Heptares awarded $5.5 million grant to combat cocaine addiction

pharmafile | September 30, 2015 | News story | Research and Development Heptares 

Heptares Therapeutics, the clinical-stage GPCR structure-guided drug discovery and development company, has been awarded a grant from the National Institute on Drug Abuse (NIDA), for a project to help combat cocaine addiction.

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, UK-based Heptares (a subsidiary of Sosei Group) will progress its already-identified lead molecules to be selective antagonists of the Orexin-1 receptor to selection of a candidate drug, before taking this molecule through pre-clinical development.

The project will be supported by the Heptares GPCR structure-based development platform, making particular 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, comments: “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.”

Joel Levy 

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