Heptares Therapeutics signed an exclusive option agreement granting Shire Pharmaceuticals an exclusive option, upon completion of certain preclinical studies, to license worldwide development and commercial rights to the Heptares novel adenosine A2A antagonist.

Discovered by Heptares and currently in preclinical development, Adenosine A2A is a G-protein coupled receptor (GPCR) involved in the regulation of dopaminergic pathways in the brain. Inhibition of the A2A receptor has been proved to be clinically effective in treating symptoms of Parkinson’s disease and may offer benefits in additional CNS diseases.

The Heptares A2A program is a new approach to this GPCR target, the company says. Heptares stabilized the A2A receptor using its proprietary StaR technology, determined the receptor’s binding characteristics through Biophysical Mapping, and resolved its 3D crystal structure using X-ray crystallography. This advanced knowledge of the target enabled Heptares scientists to discover new types of chemical structures for inhibiting the A2A receptor.

“We are excited to sign this option agreement with Shire for the development of our novel A2A antagonist, a new agent for treating patients suffering from debilitating CNS diseases,” said Malcolm Weir, chief executive officer of Heptares. “A2A is an important and clinically validated GPCR drug target. Heptares has discovered fundamentally novel chemotypes as the basis for a new and, we believe, superior approach to A2A receptor pharmacology.”

Heptares received an upfront payment and is eligible—upon exercise of the option by Shire—to an option exercise payment, future milestone payments, plus royalties on product sales. Further terms of the agreement were not disclosed.

Release Date: May 9, 2011
Source: Heptares