Biological Activity:
TAK-875 (Fasiglifam) is the potent, selective and orally bioavailable partial GPR40 agonist with an EC50 ~14 nM. ?It has binding affinity to the human GPR40 receptor with Ki of 38 nM and the rat GPR40 receptor with Ki of 140 nM. TAK-875 has no agonist potency to other members of the FFA receptor family with EC50 >10 μM. The 2.3 ? resolution co-complex structure of hGPR40-TAK-875 reveals a unique binding mode of TAK-875 and suggests that entry to the non-canonical binding pocket most probably occurs via the lipid bilayer. Consistent with the activation of the Gqα-mediated signaling pathway, TAK-875 augments glucose-dependent insulin secretion in pancreatic β cells. Prolonged stimulation of GPR40/FFA1 by TAK-875 does not cause pancreatic β Cell dysfunction or induction of apoptosis. Termination phase III development of TAK-875 (Fasiglifam) for the potential treatment of type-2 diabetes mellitus was announced in 2013 due to concerns about liver safety.
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