CYCLOPHOSPHAMIDE CYSTITIS - STUDIES AIMED AT ITS MINIMIZATION

Two types of approach were used in an effort to alleviate cyclophosphamide-induced cystitis. which is due to acrolein liberated within the urinary tract. The more successful was the concurrent administration of 2,3-dimercaptosuccinic acid an orally effective protecting agent. Replacement of cyclophosphamide with 6-methylcyclophosphamide, an effective anti-tumour drug which liberates the less toxic crotonaldehyde in place of acrolein, resulted in less bladder toxicity but it was not sufficiently advantageous to merit further study. 5-d2-Cyclophosphamide, which on metabolism releases acrolein at less than 20 per cent of the rate of release from cyclophosphamide, was found to be much less toxic than the undeuterated form. © 1979.