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Glucuronidation of OTS167 in Humans Is Catalyzed by UDP-Glucuronosyltransferases UGT1A1, UGT1A3, UGT1A8, and UGT1A10.

Drug metabolism and disposition: the biological fate of chemicals - 1 Jul 2015

Ramírez Jacqueline, Mirkov Snezana, House Larry K, Ratain Mark J

Abstract excerpt

OTS167 is a potent maternal embryonic leucine zipper kinase inhibitor undergoing clinical testing as antineoplastic agent. We aimed to identify the UDP-glucuronosyltransferases (UGTs) involved in OTS167 metabolism, study the relationship between UGT genetic polymorphisms and hepatic OTS167 glucuronidation, and investigate the inhibitory potential of OTS167 on UGTs. Formation of a single OTS167-glucuronide...

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Identifiers

PMID: 25870101
DOI: 10.1124/dmd.115.063271
PMCID: PMC4468433

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