Shire has exercised an option with the UK's Heptares Therapeutics to license preclinical adenosine A2A antagonists discovered by the latter for the treatment of central nervous system disorders.

Under the terms of the agreement, Heptares receives upfront option grant and exercise payments. The specific amount was not disclosed but the firm noted that it is also eligible to receive future development and commercial milestones up to $190 million, plus royalties.

Adenosine A2A is a G-protein coupled receptor (GPCR) involved in the regulation of dopaminergic pathways in the brain. Its inhibition "is a validated mechanism in the treatment of CNS disorders", Heptares claimed.

Jeff Jonas, head of R&D at Shire's specialty pharmaceuticals and regenerative medicine unit, said the agreement is "a reflection of our growth strategy of investing and focusing on highly-targeted drug discovery platforms". He added that "we are impressed with the novelty and quality of the A2A antagonist leads generated by Heptares, resulting from what we believe to be the first time a structure-based drug discovery approach has been applied from the beginning to a GPCR drug target".

The exercise of the 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 the latter's chief executive Malcolm Weir. He added that the A2A programme "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".

As well as Shire, Heptares has R&D collaborations with firms such as Takeda, AstraZeneca and Novartis.