Article
Glucuronidation of 7-ethyl-10-hydroxycamptothecin (SN-38), an active metabolite of irinotecan (CPT-11), by human UGT1A1 variants, G71R, P229Q, and Y486D.
Drug metabolism and disposition: the biological fate of chemicals - 1 Jan 2003
Jinno Hideto, Tanaka-Kagawa Toshiko, Hanioka Nobumitsu, Saeki Mayumi, Ishida Seiichi, Nishimura Tetsuji, Ando Masanori, Saito Yoshiro, Ozawa Shogo, Sawada Jun-Ichi
Abstract excerpt
7-Ethyl-10-hydroxycamptothecin (SN-38), an active metabolite of antitumor agent irinotecan (CPT-11), is conjugated and detoxified to SN-38-glucuronide by UDP-glucuronosyltransferase (UGT) 1A1. Genetic polymorphisms in UGT1A1 are thought to contribute to severe diarrhea and/or leukopenia caused by CPT-11. In this regard, it has been reported that polymorphisms in the promoter region could affect the CPT-11...
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