Obinepitide

Target: Y2+Y4
Product progress: Phase II

7TM Pharma has established a platform of proprietary selective peptide agonists targeting the Y receptors for treatment of obesity. This program includes peptide agonists having potent efficacy on the Y2 and/or Y4 receptor with excellent selectivity over the Y1 receptor, which is involved in causing cardiovascular side effects. From this program, 7TM Pharma has selected its lead candidate for clinical development and completed a Phase I/II study in early 2006. A Phase IIa study was initiated in June 2007.

The drug candidate Obinepitide is a synthetic analogue of two natural human hormones, PYY3-36 and Pancreatic Polypeptide, which normally are released during a meal. These hormones are known to play a role in the regulation of food intake and appetite in man as satiety signals from the GI-tract. In Obinepitide, the properties of both of these hormones have been integrated into a single molecule.

Obinepitide is the lead candidate in 7TM Pharma’s program of NPY receptor agonists, with a dual selectivity profile, targeting the Y2 and Y4 receptor. In pre-clinical studies in diet-induced obese animals the dual active Obinepitide has demonstrated clear superiority in respect of long term reduction in body weight as compared e.g. to the natural hormone PYY3-36, which targets the Y2 receptor only.

A first-in-man Phase I/II clinical study demonstrated that the drug candidate is safe and well tolerated in man. Importantly, in obese human subjects once-a-day subcutaneous (s.c.) dosing of Obinepitide inhibited food intake at a statistically significant level up to 9 hours after dosing.

The Target

The Y2 and the Y4 receptors have both previously been validated in man as independent appetite suppressive drug targets through the use of the natural hormones. 7TM Pharma’s Y receptor peptides have been developed as first-in-class compounds,using the company’s structure-based drug discovery approach as well as world-leading expertise within the Y receptor field, i.e. detailed structural insight and knowledge about drug-receptor interactions.