National Toxicology Program

CASRN: 604-75-1

Formula: C15-H11-CL-N2-02

Synonyms/Common Names:

• 2H-1,4-BENZODIAZEPIN-2-ONE, 7-CHLORO-1,3-DIHYDRO-3-HYDROXY-5-PHENYL- (9CI)

Known Uses:

TRANQUILIZER

Short-Term Toxicity

• 13-WEEK (Dosed-Feed)  (C62453) Completed 
  • NTIS No. PB94-184181  (Peer Review 12/01/1992)
    Citation: Toxicology and Carcinogenesis Studies of Oxazepam (CAS No. 604-75-1) in Swiss-Webster and B6C3F1 Mice (Feed Studies)
  • Mice: B6C3F1; Mice: Swiss Webster
  • Dose: TWO MICE STRAINS: 0, 0.0625, 0.125, 0.25, 0.5, OR 1%

Long-Term Carcinogenicity

• 2-YEAR (Dosed-Feed)  (C62453B) Report Complete 
  • TR-468 (NTIS No. PB99-120875)  (Peer Review 12/11/1996)
    Toxicology and Carcinogenesis Studies of Oxazepam (CAS No. 604-75-1) in F344/N Rats (Feed Studies)
  • Rats: F344/N
  • Carcinogenesis Results
  • Male Rats Equivocal Evidence 
  • Female Rats No Evidence 
  • Dose: 0, 625, 1250, 2500, 5000, OR 10000 PPM; 50/SEX/GROUP
• 2-YEAR (Dosed-Feed)  (C62453) Report Complete 
  • TR-443 (NTIS No. PB94-184181)  (Peer Review 12/01/1992)
    Toxicology and Carcinogenesis Studies of Oxazepam (CAS No. 604-75-1) in Swiss-Webster and B6C3F1 Mice (Feed Studies)
  • Mice: B6C3F1; Mice: Swiss Webster
  • Carcinogenesis Results
  • Male Mice Clear Evidence 
  • Female Mice Clear Evidence 
  • Dose: SW: 0, 2500, OR 5000; B6: 0, 125, 2500, OR 5000 PPM; 60/GROUP

Special Studies

• Absorption Disposition Metabolism Elimination (Dosed-Feed)  (S0765) Completed 
  • Citation: DEMBY, K.B., GRIFFIN, R.J., BURKA, L.T. THE PHARMACOKINETICS AND BILIARY EXCRETION OF OXAZEPAM IN THE F344 RAT FOLLOWING 0, 14, AND 28 DAYS OF EXPOSURE IN THE DIET. THE TOXICOLOGIST, VOL. 13, NO. 1, MARCH 1993
  • Rats: F344/N
• Cell Proliferation (Dosed-Feed)  (S0205) Completed 
  • Citation: CUNNINGHAM, M.L., ET.AL., EARLY RESPONSES OF THE LIVER OF B6C3F1 MICE TO THE HEPATOCARCINOGEN OXAZEPAM, TOXICOL & APPL PHARM 124:31-38,1994.
  • M Rats: F344/N; M Mice: B6C3F1
  • Dose: 25, 125, 2500, 5000 PPM
• Cell Proliferation (Dosed-Feed)  (S0639) Completed 
  • M Rats: F344/N
  • Dose: 5000 ppm
• Metabolism (Gavage)  (S0751) Completed 
  • Citation: GRIFFIN, R.J., & BURKA, L.T. METABOLISM AND ELIMINATION OF OXAZEPAMIN F344 RATS. DRUG METABOLISM AND DISPOSITION. VOL 23, NO. 2: 232-239, 1995.
  • M/F Rats: F344/N
  • Dose: 25, 250, 500 mg/kg
• Metabolism (Dosed-Feed)  (S0752) Completed 
  • Citation: GRIFFIN, R.J., BURKA, L.T., CUNNINGHAM, L.M. ACTIVITY OF HEPATIC DRUG METABOLIZING ENZYMES FOLLOWING OXAZEPAM-DOSED FEED TREATMENT IN B6C3F1 MICE. TOXICOLOGY LETTERS 76 (1995) 251-256
  • M Mice: B6C3F1
  • Dose: 0, 125, 2500 ppm
• Metabolism (Gavage)  (S0753) Completed 
  • Citation: GRIFFIN, R.J., & BURKA, L.T., METABOLISM AND ELIMINATION OF OXAZEPAM IN B6C3F1 AND SWISS WEBSTER MICE. DRUG METABOLISM AND DISPOSITION, VOL 21, NO. 5, 918-926, 1993
  • M/F Mice: B6C3F1; M/F Mice: Swiss Webster
  • Dose: 25, 250 & 500 mg/kg
• Metabolism  (S0754) Completed 
  • Citation: GRIFFIN, R.J., BURKA, L.T., AND DEMBY, K.B. OXIDATIVE BIOTRANSFORMATION OF OXAZEPAM TO REACTIVE AND NON-REACTIVE PRODUCTS IN RAT, MOUSE AND HUMAN MICROSOMES. HUMAN AND EXPERIMENTAL TOXICOLOGY (1995) 14, 779-768
  • Rats; Mice: B6C3F1; Human
• Toxicokinetic Study (Intravenous; Gavage; Intravenous; Gavage; Intravenous; Gavage)  (S0301) Completed 
  • Citation: YUAN, ET.AL. TOXICOKINETICS OF OXAZEPAM IN RATS & MICE, J. PHARM SCI83(10);1373-1379, OCT 94.
  • M/F Rats: F344/N; M/F Rats: F344/N; M/F Mice: B6C3F1; M/F Mice: B6C3F1; M/F Mice: Swiss Webster; M/F Mice: Swiss Webster
  • Dose: IV - 20 MG/KG BW; GAVAGE - 50, 200, 400 MG/KG BW
• Toxicokinetic Study (Dosed-Feed)  (S0578) Completed 
  • Citation: PART OF TR 468
  • M/F Rats: F344/N
  • Dose: 625, 1250, 2500, 5000 OR 10000 PPM

Genetic Toxicology

• In Vitro Cytogenetics (CA/SCE)  (785473) Completed 
  • Chromosome Aberation Negative 
  • Sister Chromatid Exchange Negative 
• Micronucleus  (A98656) Completed 
  • Citation: Witt, K.L., Knapton, A., Wehr, C.M., Hook, G.J., Mirsalis, J., Shelby, M.D., and MacGregor, J.T. Micronucleated Erythrocyte Frequency in Peripheral Blood of B6C3F1 Mice from Short-Term, Prechronic, and Chronic Studies of the NTP Carcinogenesis Bioassay Program. Environ. Molec. Mutagen. Vol. 36 (2000) 163-194
  • Mice: B6C3F1
  • Male Negative 
  • Female Negative 
• Salmonella  (307396) Completed 
  •  Negative