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Zidovudine (Retrovir)
 
Journal Citations
 
General Reports            Therapeutic Strategies        
Animal Studies               Pharmacoeconomics  
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Diagnostics
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 Pharmacokinetics
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Last Update:  March 21, 2018
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General Reports
       
 

Zidovudine protects hyperosmolarity-stressed human corneal epithelial cells via antioxidant pathway.
 Liu H, Gambino F Jr., Algenio C,et al
iochem Biophys Res Commun. 2018 Mar 16
 Abstract

Calorimetric and spectroscopic studies of the interaction between zidovudine and human serum albumin.
Pîrnău A, Mic M, Neamţu S,  et al
Spectrochim Acta A Mol Biomol Spectrosc. 2017 Oct 10;
 Abstract

Evaluation of in-vitro cytotoxicity and cellular uptake efficiency of zidovudine-loaded solid lipid nanoparticles modified with Aloe Vera in glioma cells.
K S J, Sharma CP, Kalarikkal N, Sandeep K, et al
Mater Sci Eng C Mater Biol Appl. 2016 Sep 1;66:40-50.
Abstract

Amperometric sensing of anti-HIV drug zidovudine on Ag nanofilm-multiwalled carbon nanotubes modified glassy carbon electrode.
 Rafati AA, Afraz A.Mater
Sci Eng C Mater Biol Appl. 2014 Jun 1;39:105-12.
 Abstract

Brain Uptake of a Zidovudine Prodrug after Nasal Administration of Solid Lipid Microparticles.
Dalpiaz A, Ferraro L, Perrone D, et al.
Mol Pharm. 2014 Apr 9.
Abstract

FULL-TEXT ARTICLE
 Exposure of Allium cepa Root Cells to Zidovudine or Nevirapine Induces Cytogenotoxic Changes.
 Onwuamah CK, Ekama SO, Audu RA, et al
 PLoS One. 2014 Mar 5;9(3):e90296.
Paper

Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine.
Fang JL, Han T, Wu Q, et al
Arch Toxicol. 2013 Nov 30.
Abstract

Haemoglobin recovery among HIV-1 infected patients on zidovudine-based antiretroviral therapy and other regimens in north-central Nigeria.
 Parrish DD, Blevins M, Megazzini KM,  et al
Int J STD AIDS. 2013 Oct 8.
 Abstract

Mean Corpuscular Volume (MCV) Values Reflect Therapeutic Effectiveness in Zidovudine-Receiving HIV Patients.
 Kim AH, Jang W, Kim Y,  et al
 J Clin Lab Anal. 2013 Sep;27(5):373-8.
 Abstract

FULL-TEXT ARTICLE
AZT as a telomerase inhibitor.
 Gomez DE, Armando RG, Alonso DF.
Front Oncol. 2012;2:113.
 Paper

N348I in HIV-1 Reverse Transcriptase Counteracts the Synergy Between Zidovudine and Nevirapine.
Huey Yap S, Herman BD, Radzio J,  et al
J Acquir Immune Defic Syndr. 2012 Jun 27.
 Abstract

Regional Anthropometry Changes in Antiretroviral-naïve Persons Initiating a Zidovudine-containing Regimen in Mbarara, Uganda.
 Thompson V, Medard B, Taseera K,  et al
AIDS Res Hum Retroviruses. 2010 Dec 5.
 Abstract

Antiviral Activity of Zidovudine and Tenofovir in the Presence of the K65R Mutationin Reverse Transcriptase: An International Cohort Analysis.
 Grant PM, Taylor J, Nevins AB, et al  
Antimicrob Agents Chemother. 2010 Feb 1.
Abstract

Durability of initial antiretroviral therapy in a resource-constrained setting and the potential need for Zidovudine weight-based dosing.
 Willig JH, Echevarria J, Westfall AO, et al
 J Acquir Immune Defic Syndr. 2010 Feb 1;53(2):215-21.
 Abstract

Durability of Initial Antiretroviral Therapy in a Resource Constrained Setting and the Potential Need for Zidovudine Weight-Based Dosing.
 Willig JH, Echevarria J, Westfall AO, et al
 J Acquir Immune Defic Syndr. 2009 Sep 30.
Abstract

Development of an optimized dose for coformulation of zidovudine with drugs that select for the K65R mutation using a population pharmacokinetic and enzyme kinetic simulation model.
Hurwitz SJ, Asif G, Kivel NM, Schinazi RF. 
Antimicrob Agents Chemother. 2008 Dec;52(12):4241-50
 Abstract
 
Inhibition of cation channels and suicidal death of human erythrocytes by zidovudine.
 Kucherenko Y, Geiger C, Shumilina E, et aL
 Toxicology. 2008 Sep 4.
 Abstract
 
Development of an Optimized Dose for Co-formulation of Zidovudine with Drugs that Select for the K65R Mutation Using a Population Pharmacokinetic and Enzyme Kinetic Simulation Model.
Hurwitz SJ, Asif G, Kivel NM, Schinazi RF .
Antimicrob Agents Chemother. 2008 Oct 6.
Abstract
 
Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion.
Stankov MV, Schmidt RE, Behrens GM;, et al
 Antimicrob Agents Chemother. 2008 May 12
 Abstract
 
Food affects Zidovudine concentration independent of effects on gastrointestinal absorption.
 Ndovi TT, Cao YJ, Fuchs E, et al 
J Clin Pharmacol. 2007 Nov;47(11):1366-73
 Abstract
 
HIV-1 and HIV-2 Exhibit Comparable Sensitivity to AZT and Other Nucleoside Analog Inhibitors
In Vitro. Smith RA, Gottlieb GS, Anderson DJ, et al 
Antimicrob Agents Chemother. 2007 Oct 29;
 Abstract 

Concentrations of zidovudine- and lamivudine-triphosphate according to cell type in HIV-seronegative adults.
Anderson PL, Zheng JH, King T, et al
AIDS. 2007 Sep;21(14):1849-54.
 Abstract 
Animal Studies
       
 

Zidovudine induces visceral mitochondrial toxicity and intraabdominal fat gain in a rodent model of lipodystrophy.
Walker UA, Lebrecht D, Reichard W,  et al 
Antivir Ther. 2014 Feb 28.
Abstract 

Effects of combined zidovudine/lopinavir/ritonavir therapy during rat pregnancy: morphological aspects.
de Carvalho LP, Simões RS, Wagner A, et al
 Clin Exp Obstet Gynecol. 2013;40(3):345-9.
 Abstract 

FULL-TEXT PDF ARTICLE
 An unusual phenotypic and genotypic expression in F2 generation following one stage zidovudine exposure during pregnancy and lactation- an experiment in mice.
 Rajlakshmi C, Roy JK, Rai AK,  et al  
J Toxicol Sci. 2012;37(1):51-61
 Paper

Cycle arrest and aneuploidy induced by zidovudine in murine embryonic stem cells.
 Campos PB, Sartore RC, Ramalho BL, et al
Mutagenesis. 2012 Jan 4.
 Abstract 

Neurobehavioral effects of prenatal exposure to AZT: a preliminary investigation with the D1 receptor agonist SKF 38393 in mice.
 Venerosi A, Valanzano A, Puopolo M, Calamandrei G.
Neurotoxicol Teratol. 2005 Jan-Feb;27(1):169-173.
 Abstract 
Pharmacokinetics
       
 

Kinetics of HIV-1 in Cerebrospinal Fluid and Serum After Zidovudine Treatment
Hagberg L, Gisslen M, Norkrans G, Svennerholm B. et al;  
J NeuroAIDS. 1999;2(2):29-35.
Abstract 
Delivery Systems
       
 
Transdermal delivery of zidovudine: effect of terpenes and their mechanism of action.
Narishetty ST, Panchagnula R 
J Control Release. 2004 Mar 24;95(3):367-79.
 Abstract 

Transdermal delivery system for zidovudine: in vitro, ex vivo and in vivo evaluation.
 Narishetty ST, Panchagnula R.
Biopharm Drug Dispos. 2004 Jan;25(1):9-20
 Abstract 
Formulations
       
 
Comparative bioavailability study of zidovudine administered as two different tablet formulations in healthy adult subjects.
Marier JF, Manthos H, Kebir S, et al 
Int J Clin Pharmacol Ther. 2006 May;44(5):240-6.
 Abstract 
Diagnostics
       
 
Ultrasensitive method to quantify intracellular zidovudine mono-, di- and triphosphate concentrations in peripheral blood mononuclear cells by liquid chromatography-tandem mass spectrometry.
Kinai E, Gatanaga H, Kikuchi Y, et al
J Mass Spectrom. 2015 Jun;50(6):ii.
Abstract 

Quantitative analysis of the effect of zidovudine, efavirenz, and ritonavir on insulin aggregation by multivariate curve resolution alternating least squares of infrared spectra.
Martí-Aluja I, Ruisánchez I, Larrechi MS.
 Anal Chim Acta. 2013 Jan 14;760:16-24
Abstract 

Simultaneous determination of lamivudine, lopinavir, ritonavir, and zidovudine concentration in plasma of HIV-infected patients by HPLC-MS/MS.
 Notari S, Sergi M, Montesano C, Ivanovic J,  et al
IUBMB Life. 2012 Apr 4.
Abstract

Improved method to quantify intracellular zidovudine mono- and triphosphate in peripheral bloodmononuclear cells by liquid chromatography-tandem mass spectrometry.
Compain S, Durand-Gasselin L, Grassi J, Benech H.
 J Mass Spectrom. 2007 Jan 22
 Abstract 
 
A simple and rapid liquid chromatography method for simultaneous determination of zidovudine and nevirapine  in plasma.
 Ramachandran G, Hemanthkumar AK, Kumaraswami V, Swaminathan S.
J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Jun 30
 Abstract 
 
A novel rearrangement in electrospray ionization multistage tandem mass spectrometry of amino acid ester cyclohexyl phosphoramidates of AZT.
 Chen Y, Yin Y, Sun X, et al 
J Mass Spectrom. 2005 Feb 15;
 Abstract 

Evaluation of DNA adduction of AZT in peripheral blood leukocytes of HIV-infected individuals by 32)P-post-labeling thin-layer chromatography: a feasibility study.
Huang JM, Anastos K, Robison E, et al 
J Chromatogr B Analyt Technol Biomed Life Sci. 2004 Oct 15;810(1):1-6.
 Abstract 
Oncology Indications
       
  Phase I study of cisdiamminedichloroplatinum in combination with azidothymidine in the treatment of patients with advanced malignancies.
Morgan RJ Jr, Newman EM, Sowers L, et al.
Cancer Chemother Pharmacol 2003 Apr 15
 Abstract 		  
Pharmacokinetics
       

FULL-TEXT ARTICLE
Steady-state pharmacokinetics of zidovudine in Chinese HIV-infected patients.
Liu LF, Wang L, Fu Q,
 Chin Med J (Engl). 2012 Jun;125(11):1931-5

Paper

Pharmacokinetics of Generic Nucleoside Reverse Transcriptase Inhibitors in TB/HIV-Coinfected Ghanaian Patients: UGT2B7*1c Is Associated With Faster Zidovudine Clearance and Glucuronidation.
 Kwara A, Lartey M, Boamah I, et al 
J Clin Pharmacol. 2009 Jul 23
 Abstract 

In vitro and in vivo pharmacokinetic characterization of two novel prodrugs of zidovudine.
 Quevedo MA, Briñón MC.
Antiviral Res. 2009 Aug;83(2):103-11.
 Abstract 

Zidovudine induces S-phase arrest and cell cycle gene expression changes in
human cells.
Olivero OA, Tejera AM, Fernandez JJ, et al  
Mutagenesis. 2005 Mar 22;
 Abstract 
 
AZT Binds RNA at Multiple Sites.
 Ahmed Ouameur A, Marty R, Neault JF, Tajmir-Riahi HA. 
DNA Cell Biol. 2004 Nov;23(11):783-8.
Abstract 

Azidodeoxythymidine and didehydrodeoxythymidine as inhibitors and substrates of the human herpesvirus 8 thymidine kinase. 
Lock MJ, Thorley N, Teo J, Emery VC.
J Antimicrob Chemother 2002 Feb;49(2):359-366
 Abstract 
   
  FULL-TEXT ARTICLE
 Multiple-Dose Pharmacokinetics and Pharmacodynamics of Abacavir Alone and in Combination with Zidovudine in Human Immunodeficiency Virus-Infected Adults
McDowell JA, Lou Y, Symonds WS, Stein DS.
Antimicrob. Agents Chemother. 2000 44: 2061-2067
 Paper
 
Kinetics of HIV-1 in Cerebrospinal Fluid and Serum After Zidovudine Treatment
Hagberg L, Gisslen M, Norkrans G, Svennerholm B. et al;  
J NeuroAIDS. 1999;2(2):29-35.
Abstract 
Drug/Drug Interactions
       
 
Adverse events caused by drug interactions involving glucuronoconjugates of zidovudine, valproic acid and lamotrigine, and analysis of how such potential events are discussed
in package inserts of Japan, UK and USA.
Hirata-Koizumi M, Saito M, Miyake S, Hasegawa R.  
J Clin Pharm Ther. 2007 Apr;32(2):177-85.
 Abstract
 
Severe anemia secondary to a probable drug interaction between zidovudine and valproic acid.
 Antoniou T, Gough K, Yoong D, Arbess G.et al 
Clin Infect Dis. 2004 Mar 1;38(5):e38-4
 Abstract

Prophylactic clarithromycin to treat mycobacterium avium in HIV patients receiving zidovudine may significantly increase mortality by suppressing lymphopoiesis and
hematopoiesis.
Freund YR, Dousman L, Mohagheghpour N.  
 Int Immunopharmacol 2002 Sep;2(10):1465-75
 Abstract 

  
     
  FULL-TEXT ARTICLE
 Pharmacological Basis for Concentration-Controlled Therapy with Zidovudine, Lamivudine, and Indinavir
Kakuda TN, Page LM, Anderson PL, et al.
Antimicrob  Agents  Chemother 2001 Jan;45(1); 236-242 
Paper		  
Resistance
       
 
Rapid accumulation of HIV-1 thymidine analogue mutations and phenotypic impact following prolonged viral failure on zidovudine-based first-line ART in sub-Saharan Africa.
 Goodall RL, Dunn DT, Nkurunziza P,  et al
 J Antimicrob Chemother. 2017 Feb 4
 Abstract 

FULL-TEXT ARTICLE
 Zidovudine (AZT) Monotherapy Selects for the A360V Mutation in the Connection Domain of  HIV-1 Reverse Transcriptase.
 Brehm JH, Scott Y, Koontz DL, et al
 PLoS One. 2012;7(2):e31558
 Paper

Higher levels of Zidovudine resistant HIV in the colon compared to blood and other gastrointestinal compartments in HIV infection.
 van Marle G, Church DL, Nunweiler KD,  et al
Retrovirology. 2010 Sep 13;7(1):74
 Abstract

Rate of Accumulation of Thymidine Analogue Mutations in Patients Continuing to Receive Virologically Failing Regimens Containing Zidovudine or Stavudine: Implications for Antiretroviral Therapy Programs in Resource-Limited Settings.
 Cozzi-Lepri A, Phillips AN, Martinez-Picado J,  et al 
J Infect Dis. 2009 Jul 15.
Abstract

FULL TEXT ARTICLE
 N348I in the Connection Domain of HIV-1 Reverse Transcriptase Confers Zidovudine and Nevirapine Resistance.
Yap SH, Sheen CW, Fahey J, et al 
PLoS Med. 2007 Dec 1;4(12):e335
Paper
 
Mechanisms by which G333D in HIV-1 Reverse Transcriptase Inhibitors Facilitates Dual Resistance to Zidovudine and Lamivudine
Zelina S, Sheen CW, Radzio J, et al
Antimicrob Agents Chemother. 2007 Oct 29;
 Abstract
 
FULL-TEXT ARTICLE
 Why Do HIV-1 and HIV-2 Use Different Pathways to Develop AZT Resistance?
Boyer PL, Sarafianos SG, Clark PK, et al
PLoS Pathog. 2006 Feb 17;2(2):e10
Paper
 
Effect of the Q207D Mutation in HIV Type 1 Reverse Transcriptase on Zidovudine Susceptibility and Replicative Fitness.
 Lu J, Whitcomb J, Kuritzkes DR.
 J Acquir Immune Defic Syndr. 2005 Sep 1;40(1):20-23.
 Abstract
 
Natural resistance of human immunodeficiency virus type 2 to zidovudine.
 Reid P, Macinnes H, Cong ME, et al 
Virology. 2005 Jun 5;336(2):251-64.
 Abstract
 
Primer unblocking by HIV-1 reverse transcriptase and resistance to nucleoside RT inhibitors (NRTIs).
 Goldschmidt V, Marquet R.
 Int J Biochem Cell Biol. 2004 Sep;36(9):1687-705.
 Abstract
 
Rate of Thymidine Analogue Resistance Mutation Accumulation With Zidovudine- or Stavudine-Based Regimens.
 For the Adult ACTG Protocol 306 370 Teams. 
J Acquir Immune Defic Syndr. 2004 Apr 20;36(1):600-603.
 Abstract
 
FULL-TEXT PDF ARTICLE
Nonnucleoside inhibitors of HIV-1 reverse transcriptase inhibit phosphorolysis and resensitize the 3′-azido-3′-deoxythymidine (AZT)-resistant polymerase to AZTTP.
Odriozola L, Cruchaga C, Andreola M, et al.
J Biol Chem. 2003 Aug 13
 Paper
 
Probing the Molecular Mechanisms of AZT Drug Resistance Mediated by HIV-1 Reverse Transcriptase Using a Transient Kinetic Analysis.
Ray AS, Murakami E, Basavapathruni A, et al 
Biochemistry. 2003 Jul 29;42(29):8831-8841.
Abstract
 
Sustained high proportion of zidovudine-resistant HIV variants despite prolonged substitution of zidovudine by other nucleoside reverse transcriptase inhibitors.
Belec L, Legoff J, Si-Mohamed A, et al.
J Med Virol 2002 Sep;68(1):1-6
 Abstract 

Correlation of Phenotypic Zidovudine Resistance with Mutational Patterns in the Reverse Transcriptase of Human Immunodeficiency Virus Type 1: Interpretation of Established Mutations and Characterization of New Polymorphisms at Codons
208, 211, and 214.
Sturmer M, Staszewski S, Doerr HW, et al.
Antimicrob Agents Chemother 2003 Jan;47(1):54-61
 Abstract 

Sustained high proportion of zidovudine-resistant HIV variants despite prolonged substitution of zidovudine by other nucleoside reverse transcriptase inhibitors.
Belec L, Legoff J, Si-Mohat al.
J Med Virol 2002 Sep;68(1):1-6
 Abstract 
 
Carrier rate of zidovudine-resistant HIV-1: the impact of failing therapy on transmission of resistant strains.
Goudsmit J, Weverling GJ, van Der Hoek L, et al
AIDS 2001 Nov 23;15(17):2293-2301
 Abstract 
 
Tenofovir, Adefovir, and Zidovudine Susceptibilities of Primary Human  immunodeficiency Virus Type 1 Isolates with Non-B Subtypes or Nucleoside
Resistance.
Palmer S, Margot N, Gilbert H, et al.
AIDS Res Hum Retroviruses 2001 Aug 10;17(12):1167-1173
 Abstract 
 
FULL-TEXT ARTICLE
 Delavirdine in Combination with Zidovudine in Treatment of Human Immunodeficiency Virus Type 1-Infected Patients: Evaluation of Efficacy and Emergence of Viral Resistance in a Randomized, Comparative Phase III Trial
Joly V, Moroni M, Concia E, et al.
Antimicrob Agents Chemother 2000 Nov;44(11):3155-3157
 Paper

 
Efficacy
       
 
Is Zidovudine 1st line therapy virologically comparable to Tenofovir in resource-limited settings?
Labhardt ND, Bader J, Lejone TI, et al 
Trop Med Int Health. 2015 Mar 1
 Abstract

AZT impairs immunological recovery on first-line ART: collaborative analysis of cohort studies in Southern Africa.
Wandeler G, Gsponer T, Mulenga L, et al
AIDS. 2013 May 8.
 Abstract

Stavudine or zidovudine in three-drug combination therapy for initial treatment of HIV infection in antiretroviral-naïve individuals.
 Spaulding A, Rutherford GW, Siegfried N.
Cochrane Database Syst Rev. 2010 Aug 4;8:CD008651
 Abstract

Intensification of a Failing Regimen with Zidovudine May Cause Sustained Virological Suppression in the Presence of Resensitising Mutations Including K65R.
 Stephan C, Dauer B, Bickel M,  et al