UDP-glucoronosyltransferases are enzymes responsible for detoxification and elimination of various metabolites and drugs. These enzymes also catalyze the inactivation of irinotecan (CPT-11), an analog of the alkaloid campto-thecin. CPT-11 is clinically used for the treatment of refractory and advanced colorectal cancers. Dose-limiting toxicities are diarrhea and pancytopenia. CPT-11 is metabolized to its active product, SN-38, by the enzyme carboxylesterase 2. As depicted in Fig. 3, UGT1A1 is responsible for the inactivation of SN-38, the most relevant metabolite of CPT-11, to the glucuronide of SN-38. CPT-11 can also be directly inactivated by formation of the inactive oxidation product, aminopenthan carboxylic acid (APC). Responsible for this step are cytochromes P450 3A4 and 3A5, as shown in Fig. 3. However, the formation of the SN-38 glucuronide is the
Irinotecan Carboxylesterase-2 (CPT-11) -► SN-38
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