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The inactivation of the active form (SN-38) to glucuronide form (SN-38G) is catalyzed by uridine 5'-diphospho-glucuronosyltransferase (UGT). The inactive form (SN-38G) is excreted with the bile into intestinal lumen
The active metabolite of irinotecan is 7-ethyl-10-hydroxycamptothecin (SN-38), responsible for irreversible DNA damage and stronger antitumor activity.
SN-38 is conjugated in the liver by glucuronyltransferase to SN-38 glucuronide (SN-38G), a less toxic metabolite and is excreted into the gastrointestinal tract via bile.
SN-38G is susceptible to hydrolysis by [beta-glucuronidase](brain://aC…