Skip to Main Navigation
Skip to Page Content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Testing Status of 3'-Azido-3'-deoxythymidine (AIDS) M88195

CASRN: 30516-87-1

Formula: C10-H13-N5-O4

Synonyms/Common Names

  • Azidothymidine
  • AZT (AIDS initiative)
  • Retrovir
  • Zidovudina

Short-Term Toxicity

  • 13 weeks (Gavage)  (C88072)  Completed 
    • Rats: F344/N; Mice: B6C3F1
    • Dose: DOSES GIVEN twice a day AT 9AM & 3PM--R: 0, 125, 250, 500, OR 1000; M: 0, 25, 50, 100, 400, OR 1000 MG/KG.

Long-Term Carcinogenicity

  • 2 years (Gavage)  (C20309)  Completed 
    • AZT
    • TR-569 (NIH Number: 11-5911)  (Peer Review Approval 04/05/2011A )
      Toxicology and Carcinogenesis Studies of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), Nevirapine (NVP), and Nelfinavir Mesylate (NFV) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2, 159989-65-8) in B6C3F1 Mice (Transplacental Exposure Studies)
    • Mice: B6C3F1; Mice: B6C3F1 (NCTR)
    • Dose: Dosed: GD 12-18 -- 1) AZT 80 mg/kg + 3TC 40 mg/kg; 2) AZT 160 mg/kg + 3TC 80 mg/kg; 3) AZT 240 mg/kg + 3TC 120 mg/kg + 168 mg/kg NVP; 4) AZT 80 mg/kg + 3TC 40 mg/kg + 336 mg/kg NVP; 5) AZT 160 mg/kg + 3TC 80 mg/kg + 672 mg/kg NVP; 6) controls.
    • Carcinogenesis Results
      • Male Mice No Evidence 
      • Female Mice Equivocal Evidence AZT
  • 2 years (Gavage)  (C20309B)   
    • AZT/3TC
    • TR-569 (NIH Number: 11-5911)  (Peer Review Approval 04/05/2011A )
      Toxicology and Carcinogenesis Studies of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), Nevirapine (NVP), and Nelfinavir Mesylate (NFV) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2, 159989-65-8) in B6C3F1 Mice (Transplacental Exposure Studies)
    • Mice: B6C3F1 (NCTR)
    • Dose: 0, 80/40, 160/80, or 240/120 mg/kg.
    • Carcinogenesis Results
      • Male Mice No Evidence 
      • Female Mice Equivocal Evidence 
  • 2 years (Gavage)  (C20309C)   
    • AZT/3TC/NVP
    • TR-569 (NIH Number: 11-5911)  (Peer Review Approval 04/05/2011A )
      Toxicology and Carcinogenesis Studies of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), Nevirapine (NVP), and Nelfinavir Mesylate (NFV) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2, 159989-65-8) in B6C3F1 Mice (Transplacental Exposure Studies)
    • Mice: B6C3F1 (NCTR)
    • Dose: 0, 80/40/56, 160/80/112, or 240/120/168 mg/kg.
    • Carcinogenesis Results
      • Male Mice Some Evidence 
      • Female Mice Equivocal Evidence 
  • 2 years (Gavage)  (C20309D)   
    • AZT/3TC/NFV
    • TR-569 (NIH Number: 11-5911)  (Peer Review Approval 04/05/2011A )
      Toxicology and Carcinogenesis Studies of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), Nevirapine (NVP), and Nelfinavir Mesylate (NFV) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2, 159989-65-8) in B6C3F1 Mice (Transplacental Exposure Studies)
    • Mice: B6C3F1 (NCTR)
    • Dose: 0, 80/40/336, 160/80/672, or 240/120/1, 008 mg/kg.
    • Carcinogenesis Results
      • Male Mice No Evidence 
      • Female Mice No Evidence 
  • 30 weeks and 45 weeks (Gavage)  (C20310C)  Completed 
    • GMM-14 (NIH Number: 14-5967)  (Peer Review Approval 02/00/2012A )
      Toxicology and Carcinogenicity Studies of 3'-Azido-3'-Deoxythymidine (CASRN 30516-87-1) in Genetically Modified C3B6.129F1-Trp53tm1Brd N12 Haploinsufficient Mice (In utero and Postnatal Gavage Studies)
    • Mice: C3B6F1-+/TRP53<TM1BRD> (NCTR)
    • Dose: 30-Week Study: 0 or 240 mg/kg (GD 12-18 -- AZT only); 0 or 120 mg/kg (PND 1-10); 0 or 240 mg/kg (PND 11-9 mo) -- 45-Week Study: 0, 80, 160, or 240 mg/kg (GD 12-18 -- AZT only); 0, 40, 80, or 120 mg/kg (PND 1-10); 0, 80, 160, or 240 mg/kg (PND 11-9 mo) -- 45-Week Stop-Study: 0 or 240 mg/kg (GD 12-18 -- AZT only); 0 or 40 mg/kg (PND 1-8); pups were then maintained on study until 45 weeks of age without dosing.
    • Carcinogenesis Results
      • Male Mice Clear Evidence 
      • Female Mice Equivocal Evidence 
  • 45 weeks (Gavage)  (C20310D)  Completed 
    • GMM-16 (NIH Number: 14-5973)  (Peer Review Approval 02/00/2012A )
      Toxicology and Carcinogenicity Study of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), and Nevirapine (NVP) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2) in Genetically Modified C3B6.129F1-Trp53tm1Brd N12 Haploinsufficient Mice (In Utero and Postnatal Gavage Studies)
    • Mice: P53 +/- (FVB/N)
    • Dose: AZT/3TC: 0, 240, or 150 mg/kg bw/day -- AZT/3TC/NVP combo for P53 mice: AZT: 0, 80, 160, or 240 mg/kg bw/day; 3TC: 0, 50, 100, or 150 mg/kg bw/day; NVP 1-3: 0, 56, 112, or 168 mg/kg bw/day; 1/8 dose NVP PND 1-3 and 1/2 dose NVP PND 4-10.
    • Carcinogenesis Results
      • Male Mice Clear Evidence 
      • Female Mice No Evidence 
  • 45 weeks (Gavage)  (C20310E)  Completed 
    • 3TC-H
    • GMM-16 (NIH Number: 14-5973)  (Peer Review Approval 02/00/2012A )
      Toxicology and Carcinogenicity Study of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), and Nevirapine (NVP) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2) in Genetically Modified C3B6.129F1-Trp53tm1Brd N12 Haploinsufficient Mice (In Utero and Postnatal Gavage Studies)
    • Mice: P53 +/- (FVB/N)
    • Dose: AZT/3TC: 0, 240, or 150 mg/kg bw/day - AZT/3TC/NVP combo for P53 mice: AZT: 0, 80, 160, or 240 mg/kg bw/day; 3TC: 0, 50, 100, or 150 mg/kg bw/day; NVP 1-3: 0, 56, 112, or 168 mg/kg bw/day; 1/8 dose NVP PND 1-3 and 1/2 dose NVP PND 4-10.
    • Carcinogenesis Results
      • Male Mice No Evidence 
      • Female Mice Equivocal Evidence 
  • 45 weeks (Gavage)  (C20310F)  Completed 
    • NVP-H
    • GMM-16 (NIH Number: 14-5973)  (Peer Review Approval 02/00/2012A )
      Toxicology and Carcinogenicity Study of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), and Nevirapine (NVP) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2) in Genetically Modified C3B6.129F1-Trp53tm1Brd N12 Haploinsufficient Mice (In Utero and Postnatal Gavage Studies)
    • Mice: P53 +/- (FVB/N)
    • Dose: AZT/3TC: 0, 240, or 150 mg/kg bw/day -AZT/3TC/NVP combo for P53 mice: AZT: 0, 80, 160, or 240 mg/kg bw/day; 3TC: 0, 50, 100, or 150 mg/kg bw/day; NVP 1-3: 0, 56, 112, or 168 mg/kg bw/day; 1/8 dose NVP PND 1-3 and 1/2 dose NVP PND 4-10.
    • Carcinogenesis Results
      • Male Mice No Evidence 
      • Female Mice Equivocal Evidence 
  • 45 weeks (Gavage)  (C20310G)  Completed 
    • AZT/3TC-H
    • GMM-16 (NIH Number: 14-5973)  (Peer Review Approval 02/00/2012A )
      Toxicology and Carcinogenicity Study of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), and Nevirapine (NVP) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2) in Genetically Modified C3B6.129F1-Trp53tm1Brd N12 Haploinsufficient Mice (In Utero and Postnatal Gavage Studies)
    • Mice: P53 +/- (FVB/N)
    • Dose: AZT/3TC: 0, 240, or 150 mg/kg bw/day - AZT/3TC/NVP combo for P53 mice: AZT: 0, 80, 160, or 240 mg/kg bw/day; 3TC: 0, 50, 100, or 150 mg/kg bw/day; NVP 1-3: 0, 56, 112, or 168 mg/kg bw/day; 1/8 dose NVP PND 1-3 and 1/2 dose NVP PND 4-10.
    • Carcinogenesis Results
      • Male Mice Clear Evidence 
      • Female Mice Equivocal Evidence 
  • 45 weeks (Gavage)  (C20310H)  Completed 
    • AZT/3TC/NVP- L,M,H
    • GMM-16 (NIH Number: 14-5973)
      Toxicology and Carcinogenicity Study of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), and Nevirapine (NVP) (CASRNs 30516-87-1, 134678-17-4, 129618-40-2) in Genetically Modified C3B6.129F1-Trp53tm1Brd N12 Haploinsufficient Mice (In Utero and Postnatal Gavage Studies)
    • Mice: P53 +/- (FVB/N)
    • Dose: AZT/3TC: 0, 240, or 150 mg/kg bw/day - AZT/3TC/NVP combo for P53 mice: AZT: 0, 80, 160, or 240 mg/kg bw/day; 3TC: 0, 50, 100, or 150 mg/kg bw/day; NVP 1-3: 0, 56, 112, or 168 mg/kg bw/day; 1/8 dose NVP PND 1-3 and 1/2 dose NVP PND 4-10.
    • Carcinogenesis Results
      • Male Mice Clear Evidence 
      • Female Mice Equivocal Evidence 
  • 2 years (Gavage)  (C88072)  Completed 
    • TR-469 (NIH Number: 99-3959)  (Peer Review Approval 12/11/1996A )
      Toxicology and Carcinogenesis Studies of AZT (CASRN 30516-87-1) and AZT/ a-Interferon A/D in B6C3F1 Mice (Gavage Studies)
    • Mice: B6C3F1
    • Dose: MICE ONLY: 0, 30, 60, OR 120 MG/KG; 50/SEX.
    • Carcinogenesis Results
      • Male Mice Equivocal Evidence 
      • Female Mice Clear Evidence 

Special Studies

  • Toxicokinetic Study (Gavage)  (K88072)  Completed 
    • Single Dose Plasma Drug Concentration Study
    • Male Rats [R]: Fischer 344
    • Dose: (gavage) 125, 250, 500, 1000, 2000 mg/kg [R].
  • Toxicokinetic Study (Gavage; Intravenous)  (K88072B)  Completed 
    • Pharmacokinetic Study
    • Citation: Trang JM, Prejean JD, James RH, Irwin RD, Goehl TJ, Page JG. Zidovudine bioavailability and linear pharmacokinetics in female B6C3F1 mice. Drug Metab Dispos. 1993 Jan-Feb;21(1):189-93.Pubmed Abstract
    • Female Mice [M]: B6C3F1
    • Dose: (gavage) 15, 30, or 60 mg/kg [M]. (intravenous) 15, 30, or 60 mg/kg [M].

Genetic Toxicology

  • In Vitro Cytogenetics (CA/SCE)  (476222)  Completed 
    • Sister Chromatid Exchange Positive 
    • Chromosome Aberrations Negative 
  • Micronucleus  (912603)  Completed 
    • Citation: Phillips, M.D., Nascimbeni, B., Tice, R.R., and Shelby, M.D. Induction of MN in Mouse BM cells: An evaluation of nucleoside analogues used in the treatment of Aids. Environ. Molec. Mutag. Vol. 18 (1991) 168-183
    • Mice: B6C3F1
    • Male Positive 
  • Micronucleus  (A69895)  Completed 
    • Citation: Phillips, M.D., Nascimbeni, B., Tice, R.R., and Shelby, M.D. Induction of MN in Mouse BM cells: An evaluation of nucleoside analogues used in the treatment of Aids. Environ. Molec. Mutag. Vol. 18 (1991) 168-183
    • Male Positive 
  • Micronucleus  (A88072)  Completed 
    • Mice: B6C3F1
    • Male Positive 
  • Salmonella  (860655)  Completed 
    •  Positive 
  • Salmonella  (G88195)  Completed 
    •  Weakly Positive 

Organ Systems Toxicity

  • 2nd generation Continuous Breeding (Legacy) (Gavage)  (RACB98003)  Completed 
    • Male and Female Mice: Swiss CD-1
    • Dose: 0, 50, 100, OR 200 MG/KG; 2X/DAY.
  • Dominant Lethal (Female) (Gavage)  (DLF96001)  Completed 
    • Female Mice: C3H X 101
    • Mice Female Negative 
  • Dominant Lethal (Male)  (DLM96001)  Completed 
    • Citation: Shelby, MD, Russell, LB, Generoso, W. AZT, rodent somatic and germ cell mutagenicity and reproductive toxicity tests. Environ. Mol. Mutagen. 25 (Suppl.25): 48. (1995)
    • Male Mice: C3H X 101
    • Mice Male Negative 
  • 28 days Immunotoxicity (Gavage)  (IMM20306)  Completed 
    • Female Mice: B6C3F1
    • Dose: 0, 134, 266, or 400 mg/kg/day.
  • 28 days Immunotoxicity (Gavage)  (IMM20401)  Completed 
    • Female Mice: B6C3F1
    • Dose: 0, 134, 266, or 400 mg/kg/day (dams).
  • 180 days Immunotoxicity (Gavage)  (IMM96003)  Completed 
    • Female Mice: B6C3F1
    • Dose: 0, 50, 125, 250, OR 500 MG/KG/DAY.