Etravirine.
FelodipineThe serum concentration of Lamivudine can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Lamivudine can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Lamivudine can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Lamivudine can be increased when it is combined with Fidaxomicin.
FluconazoleThe serum concentration of Lamivudine can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Lamivudine can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Lamivudine can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Lamivudine can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Lamivudine can be increased when it is combined with Flurazepam.
FluvoxamineThe serum concentration of Lamivudine can be increased when it is combined with Fluvoxamine.
GefitinibThe serum concentration of Lamivudine can be increased when it is combined with Gefitinib.
GenisteinThe serum concentration of Lamivudine can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Lamivudine can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Lamivudine can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Lamivudine can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Lamivudine can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Lamivudine can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Lamivudine can be increased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Lamivudine can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Lamivudine can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Lamivudine can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Lamivudine can be decreased when it is combined with Indinavir.
IndomethacinThe serum concentration of Lamivudine can be increased when it is combined with Indomethacin.
IsavuconazoniumThe serum concentration of Lamivudine can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Lamivudine can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Lamivudine can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Lamivudine can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Lamivudine can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Lamivudine can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Lamivudine can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Lamivudine can be increased when it is combined with Lapatinib.
LevofloxacinThe serum concentration of Lamivudine can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Lamivudine can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Lamivudine can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Lamivudine can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Lamivudine can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Lamivudine can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Lamivudine can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Lamivudine can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Lamivudine can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Lamivudine can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Lamivudine can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Lamivudine can be increased when it is combined with Lovastatin.
LumacaftorThe serum concentration of Lamivudine can be decreased when it is combined with Lumacaftor.
MaprotilineThe serum concentration of Lamivudine can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Lamivudine can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Lamivudine can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Lamivudine can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Lamivudine can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Lamivudine can be increased when it is combined with Methadone.
MetoprololThe serum concentration of Lamivudine can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Lamivudine can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Lamivudine can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Lamivudine can be decreased when it is combined with Midazolam.
MifepristoneThe serum concentration of Lamivudine can be decreased when it is combined with Mifepristone.
MitomycinThe serum concentration of Lamivudine can be increased when it is combined with Mitomycin.
MitoxantroneThe serum concentration of Lamivudine can be decreased when it is combined with Mitoxantrone.
MorphineThe serum concentration of Lamivudine can be increased when it is combined with Morphine.
NaltrexoneThe serum concentration of Lamivudine can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Lamivudine can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Lamivudine can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Lamivudine can be decreased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Lamivudine can be increased when it is combined with Neostigmine.
NicardipineThe serum concentration of Lamivudine can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Lamivudine can be decreased when it is combined with Nifedipine.
NilotinibThe serum concentration of Lamivudine can be increased when it is combined with Nilotinib.
NisoldipineThe serum concentration of Lamivudine can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Lamivudine can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Lamivudine can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Lamivudine can be decreased when it is combined with Norethisterone.
OmeprazoleThe serum concentration of Lamivudine can be increased when it is combined with Omeprazole.
P-NitrophenolThe serum concentration of Lamivudine can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Lamivudine can be increased when it is combined with Paclitaxel.
Palmitic AcidThe serum concentration of Lamivudine can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Lamivudine can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Lamivudine can be increased when it is combined with Paroxetine.
PerindoprilThe serum concentration of Lamivudine can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Lamivudine can be decreased when it is combined with Phenobarbital.
PimozideThe serum concentration of Lamivudine can be increased when it is combined with Pimozide.
Platelet Activating FactorThe serum concentration of Lamivudine can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Lamivudine can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Lamivudine can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Lamivudine can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Lamivudine can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Lamivudine can be increased when it is combined with Prednisone.
ProbenecidThe serum concentration of Lamivudine can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Lamivudine can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Lamivudine can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Lamivudine can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Lamivudine can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Lamivudine can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Lamivudine can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Lamivudine can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Lamivudine can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Lamivudine can be increased when it is combined with Quinine.
RanitidineThe serum concentration of Lamivudine can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Lamivudine can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Lamivudine can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Lamivudine can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Lamivudine can be decreased when it is combined with Reserpine.
RifampicinThe serum concentration of Lamivudine can be decreased when it is combined with Rifampicin.
RilpivirineThe serum concentration of Lamivudine can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Lamivudine can be decreased when it is combined with Ritonavir.
RolapitantThe serum concentration of Lamivudine can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of Lamivudine can be decreased when it is combined with Saquinavir.
ScopolamineThe serum concentration of Lamivudine can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Lamivudine can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Lamivudine can be increased when it is combined with Sertraline.
SimeprevirThe serum concentration of Lamivudine can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Lamivudine can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Lamivudine can be decreased when it is combined with Sirolimus.
SorafenibThe serum concentration of Lamivudine can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Lamivudine can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Lamivudine can be decreased when it is combined with St. John&#39;s Wort.
StaurosporineThe serum concentration of Lamivudine can be increased when it is combined with Staurosporine.
StreptozocinThe serum concentration of Lamivudine can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Lamivudine can be increased when it is combined with Sulfinpyrazone.
SumatriptanThe serum concentration of Lamivudine can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Lamivudine can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Lamivudine can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Lamivudine can be decreased when it is combined with Tacrolimus.
TamoxifenThe serum concentration of Lamivudine can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Lamivudine can be increased when it is combined with Taurocholic Acid.
TelmisartanThe serum concentration of Lamivudine can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Lamivudine can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Lamivudine can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Lamivudine can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Lamivudine can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Lamivudine can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Lamivudine can be increased when it is combined with Testosterone.
TicagrelorThe serum concentration of Lamivudine can be increased when it is combined with Ticagrelor.
TolvaptanThe serum concentration of Lamivudine can be increased when it is combined with Tolvaptan.
TrazodoneThe serum concentration of Lamivudine can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Lamivudine can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Lamivudine can be increased when it is combined with Triflupromazine.
TrimethoprimTrimethoprim may decrease the excretion rate of Lamivudine which could result in a lower serum level and potentially a reduction in efficacy.
TrimipramineThe serum concentration of Lamivudine can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Lamivudine can be increased when it is combined with Troleandomycin.
VenlafaxineThe serum concentration of Lamivudine can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Lamivudine can be decreased when it is combined with Verapamil.
VinblastineThe serum concentration of Lamivudine can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Lamivudine can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Lamivudine can be increased when it is combined with Vinorelbine.
ZimelidineThe serum concentration of Lamivudine can be increased when it is combined with Zimelidine.
Food Interactions
  • Take without regard to meals. Food does not decrease the extent of absorption, but it decreases the Cmax by slowing the rate of absorption.

Targets

Kind
Protein
Organism
Human immunodeficiency virus 1
Pharmacological action
yes
Actions
inhibitor
General Function:
Rna-dna hybrid ribonuclease activity
Specific Function:
Not Available
Gene Name:
pol
Uniprot ID:
Q72547
Molecular Weight:
65223.615 Da
References
  1. van Leeuwen R, Lange JM, Hussey EK, Donn KH, Hall ST, Harker AJ, Jonker P, Danner SA: The safety and pharmacokinetics of a reverse transcriptase inhibitor, 3TC, in patients with HIV infection: a phase I study. AIDS. 1992 Dec;6(12):1471-5. [PubMed:1283519 ]
2. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
adduct
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Pan XP, Li LJ, Du WB, Li MW, Cao HC, Sheng JF: Differences of YMDD mutational patterns, precore/core promoter mutations, serum HBV DNA levels in lamivudine-resistant hepatitis B genotypes B and C. J Viral Hepat. 2007 Nov;14(11):767-74. [PubMed:17927612 ]
  4. Dai CY, Yu ML, Hsieh MY, Lee LP, Hou NJ, Huang JF, Chen SC, Lin ZY, Hsieh MY, Wang LY, Tsai JF, Chang WY, Chuang WL: Early response to lamivudine therapy in clinically non-cirrhotic chronic hepatitis B patients with decompensation. Liver Int. 2007 Dec;27(10):1364-70. Epub 2007 Sep 26. [PubMed:17900250 ]
  5. Ma H, Guo F, Wei L, Sun Y, Wang H: [The prospective study of the clinical features and outcome of HBeAg-negative and HBeAg-positive cirrhosis in patients with chronic type B hepatitis]. Zhonghua Yi Xue Za Zhi. 2007 Jul 10;87(26):1832-5. [PubMed:17922993 ]
Kind
Protein
Organism
HBV-F
Pharmacological action
yes
Actions
inhibitor
General Function:
Rna-dna hybrid ribonuclease activity
Specific Function:
Multifunctional enzyme that converts the viral RNA genome into dsDNA in viral cytoplasmic capsids. This enzyme displays a DNA polymerase activity that can copy either DNA or RNA templates, and a ribonuclease H (RNase H) activity that cleaves the RNA strand of RNA-DNA heteroduplexes in a partially processive 3'- to 5'-endonucleasic mode. Neo-synthesized pregenomic RNA (pgRNA) are encapsidated to...
Gene Name:
P
Uniprot ID:
Q05486
Molecular Weight:
94257.43 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Stuyver LJ, Locarnini SA, Lok A, Richman DD, Carman WF, Dienstag JL, Schinazi RF: Nomenclature for antiviral-resistant human hepatitis B virus mutations in the polymerase region. Hepatology. 2001 Mar;33(3):751-7. [PubMed:11230757 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Protein homodimerization activity
Specific Function:
Required for the phosphorylation of the deoxyribonucleosides deoxycytidine (dC), deoxyguanosine (dG) and deoxyadenosine (dA). Has broad substrate specificity, and does not display selectivity based on the chirality of the substrate. It is also an essential enzyme for the phosphorylation of numerous nucleoside analogs widely employed as antiviral and chemotherapeutic agents.
Gene Name:
DCK
Uniprot ID:
P27707
Molecular Weight:
30518.315 Da
References
  1. Hunsucker SA, Mitchell BS, Spychala J: The 5'-nucleotidases as regulators of nucleotide and drug metabolism. Pharmacol Ther. 2005 Jul;107(1):1-30. [PubMed:15963349 ]
  2. Cihlar T, Ray AS: Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine. Antiviral Res. 2010 Jan;85(1):39-58. doi: 10.1016/j.antiviral.2009.09.014. Epub 2009 Nov 1. [PubMed:19887088 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Uridylate kinase activity
Specific Function:
Catalyzes the phosphorylation of pyrimidine nucleoside monophosphates at the expense of ATP. Plays an important role in de novo pyrimidine nucleotide biosynthesis. Has preference for UMP and CMP as phosphate acceptors. Also displays broad nucleoside diphosphate kinase activity.
Gene Name:
CMPK1
Uniprot ID:
P30085
Molecular Weight:
22222.175 Da
References
  1. Hunsucker SA, Mitchell BS, Spychala J: The 5'-nucleotidases as regulators of nucleotide and drug metabolism. Pharmacol Ther. 2005 Jul;107(1):1-30. [PubMed:15963349 ]
  2. Cihlar T, Ray AS: Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine. Antiviral Res. 2010 Jan;85(1):39-58. doi: 10.1016/j.antiviral.2009.09.014. Epub 2009 Nov 1. [PubMed:19887088 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Phosphoglycerate kinase activity
Specific Function:
In addition to its role as a glycolytic enzyme, it seems that PGK-1 acts as a polymerase alpha cofactor protein (primer recognition protein).
Gene Name:
PGK1
Uniprot ID:
P00558
Molecular Weight:
44614.36 Da
References
  1. Hunsucker SA, Mitchell BS, Spychala J: The 5'-nucleotidases as regulators of nucleotide and drug metabolism. Pharmacol Ther. 2005 Jul;107(1):1-30. [PubMed:15963349 ]
  2. Cihlar T, Ray AS: Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine. Antiviral Res. 2010 Jan;85(1):39-58. doi: 10.1016/j.antiviral.2009.09.014. Epub 2009 Nov 1. [PubMed:19887088 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Ribosomal small subunit binding
Specific Function:
Major role in the synthesis of nucleoside triphosphates other than ATP. The ATP gamma phosphate is transferred to the NDP beta phosphate via a ping-pong mechanism, using a phosphorylated active-site intermediate. Possesses nucleoside-diphosphate kinase, serine/threonine-specific protein kinase, geranyl and farnesyl pyrophosphate kinase, histidine protein kinase and 3'-5' exonuclease activities....
Gene Name:
NME1
Uniprot ID:
P15531
Molecular Weight:
17148.635 Da
References
  1. Hunsucker SA, Mitchell BS, Spychala J: The 5'-nucleotidases as regulators of nucleotide and drug metabolism. Pharmacol Ther. 2005 Jul;107(1):1-30. [PubMed:15963349 ]
  2. Cihlar T, Ray AS: Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine. Antiviral Res. 2010 Jan;85(1):39-58. doi: 10.1016/j.antiviral.2009.09.014. Epub 2009 Nov 1. [PubMed:19887088 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transcription factor activity, sequence-specific dna binding
Specific Function:
Major role in the synthesis of nucleoside triphosphates other than ATP. Negatively regulates Rho activity by interacting with AKAP13/LBC. Acts as a transcriptional activator of the MYC gene; binds DNA non-specifically (PubMed:8392752). Exhibits histidine protein kinase activity.
Gene Name:
NME2
Uniprot ID:
P22392
Molecular Weight:
17297.935 Da
References
  1. Hunsucker SA, Mitchell BS, Spychala J: The 5'-nucleotidases as regulators of nucleotide and drug metabolism. Pharmacol Ther. 2005 Jul;107(1):1-30. [PubMed:15963349 ]
  2. Cihlar T, Ray AS: Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine. Antiviral Res. 2010 Jan;85(1):39-58. doi: 10.1016/j.antiviral.2009.09.014. Epub 2009 Nov 1. [PubMed:19887088 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Lipid binding
Specific Function:
Controls phosphatidylcholine synthesis.
Gene Name:
PCYT1A
Uniprot ID:
P49585
Molecular Weight:
41730.67 Da
References
  1. Zhou Z, Rodman JH, Flynn PM, Robbins BL, Wilcox CK, D'Argenio DZ: Model for intracellular Lamivudine metabolism in peripheral blood mononuclear cells ex vivo and in human immunodeficiency virus type 1-infected adolescents. Antimicrob Agents Chemother. 2006 Aug;50(8):2686-94. [PubMed:16870759 ]
  2. KENNEDY EP, BORKENHAGEN LF, SMITH SW: Possible metabolic functions of deoxycytidine diphosphate choline and deoxycytidine diphosphate ethanolamine. J Biol Chem. 1959 Aug;234(8):1998-2000. [PubMed:13673002 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Ethanolamine-phosphate cytidylyltransferase activity
Specific Function:
Plays an important role in the biosynthesis of the phospholipid phosphatidylethanolamine. Catalyzes the formation of CDP-ethanolamine.
Gene Name:
PCYT2
Uniprot ID:
Q99447
Molecular Weight:
43835.23 Da
References
  1. Zhou Z, Rodman JH, Flynn PM, Robbins BL, Wilcox CK, D'Argenio DZ: Model for intracellular Lamivudine metabolism in peripheral blood mononuclear cells ex vivo and in human immunodeficiency virus type 1-infected adolescents. Antimicrob Agents Chemother. 2006 Aug;50(8):2686-94. [PubMed:16870759 ]
  2. KENNEDY EP, BORKENHAGEN LF, SMITH SW: Possible metabolic functions of deoxycytidine diphosphate choline and deoxycytidine diphosphate ethanolamine. J Biol Chem. 1959 Aug;234(8):1998-2000. [PubMed:13673002 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Pyrimidine nucleotide binding
Specific Function:
Dephosphorylates the 5' and 2'(3')-phosphates of deoxyribonucleotides, with a preference for dUMP and dTMP, intermediate activity towards dGMP, and low activity towards dCMP and dAMP.
Gene Name:
NT5C
Uniprot ID:
Q8TCD5
Molecular Weight:
23382.54 Da
References
  1. Hunsucker SA, Mitchell BS, Spychala J: The 5'-nucleotidases as regulators of nucleotide and drug metabolism. Pharmacol Ther. 2005 Jul;107(1):1-30. [PubMed:15963349 ]
  2. Cihlar T, Ray AS: Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine. Antiviral Res. 2010 Jan;85(1):39-58. doi: 10.1016/j.antiviral.2009.09.014. Epub 2009 Nov 1. [PubMed:19887088 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Olson DP, Scadden DT, D'Aquila RT, De Pasquale MP: The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein 1 (MRP-1). AIDS. 2002 Sep 6;16(13):1743-7. [PubMed:12218384 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Wada S, Tsuda M, Sekine T, Cha SH, Kimura M, Kanai Y, Endou H: Rat multispecific organic anion transporter 1 (rOAT1) transports zidovudine, acyclovir, and other antiviral nucleoside analogs. J Pharmacol Exp Ther. 2000 Sep;294(3):844-9. [PubMed:10945832 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Wang X, Furukawa T, Nitanda T, Okamoto M, Sugimoto Y, Akiyama S, Baba M: Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. Mol Pharmacol. 2003 Jan;63(1):65-72. [PubMed:12488537 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Minuesa G, Volk C, Molina-Arcas M, Gorboulev V, Erkizia I, Arndt P, Clotet B, Pastor-Anglada M, Koepsell H, Martinez-Picado J: Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3. J Pharmacol Exp Ther. 2009 Apr;329(1):252-61. doi: 10.1124/jpet.108.146225. Epub 2009 Jan 13. [PubMed:19141712 ]
  2. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Minuesa G, Volk C, Molina-Arcas M, Gorboulev V, Erkizia I, Arndt P, Clotet B, Pastor-Anglada M, Koepsell H, Martinez-Picado J: Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3. J Pharmacol Exp Ther. 2009 Apr;329(1):252-61. doi: 10.1124/jpet.108.146225. Epub 2009 Jan 13. [PubMed:19141712 ]
  2. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxin transporter activity
Specific Function:
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name:
SLC22A3
Uniprot ID:
O75751
Molecular Weight:
61279.485 Da
References
  1. Minuesa G, Volk C, Molina-Arcas M, Gorboulev V, Erkizia I, Arndt P, Clotet B, Pastor-Anglada M, Koepsell H, Martinez-Picado J: Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3. J Pharmacol Exp Ther. 2009 Apr;329(1):252-61. doi: 10.1124/jpet.108.146225. Epub 2009 Jan 13. [PubMed:19141712 ]
  2. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Errasti-Murugarren E, Pastor-Anglada M: Drug transporter pharmacogenetics in nucleoside-based therapies. Pharmacogenomics. 2010 Jun;11(6):809-41. doi: 10.2217/pgs.10.70. [PubMed:20504255 ]
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Drug created on June 13, 2005 07:24 / Updated on October 01, 2016 03:35