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CPL207280 is an orally administered small molecule agonist of G-protein coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1). It was developed by Celon Pharma for the treatment of type 2 diabetes mellitus and has also been investigated in preclinical studies for neuropathic pain. The drug enhances glucose-stimulated insulin secretion, thereby exerting antidiabetic effects without increasing the risk of hypoglycemia. Compared to earlier GPR40 agonists such as TAK-875, CPL207280 was designed with lower molecular weight and lipophilicity to improve safety, particularly regarding hepatotoxicity. Preclinical and early clinical studies indicate that it is well tolerated with a favorable liver safety profile[1][2][3][4][5][6].
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