Article
Influence of N-acetyltransferase 2 gene polymorphisms on the in vitro metabolism of the epidermal growth factor receptor inhibitor rociletinib.
British journal of clinical pharmacology - 1 Nov 2021
Ramirez Jacqueline, House Larry K, Ratain Mark J
Abstract excerpt
AIMS: Rociletinib showed activity in T790M-positive non-small cell lung cancer patients. It undergoes amide hydrolysis to form M502, followed by N-acetylation to M544 or amide hydrolysis to M460. We identified the enzymes responsible for rociletinib metabolism, and investigated the relationship between M544 formation and N-acetyltransferase 2 (NAT2) polymorphisms. METHODS: Rociletinib and metabolites were...
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