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Identification
NameZidovudine
Accession NumberDB00495  (APRD00449)
TypeSmall Molecule
GroupsApproved
Description

A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
AzidothymidineNot AvailableNot Available
AZTNot AvailableNot Available
ZDVNot AvailableNot Available
ZidovudinNot AvailableNot Available
ZidovudinumNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
RetrovirNot Available
Brand mixtures
Brand NameIngredients
CombivirLamivudine + Zidovudine
TrizivirAbacavir sulfate + Lamivudine + Zidovudine
Categories
CAS number30516-87-1
WeightAverage: 267.2413
Monoisotopic: 267.096753929
Chemical FormulaC10H13N5O4
InChI KeyHBOMLICNUCNMMY-XLPZGREQSA-N
InChI
InChI=1S/C10H13N5O4/c1-5-3-15(10(18)12-9(5)17)8-2-6(13-14-11)7(4-16)19-8/h3,6-8,16H,2,4H2,1H3,(H,12,17,18)/t6-,7+,8+/m0/s1
IUPAC Name
1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dione
SMILES
CC1=CN([C@H]2C[C@H](N=[N+]=[N-])[C@@H](CO)O2)C(=O)NC1=O
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassOrganooxygen Compounds
ClassCarbohydrates and Carbohydrate Conjugates
SubclassGlycosyl Compounds
Direct parentPyrimidine Nucleosides and Analogues
Alternative parentsPyrimidones; Hydropyrimidines; Tetrahydrofurans; Oxolanes; Organic Azides; Polyamines; Primary Alcohols; Ethers
Substituentspyrimidone; pyrimidine; hydropyrimidine; tetrahydrofuran; oxolane; azide; ether; polyamine; primary alcohol; organonitrogen compound; amine; alcohol
Classification descriptionThis compound belongs to the pyrimidine nucleosides and analogues. These are compounds comprising a pyrimidine base attached to a sugar.
Pharmacology
IndicationUsed in combination with other antiretroviral agents for the treatment of human immunovirus (HIV) infections.
PharmacodynamicsZidovudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Zidovudine 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 actionZidovudine, a structural analog of thymidine, is a prodrug that must be phosphorylated to its active 5′-triphosphate metabolite, zidovudine triphosphate (ZDV-TP). It inhibits the activity of HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleotide analogue. It competes with the natural substrate dGTP and incorporates itself into viral DNA. It is also a weak inhibitor of cellular DNA polymerase α and γ.
AbsorptionRapid and nearly complete absorption from the gastrointestinal tract following oral administration; however, because of first-pass metabolism, systemic bioavailability of zidovudine capsules and solution is approximately 65% (range, 52 to 75%). Bioavailability in neonates up to 14 days of age is approximately 89%, and it decreases to approximately 61% and 65% in neonates over 14 days of age and children 3 months to 12 years, respectively. Administration with a high-fat meal may decrease the rate and extent of absorption.
Volume of distribution

Apparent volume of distribution, HIV-infected patients, IV administration = 1.6 ± 0.6 L/kg

Protein binding30-38%
Metabolism

Hepatic. Metabolized by glucuronide conjugation to major, inactive metabolite, 3′-azido-3′-deoxy-5′- O-beta-D-glucopyranuronosylthymidine (GZDV). UGT2B7 is the primary UGT isoform that is responsible for glucuronidation. Compared to zidovudine, GZDV's area under the curve is approximately 3-fold greater. The cytochrome P450 isozymes are responsible for the reduction of the azido moiety to form 3'-amino-3'- deoxythymidine (AMT).

SubstrateEnzymesProduct
Zidovudine
Not Available
3'-azido-3'-deoxy-5'- O-beta-D-glucopyranuronosylthymidineDetails
Zidovudine
Not Available
3’-amino-3’-deoxythimidineDetails
Zidovudine
Not Available
3’-amino-3’-deoxythimidine glucuronideDetails
Zidovudine
Not Available
5’glucuronyl zidovudineDetails
Route of eliminationAs in adult patients, the major route of elimination was by metabolism to GZDV. After intravenous dosing, about 29% of the dose was excreted in the urine unchanged and about 45% of the dose was excreted as GZDV.
Half lifeElimination half life, HIV-infected patients, IV administration = 1.1 hours (range of 0.5 - 2.9 hours)
Clearance
  • 0.65 +/- 0.29 L/hr/kg [HIV-infected, Birth to 14 Days of Age]
  • 1.14 +/- 0.24 L/hr/kg [HIV-infected, 14 Days to 3 Months of Age]
  • 1.85 +/- 0.47 L/hr/kg [HIV-infected, 3 Months to 12 Years of Age].
    The transporters, ABCB1, ABCC4, ABCC5, and ABCG2 are involved with the clearance of zidovudine.
ToxicitySymptoms of overdose include fatigue, headache, nausea, and vomiting. LD50 is 3084 mg/kg (orally in mice).
Affected organisms
  • Human Immunodeficiency Virus
Pathways
PathwayCategorySMPDB ID
Zidovudine Action PathwayDrug actionSMP00747
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.9343
Blood Brain Barrier + 0.6224
Caco-2 permeable - 0.8728
P-glycoprotein substrate Non-substrate 0.6959
P-glycoprotein inhibitor I Non-inhibitor 0.9118
P-glycoprotein inhibitor II Non-inhibitor 0.8981
Renal organic cation transporter Non-inhibitor 0.8798
CYP450 2C9 substrate Non-substrate 0.663
CYP450 2D6 substrate Non-substrate 0.8987
CYP450 3A4 substrate Substrate 0.5329
CYP450 1A2 substrate Non-inhibitor 0.9355
CYP450 2C9 substrate Non-inhibitor 0.9143
CYP450 2D6 substrate Non-inhibitor 0.9315
CYP450 2C19 substrate Non-inhibitor 0.9175
CYP450 3A4 substrate Non-inhibitor 0.848
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9585
Ames test AMES toxic 0.9107
Carcinogenicity Non-carcinogens 0.7484
Biodegradation Ready biodegradable 0.5673
Rat acute toxicity 2.0464 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.7124
hERG inhibition (predictor II) Non-inhibitor 0.8821
Pharmacoeconomics
Manufacturers
  • Viiv healthcare co
  • Aurobindo pharma ltd inc
  • Cipla ltd
  • Pharmaforce inc
  • Aurobindo pharma ltd
  • Hetero drugs ltd unit iii
  • Matrix laboratories ltd
  • Ranbaxy laboratories ltd
  • Roxane laboratories inc
Packagers
Dosage forms
FormRouteStrength
CapsuleOral100 mg
Injection, solutionIntravenous10 mg/mL
SyrupOral50 mg/5 mL
TabletOral300 mg
Prices
Unit descriptionCostUnit
Retrovir 50 mg/5ml Syrup 240ml Bottle74.11USDbottle
Retrovir 300 mg tablet9.1USDtablet
Zidovudine 300 mg tablet6.17USDtablet
Retrovir 100 mg capsule3.09USDcapsule
Retrovir iv infusion vial1.61USDml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada22166342004-07-202016-03-28
Canada21054872002-09-242012-03-05
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point113-115 °CPhysProp
water solubility2.01E+004 mg/L (at 25 °C)PHYSICIANS DESK REFERENCE (2003)
logP0.05HANSCH,C ET AL. (1995)
Caco2 permeability-5.16ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility16.3ALOGPS
logP-0.1ALOGPS
logP-0.3ChemAxon
logS-1.2ALOGPS
pKa (Strongest Acidic)9.96ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area108.3 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity61.7 m3·mol-1ChemAxon
Polarizability24.93 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Spectra
Spectra1D NMR
References
Synthesis ReferenceNot Available
General Reference
  1. De Clercq E: HIV resistance to reverse transcriptase inhibitors. Biochem Pharmacol. 1994 Jan 20;47(2):155-69. Pubmed
  2. Yarchoan R, Mitsuya H, Broder S: AIDS therapies. Sci Am. 1988 Oct;259(4):110-9. Pubmed
  3. Connor EM, Sperling RS, Gelber R, Kiselev P, Scott G, O’Sullivan MJ, VanDyke R, Bey M, Shearer W, Jacobson RL, et al.: Reduction of maternal-infant transmission of human immunodeficiency virus type 1 with zidovudine treatment. Pediatric AIDS Clinical Trials Group Protocol 076 Study Group. N Engl J Med. 1994 Nov 3;331(18):1173-80. Pubmed
  4. Mitsuya H, Yarchoan R, Broder S: Molecular targets for AIDS therapy. Science. 1990 Sep 28;249(4976):1533-44. Pubmed
  5. Mitsuya H, Weinhold KJ, Furman PA, St Clair MH, Lehrman SN, Gallo RC, Bolognesi D, Barry DW, Broder S: 3’-Azido-3’-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proc Natl Acad Sci U S A. 1985 Oct;82(20):7096-100. Pubmed
  6. Court MH, Krishnaswamy S, Hao Q, Duan SX, Patten CJ, Von Moltke LL, Greenblatt DJ: Evaluation of 3’-azido-3’-deoxythymidine, morphine, and codeine as probe substrates for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human liver microsomes: specificity and influence of the UGT2B7*2 polymorphism. Drug Metab Dispos. 2003 Sep;31(9):1125-33. Pubmed
External Links
ResourceLink
KEGG DrugD00413
KEGG CompoundC07210
PubChem Compound35370
PubChem Substance46508240
ChemSpider32555
BindingDB50002692
ChEBI10110
ChEMBLCHEMBL129
Therapeutic Targets DatabaseDAP000701
PharmGKBPA451954
Drug Product Database1946323
RxListhttp://www.rxlist.com/cgi/generic3/zidovud.htm
Drugs.comhttp://www.drugs.com/cdi/zidovudine.html
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ret1375.shtml
WikipediaZidovudine
ATC CodesJ05AF01
AHFS Codes
  • 08:18.08.20
PDB EntriesNot Available
FDA labelshow(217 KB)
MSDSshow(57.2 KB)
Interactions
Drug Interactions
Drug
AtovaquoneAtovaquone increases the effect and toxicity of zidovudine
ClarithromycinClarithromycin may decrease the serum concentration of zidovudine. Increased myelosuppression in mice has been observed. Consider staggering doses during concomitant therapy and closely monitor response to zidovudine therapy.
DoxorubicinAdditive myelosuppression may occur. Doxorubicin may decrease the efficacy of zidovudine. Concomitant therapy should be avoided.
GanciclovirIncreased risk of hematologic toxicity. Concomitant therapy should be avoided.
Interferon beta-1bThe interferon increases the effect and toxicity of zidovudine
MethadoneMethadone increases the effect and toxicity of zidovudine
ProbenecidRash, malaise, myalgia
RibavirinIncreased risk or severity of anemia. Consider alternate therapy or monitor more closely for anemia.
RifabutinThe rifamycin decreases levels of zidovudine
RifampicinRifampin may decrease the serum concentration of zidovudine by increasing its metabolism. Monitor for changes in the serum concentration and therapeutic and adverse effects of zidovudine if rifampin is initiated, discontinued or dose changed.
RifapentineRifapentin may decrease the serum concentration of zidovudine by increasing its metabolism. Monitor for changes in the serum concentration and therapeutic and adverse effects of zidovudine if rifapentin is initiated, discontinued or dose changed.
StavudineZidovudine may decrease the efficacy of stavudine. Concomitant therapy should be avoided.
TipranavirTipranavir decreases the concentration of Zidovudine.
ValganciclovirThe adverse/toxic effects of Zidovudine, a reverse transcriptase inhibitor (nucleoside), may be enhanced by Valganciclovir. There is a significant risk of hematologic toxicity. Concomitant therapy should be avoided.
Food InteractionsNot Available

Targets

1. Reverse Transcriptase

Kind: protein

Organism: Human immunodeficiency virus 1

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Reverse transcriptase/RNaseH Q72547 Details

References:

  1. 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
  2. Barry M, Gibbons S, Back D, Mulcahy F: Protease inhibitors in patients with HIV disease. Clinically important pharmacokinetic considerations. Clin Pharmacokinet. 1997 Mar;32(3):194-209. Pubmed
  3. De Clercq E: Antiretroviral drugs. Curr Opin Pharmacol. 2010 May 12. Pubmed

2. Telomerase reverse transcriptase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Telomerase reverse transcriptase O14746 Details

References:

  1. Leeansyah E, Cameron PU, Solomon A, Tennakoon S, Velayudham P, Gouillou M, Spelman T, Hearps A, Fairley C, Smit de V, Pierce AB, Armishaw J, Crowe SM, Cooper DA, Koelsch KK, Liu JP, Chuah J, Lewin SR: Inhibition of telomerase activity by human immunodeficiency virus (HIV) nucleos(t)ide reverse transcriptase inhibitors: a potential factor contributing to HIV-associated accelerated aging. J Infect Dis. 2013 Apr;207(7):1157-65. doi: 10.1093/infdis/jit006. Epub 2013 Jan 9. Pubmed

Enzymes

1. Cytochrome P450 2A6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2A6 P11509 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  2. Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. Pubmed
  3. Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. Pubmed
  4. Letter: Exercise testing and coronary heart disease. N Engl J Med. 1975 Dec 4;293(23):1208-10. Pubmed
  5. Letter: Exercise testing and coronary heart disease. N Engl J Med. 1975 Dec 4;293(23):1208-10. Pubmed

3. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

6. Thymidine kinase, cytosolic

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Thymidine kinase, cytosolic P04183 Details

References:

  1. Furman PA, Fyfe JA, St Clair MH, Weinhold K, Rideout JL, Freeman GA, Lehrman SN, Bolognesi DP, Broder S, Mitsuya H, et al.: Phosphorylation of 3’-azido-3’-deoxythymidine and selective interaction of the 5’-triphosphate with human immunodeficiency virus reverse transcriptase. Proc Natl Acad Sci U S A. 1986 Nov;83(21):8333-7. Pubmed

7. UDP-glucuronosyltransferase 2B7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 2B7 P16662 Details

References:

  1. Court MH, Krishnaswamy S, Hao Q, Duan SX, Patten CJ, Von Moltke LL, Greenblatt DJ: Evaluation of 3’-azido-3’-deoxythymidine, morphine, and codeine as probe substrates for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human liver microsomes: specificity and influence of the UGT2B7*2 polymorphism. Drug Metab Dispos. 2003 Sep;31(9):1125-33. Pubmed

Carriers

1. Serum albumin

Kind: protein

Organism: Human

Pharmacological action: no

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. Quevedo MA, Moroni GN, Brinon MC: Human serum albumin binding of novel antiretroviral nucleoside derivatives of AZT. Biochem Biophys Res Commun. 2001 Nov 9;288(4):954-60. Pubmed

Transporters

1. Solute carrier family 22 member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier family 22 member 2 O15244 Details

References:

  1. Urakami Y, Akazawa M, Saito H, Okuda M, Inui K: cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. J Am Soc Nephrol. 2002 Jul;13(7):1703-10. Pubmed

2. Solute carrier family 22 member 6

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier family 22 member 6 Q4U2R8 Details

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
  2. Takeda, M. et al. Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther 300, 918- 924 (2002).Pubmed

3. Solute carrier family 22 member 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier family 22 member 7 Q9Y694 Details

References:

  1. Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. Pubmed

4. Solute carrier family 22 member 8

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

References:

  1. Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. Pubmed

5. Solute carrier family 22 member 11

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

References:

  1. Takeda M, Khamdang S, Narikawa S, Kimura H, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Endou H: Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24. Pubmed

6. Sodium/nucleoside cotransporter 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Sodium/nucleoside cotransporter 1 O00337 Details

References:

  1. Cano-Soldado P, Lorrayoz IM, Molina-Arcas M, Casado FJ, Martinez-Picado J, Lostao MP, Pastor-Anglada M: Interaction of nucleoside inhibitors of HIV-1 reverse transcriptase with the concentrative nucleoside transporter-1 (SLC28A1). Antivir Ther. 2004 Dec;9(6):993-1002. Pubmed

7. Equilibrative nucleoside transporter 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Equilibrative nucleoside transporter 2 Q14542 Details

References:

  1. Yao SY, Ng AM, Sundaram M, Cass CE, Baldwin SA, Young JD: Transport of antiviral 3’-deoxy-nucleoside drugs by recombinant human and rat equilibrative, nitrobenzylthioinosine (NBMPR)-insensitive (ENT2) nucleoside transporter proteins produced in Xenopus oocytes. Mol Membr Biol. 2001 Apr-Jun;18(2):161-7. Pubmed

8. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Anderson PL, Lamba J, Aquilante CL, Schuetz E, Fletcher CV: Pharmacogenetic characteristics of indinavir, zidovudine, and lamivudine therapy in HIV-infected adults: a pilot study. J Acquir Immune Defic Syndr. 2006 Aug 1;42(4):441-9. Pubmed

9. Multidrug resistance-associated protein 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance-associated protein 4 O15439 Details

References:

  1. Abla N, Chinn LW, Nakamura T, Liu L, Huang CC, Johns SJ, Kawamoto M, Stryke D, Taylor TR, Ferrin TE, Giacomini KM, Kroetz DL: The human multidrug resistance protein 4 (MRP4, ABCC4): functional analysis of a highly polymorphic gene. J Pharmacol Exp Ther. 2008 Jun;325(3):859-68. doi: 10.1124/jpet.108.136523. Epub 2008 Mar 25. Pubmed

10. Multidrug resistance-associated protein 5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance-associated protein 5 O15440 Details

References:

  1. Jorajuria S, Dereuddre-Bosquet N, Becher F, Martin S, Porcheray F, Garrigues A, Mabondzo A, Benech H, Grassi J, Orlowski S, Dormont D, Clayette P: ATP binding cassette multidrug transporters limit the anti-HIV activity of zidovudine and indinavir in infected human macrophages. Antivir Ther. 2004 Aug;9(4):519-28. Pubmed

11. ATP-binding cassette sub-family G member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

References:

  1. Pan G, Giri N, Elmquist WF: Abcg2/Bcrp1 mediates the polarized transport of antiretroviral nucleosides abacavir and zidovudine. Drug Metab Dispos. 2007 Jul;35(7):1165-73. Epub 2007 Apr 16. Pubmed

Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:10