Eli Lilly and Co (INDIANAPOLIS, Indiana) announced that it has entered into a license agreement with Glenmark Pharmaceuticals SA, a wholly owned subsidiary of Glenmark Pharmaceuticals Ltd (MUMBAI, India). Under the terms of the agreement, Lilly will acquire the rights to a portfolio of transient receptor potential vanilloid subfamily 1 (TRPV1) antagonist molecules, including the clinical compound GRC 6211. TRPV1 is an ion channel protein expressed in human pain pathways and sensory neurons that mediate nociceptive signaling. The compound is currently in early clinical phase II development as a potential next-generation treatment for various pain conditions, including osteoarthritic pain.
 
Under the terms of the agreement, Glenmark will receive an upfront fee of $45 million and could receive up to an additional $215 million in potential development and sales milestones for the initial indication, as well as royalties on sales if GRC 6211 is successfully commercialized. If other indications are successfully developed, Glenmark would be entitled to additional milestone payments up to $90 million. Lilly will have marketing rights in North America, Europe, and Japan; Glenmark will retain the marketing rights in all other countries and will have the right to copromote GRC 6211 in the US.

In 2007, Glenmark conducted a phase I study using single and multiple oral doses of GRC 6211 in healthy volunteers. Preclinical studies have shown the compound highly potent with functional IC50 (inhibition concentration reducing effect by 50%) of 3.8 nM, good bioavailability across species tested, and >2600 selectivity over other TRP ion channel proteins.

TRPV1, formerly known as vanilloid receptor 1 (VR1), is a nonselective, ligand-gated, cation ion channel activated by agonists such as capsaicin and factors such as heat and acidosis.