KGA-2727 [3-(3-{4-[3-(beta-D-glucopyranosyloxy)-5-isopropyl-1Hpyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)propionamide], is the first reported selective SGLT1 inhibitor which has a pyrazole-O-glucoside structure. KGA-2727 inhibited SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs. It has inhibition constant (Ki) values of 97 and 13,600 nM for human (h) SGLT1 and hSGLT2, respectively.
In March 2005, Kissei Pharmaceutical Co., Ltd. and Dainippon Pharmaceutical Co., Ltd. announced that they have entered into a license agreement on "KGA-2727", a novel agent for the treatment of diabetes, which was discovered by Kissei. It was reported than in future, Kissei will continue to conduct non-clinical studies while Dainippon will conduct clinical development and marketing in Japan. Kissei reserves the right to participate in the clinical development to be conducted by Dainippon as well as the right to co-market the agent. Kissei continues to own the right for this agent outside Japan, including the right for development, manufacturing and marketing.
In March 2005, Kissei Pharmaceutical Co., Ltd. and Dainippon Pharmaceutical Co., Ltd. announced that they have entered into a license agreement on "KGA-2727", a novel agent for the treatment of diabetes, which was discovered by Kissei. It was reported than in future, Kissei will continue to conduct non-clinical studies while Dainippon will conduct clinical development and marketing in Japan. Kissei reserves the right to participate in the clinical development to be conducted by Dainippon as well as the right to co-market the agent. Kissei continues to own the right for this agent outside Japan, including the right for development, manufacturing and marketing.