Lower hepatotoxicity risk in Xelaglifam, a novel GPR40 agonist, compared to Fasiglifam for type 2 diabetes therapy
Year: 2024
Type: article
Abstract: . Additionally, the glucuronide metabolite of Xelaglifam was negligible (<1 % of the parent) in the Safety Testing, indicating a limited contribution to DILI. Fasiglifam activated genes related to liver disease, whereas Xelaglifam had no effect; instead, it increased FXR activity, a bile acid regulator. Notably, toxicity studies in rats and monkeys showed no adverse liver effects at higher exposure levels than the effective human blood concentration. Overall, these results support a low risk of DILI for Xelaglifam treatment and the justification for its long-term use for treating type 2 diabetes.
Source: Biomedicine & Pharmacotherapy
Authors: Jongmin Yoon, Haengjin Song, Ji Soo Park, Jeong Ho Kim, Yearin Jun, Sang-Ah Gim, Changhee Hong, Kyung Mi An, Joon-Tae Park, Jung Woo Lee, Hongchul Yoon, Yun Seok Kim, Sang Geon Kim
Institutions: Seoul National University, Dongguk University
Language: English
Subfield: Pharmacology
Domain: Life Sciences
Open Access status: gold
Estimated APC paid: $3,420
Award: G667647108
OpenAlex ID: W4404261238