Irinotecan
Irinotecan is a chemotherapy agent that is a topoisomerase 1 inhibitor.
Its main use is in colon cancer, particularly in combination with other chemotherapy agents. This includes the regimen FOLFIRI which consists of infusional 5-fluorouracil, leucovorin, and irinotecan.
Irinotecan is marketed by Pfizer as Camptosar®. It is also known as CPT-11.
Mechanism
Irinotecan is activated by hydrolysis to SN-38, an inhibitor of topoisomerase I. This is then inactivated by glucuronidation by uridine diphosphate glucoronosyltransferase 1A1 (UGT1A1). Eventually, this process inhibits DNA replication and transcription.
Side effects
Irinotecan is associated with severe diarrhoea, sometimes leading to hospitalization for dehydration. This side effect is managed with the aggressive use of antidiarrhoeals such as loperamide or Lomotil with the first loose bowel movement.
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