irinotecan
irinotecan
A topoisomerase-1 inhibitor and semisynthetic analogue of the natural alkaloid camptothecin, which is activated by hydrolysis in vivo to an active metabolit, SN-38, and inactivated by glucuronidation with uridine diphosphate glucoronosyltransferase 1A1 (UGT1A1). It was FDA-approved for managing colorectal carcinoma in 1994.Adverse effects
Severe diarrhoea, possibly leading to dehydration, requiring aggressive antidiarrhoeal management with loperamide or Lomotil; immunosuppression with severe neutropaenia; functional overdose in patients who under-express UGT1A1 and cannot clear irinotecan as quickly (e.g., those with Gilbert syndrome as normal patients).