Ember Therapeutics, Inc. announced the publication of key preclinical data demonstrating that inhibition of the Transient Receptor Potential Vanilloid (TRPV) family of ion channels - specifically TRPV4 - resulted in activation of brown/beige fat and protection from diet-induced obesity, inflammation and insulin resistance. Ember holds an exclusive option to license these TRPV4 findings and technology. The researchers then demonstrated that small molecule inhibition of TRPV4 not only increased PGC1 levels, but also expression of UCP1 - a gene that is specifically expressed in brown/beige fat.

In cultured fat cells, blocking TRPV4 resulted in reduced expression of multiple proinflammatory genes that are involved in the development of insulin resistance. Finally, preclinical mouse models using either mice with a null mutation for TRPV4 or wild-type mice treated with a TRPV4 antagonist demonstrated increased thermogenesis in brown/beige fat tissues and protection from diet-induced obesity, inflammation and insulin resistance. Collectively, these findings demonstrate the compelling therapeutic potential of small molecule TRPV4 inhibition in obesity, type 2 diabetes and other metabolic diseases.