Introduction/Background

The H3 receptor is predominately expressed in CNS and large body of evidence (both human and rodents studies) during last two decades have showed that antagonist of this receptor suppress the appetite and ultimately induces weight loss. Furthermore, several H3 receptor antagonists are currently in advance stage of clinical trials, testifying aforementioned findings. Thus, obtaining a novel H3R antagonist with drug like properties can be developed as first in class drug for the treatment of obesity.

Highlight Description

We discovered S013-1593, a novel chemical entity, is a selective and potent H3R antagonist active at less than 1nM. This compound produces anorexia and ameliorates glucose tolerance in Db/Db mice in Db/Db mice. Furthermore, S013-1593 (10-30 mg/kg) suppress food intake and significantly causes weight loss in DIO mice and effect is comparable to lorcaserine, a recently FDA approved weight loss drug. More importantly, S013-1593 does not bind to hERG ion channel up to 10 µM.

Importance/Unique Salient Feature

S013-1593 is a first in class H3R antagonist with in vivo efficacy, which is comparable to approved drug lorcaserine for obesity. S013-1593 is effective safe molecule which is being further optimized to a lead candidate drug for the treatment of obesity.
URDIP Report: Proposed structure would be obvious to the proposed activity, to establish enhanced efficacy

Business Exploitation Potential

S013-1593 has very good potential for first target based drug for obesity, which would be first time in India.