Licensing status

Publication and contact information

Endocrine/metabolic disease


Free fatty acid receptor 1 (FFAR1; GPR40)

In vitro and mouse studies identified an alkyne series of FFAR1 agonists that could help treat type 2
diabetes. In healthy mice, an alkyne-based FFAR1 agonist with polar substituents on the terminal phenyl ring was orally bioavailable and increased glucose tolerance at least as much as the marketed type 2 diabetes drug Glactiv sitagliptin. Next steps include testing the compounds in rodent models of diabetes.
Connexios Life Sciences Pvt. Ltd. has FFAR1 agonists including CNX-011-67 in preclinical testing to treat diabetes.
Takeda Pharmaceutical Co. Ltd.'s FFAR1 agonist, TAK-875, is in Phase III testing for the indication.
Merck & Co. Inc. and Ono Pharmaceutical Co. Ltd. market the dipeptidyl peptidase-4 (DPP-4) inhibitor Glactiv sitagliptin to treat diabetes.

SciBX 6(4); doi:10.1038/scibx.2013.87
Published online Jan. 31, 2013

Patent application filed covering compounds; available for licensing

Christiansen, E. et al. J. Med. Chem.; published online Jan. 8, 2013;
Contact: Trond Ulven, University of Southern Denmark, Odense, Denmark