comparison of pharmacological properties of cyclophosphamide and its enantiomers.
Comparison of pharmacological properties of commercial racemic Cyclophosphamide and its D- and L-enantiomers was performed in experiments on mice and rats. Acute toxicity, behavioral screening tests and the effects of subchronic treatment (influence on body mass, the increase of the mass of internal organs, mortality, morphology of peripheral blood, biochemical investigations of blood plasma, microscopic evaluation of liver and bladder) were taken into account. Summarized results revealed the most pronounced toxicity of D-cyclophosphamide. L-enantiomer was more toxic when compared with racemate. As several reports in literature confirmed the greatest antineoplastic activity of L-form in animals, the suggestion of further clinical investigation of levorotatory form as a separate preparation has been put forward.
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D001835:Body Weight / Q000187:drug effects; D003520:Cyclophosphamide / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000633:toxicity; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D007928:Lethal Dose 50; D008099:Liver / Q000187:drug effects / Q000473:pathology*; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects*; D010528:Peristalsis / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D012119:Respiration / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D003520:Cyclophosphamide