"The exercise of this option and initiation of the worldwide licensing agreement with Shire, one of the world's leading CNS specialty pharmaceutical companies, is an outstanding achievement for Heptares," said Malcolm Weir, CEO of Heptares. "The A2A programme is the most advanced example of the Heptares drug discovery platform, and highlights our ability to deliver fundamentally novel chemotypes as a basis for first-in-class and best-in-class medicines addressing a broad range of diseases."
The Heptares A2A programme reflects a new approach to this GPCR target. Recently published papers (refs 1-3) describe how Heptares technology was used to stabilise the A2A receptor, enabling the application for the first time of structure-based drug discovery (SBDD) techniques including Biophysical Mapping™, fragment screening and x-ray crystallography to the receptor. The advanced knowledge of the target generated by this approach enabled Heptares scientists to discover entirely new types of chemical structures for inhibiting the A2A receptor, potentially possessing best-in-class drug-like characteristics, a radical advance after decades of largely unsuccessful medicinal chemistry.
About Heptares Therapeutics
Heptares discovers and develops new medicines targeting GPCRs (G-protein-coupled receptors), a super-family of drug targets linked to a wide range of human diseases. We have established R&D collaborations with Shire, Takeda, AstraZeneca, MedImmune and Novartis Option Fund, and have raised $40M in venture financing from MVM Life Science Partners, Clarus Ventures, Novartis Venture Fund and Takeda Ventures. Heptares is an industry pioneer in GPCR structure-based drug design and has built a unique capability for discovering novel molecules that modulate historically undruggable or challenging GPCRs. Our integrated discovery platform
|SOURCE Heptares Therapeutics|
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