Irinotecan Hydrochloride Trihydrate

Irinotecan hydrochloride trihydrate prevents DNA from unwinding by inhibition of topoisomerase 1. Irinotecan (100 mg/kg) significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver in male Wistar rats. Irinotecan (20 mg/kg i.p.) induces tumor growth inhibition of 92% in COLO 320 xenograft mice model. Irinotecan is activated by hydrolysis to SN-38. The inhibition of topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and transcription. Irinotecan is currently in phase 2 clinical trials for the treatment of Non-small Cell Lung Cancer.