(Group 3)

For definition of Groups, see Preamble Evaluation.

VOL.: 66 (1996) (p. 97)

CAS No.: 40762-15-0
Chem. Abstr. Name: 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-3-hydroxy-1-(2-hydroxyethyl)-2H-1,4-benzodiazepin-

5. Summary of Data Reported and Evaluation

5.1 Exposure data

Doxefazepam is a benzodiazepine hypnotic that was used in the past to a limited extent in the short-term management of insomnia.

5.2 Human carcinogenicity data

No data were available to the Working Group.

5.3 Animal carcinogenicity data

Doxefazepam was tested for carcinogenicity in one experiment in rats by oral administration in the diet. A slight dose-related increase in the incidence of hepatocellular adenomas was observed.

5.4 Other relevant data

Doxefazepam disposition has received little study. In humans, the drug was eliminated in urine mainly as a conjugate, and two oxidative metabolites were identified. The elimination half-life was 3-4 h. No satisfactory metabolism studies in animals were available. Data on human toxicity were not available. In rats treated with 60 mg/kg bw per day for 26 weeks, increased liver weights were reported without other clinical, haematological or histopathological signs of toxicity. In a single study, doxefazepam was not teratogenic in rats or rabbits. The few data available on genetic effects were negative.

5.5 Evaluation

There is inadequate evidence in humans for the carcinogenicity of doxefazepam.

There is limited evidence in experimental animals for the carcinogenicity of doxefazepam.

Overall evaluation

Doxefazepam is not classifiable as to its carcinogenicity to humans (Group 3).

For definition of the italicized terms, see Preamble Evaluation.


Last updated 05/22/97

    See Also:
       Toxicological Abbreviations
       Doxefazepam (PIM 924)