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
- GMM-14 (NIH Number: 14-5967)
(Peer Review Approval 02/00/2012A )
- 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
- GMM-16 (NIH Number: 14-5973)
(Peer Review Approval 02/00/2012A )
- 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
- TR-469 (NIH Number: 99-3959)
(Peer Review Approval 12/11/1996A )
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.