Identification of a Novel Metabolite of Vildagliptin in Humans: Cysteine Targets the Nitrile Moiety to Form a Thiazoline Ring.

In conclusion, we found that VG and ANG have the potential to covalently bind to a thiol residue of l-cysteine in proteins. Such binding may lead to unpredictable immune responses in humans. l-Cysteine, rather than GSH, would likely be useful to detect the potential for covalent binding that could initiate immune-mediated hepatotoxicity.
PMID: 30172711 [PubMed - as supplied by publisher]

Source: Biochemical Pharmacology - August 30, 2018 Category: Drugs & Pharmacology Authors: Mizuno K, Takeuchi K, Umehara K, Nakajima M Tags: Biochem Pharmacol Source Type: research