Heptares Awarded $5.5 Million Research & Development Grant


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Heptares Awarded $5.5 Million Research & Development Grant from the US National Institute on Drug Abuse (NIDA)

Project to develop first-in-class Orexin-1 receptor antagonist for the treatment of cocaine addiction and dependence

London, UK and Boston, MA, USA, 28 September 2015 – Heptares Therapeutics (“Heptares”), the clinical-stage GPCR structure-guided drug discovery and development company and wholly-owned subsidiary of Sosei Group Corporation, is pleased to announce that it has been awarded a grant from the National Institute on Drug Abuse (NIDA), one of the US National Institutes of Health. The grant of approximately $5.5 million, with additional funding from Heptares, will support a three-year research project aimed at developing a selective antagonist for the human Orexin-1 receptor for use in treating cocaine addiction and dependence, for which there are currently no approved treatments.

The Orexin-1 receptor has been implicated in modulating cravings for a number of substances including cocaine, and antagonists of the receptor have been shown to be effective in models of cocaine addiction and dependence. Supported by the grant from NIDA, Heptares will progress lead molecules it has already identified to be selective antagonists of the Orexin-1 receptor to selection of a candidate drug, and then take this molecule through pre-clinical development. This project will be supported by the Heptares GPCR structure-based development platform, in particular making use of high-resolution X-ray structures Heptares has obtained of molecules bound to the closely related Orexin-1 and Orexin-2 receptors.

Fiona Marshall, Heptares Chief Scientific Officer and co-founder, said: “We are delighted to receive this grant award from NIDA. Blockade of the Orexin-1 receptor offers a new approach to address craving and relapse associated with drugs of abuse such as cocaine. We are using our structure based design approaches to identify and optimise highly selective Orexin-1 antagonists, and with the help of this grant from NIDA we intend to progress these through to clinical development.”

The research is supported by the National Institute on Drug Abuse (NIDA) of the US National Institutes of Health, under Grant Number R01DA039553-01. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.


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