GPCR drugs firm claims to have developed novel chemotypes against CNS target.

Shire Pharmaceuticals secured an option to Heptares’ adenosine small molecule A2A GPCR antagonist, which is currently in preclinical development for the potential treatment of CNS diseases. Under terms of the deal Shire has an exclusive option to license worldwide development and commercialization rights to the A2A inhibitor program at the end of specified preclinical studies.

U.K-based Heptares claims its StaR™, Biophysical Mapping™, and x-ray crystallographic platforms have allowed it to stabilize the A2A receptor, determine the GPCR’s binding characteristics, and solve its 3-D crystal structure. The resulting insights provided the foundation for Heptares discovery of new types of chemical inhibitors. “A2A is an important and clinically validated GPCR drug target, yet it has never been adequately addressed by the available older chemistries,” remarks Malcolm Weir, Heptare’s CEO. “Hepatares has discovered fundamentally novel chemotypes as the basis for a new and, we believe, superior approach to A2A receptor pharmacology.”

Heptares’ StaR technology is designed to generate stabilized GPCRs containing a small number of point mutations that improve thermostability but without disrupting receptor pharmacology, Heptares claims. The complementary SPR-based Biophysical Mapping technology can be used in combination with x-ray crystallographic data to provide additional structural data on StaR molecules and compound binding.

The deal with Shire follows less than a month after Heptares inked a drug discovery collaboration with Takeda Pharmaceutical, focused on leveraging the StaR, Biophysical Mapping, and crystallography platforms to identify new compounds against a previously intractable GPCR involved in CNS disorders. Under terms of this deal Takeda paid Heptares £1.7 million up front and made a £2.8 million equity investment in the firm.

Back in 2009 Hepatares teamed up with the Novartis Option Fund (NOF) to apply its technologies to a GPCR target provided by NOF. In January 2011 Heptares confirmed it had generated a StaR to the GPCR, making the target accessible for the first time to structure-based drug discovery technologies and approaches. The achievement earned Heptares its first milestone payment from NOF.

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