MLR-1023: A drug candidate for type II diabetes with a novel molecular target discovered by using an in vivo drug repositioning approach

CINF 14

Michael S. Saporito, msaporito@meliordiscovery.com1, Christopher A. Lipinski, clipinski@meliordiscovery.com2, Alexander Ochman, aochman@meliordiscovery.com1, Dana Koemer1, Jan Batten1, and Andrew Reaume1. (1) Melior Discovery, Inc, 860 Springdale Drive, Exton, PA 19341, (2) Scientific Advisor, Melior Discovery, 10 Connshire Drive, Waterford, CT 06385-4122
Drug repositioning is increasingly recognized as an effective strategy to uncover new therapeutics with reduced developmental risk. Melior Discovery has a unique repositioning approach involving a platform comprised of 35 in vivo models representing diverse therapeutic areas. The power of this platform is illustrated by our lead compound, MLR-1023. This compound, originally developed for ulcers, exhibits robust activity in a panel of clinically relevant models of type II diabetes. For example, when compared to metformin in acute studies, MLR-1023 produced an equivalent glucose lowering response at a significantly lower dose. In comparison to rosiglitazone in chronic studies, MLR-1023 exhibited equivalent efficacy without promoting weight gain. Of importance was the identification of a previously unknown molecular target for type II diabetes. This example of Melior Discovery's approach demonstrates the potential for capturing new indications from existing molecules, and the potential for expanding our understanding of the underlying biological basis of disease.

MLR-1023

 

Drug Reprofiling
2:00 PM-5:40 PM, Sunday, August 19, 2007 BCEC -- 252 A, Oral

Division of Chemical Information

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007