Antitumor activity of optical isomers of cyclophosphamide, ifosfamide and trofosfamide as compared to clinically used racemates.
The relationship between enantiomeric homogeneity of three oxazaphosphorine drugs: cyclophosphamide, ifosfamide and trofosfamide and their antitumor activity was evaluated by standard screening tests against four in vivo transplantable tumor models: L 1210 and P 388 lymphoid leukemias, Lewis lung carcinoma and 16/C line of mouse mammary adenocarcinoma. It was shown that the stereodifferentiation of anti-tumor effect of enantiomers was not outstanding although quite consistently in favour of levorotatory forms. The only exception was seen for cyclophosphamide enantiomers tested against leukemias where R/+/form was more effective than S/-/or racemate.
D000818:Animals; D000970:Antineoplastic Agents; D003520:Cyclophosphamide / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D005260:Female; D007069:Ifosfamide / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D007942:Leukemia, Experimental / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D008297:Male; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D010954:Plasmacytoma / Q000188:drug therapy; D013237:Stereoisomerism
D000970:Antineoplastic Agents; D003520:Cyclophosphamide; C003726:trofosfamide; D007069:Ifosfamide