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$5.5 Million NIDA Research Grant Funds New Antagonist Drug To Treat Cocaine Addiction

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The National Institute on Drug Abuse is funding a new antagonist drug to address cocaine abuse. NIDA awarded a $5.5 million research grant to Heptares Therapeutics to support a three-year project to develop a selective antagonist for the human Orexin-1 receptor for use in treating cocaine addiction and dependence. With the success of opiate antagonists like naloxone and naltrexone, there has been a push in the medical community to produce a similar drug for cocaine and other drugs.
Heptares, a GPCR structure-guided drug discovery and development company, believes the grant will lead to a viable treatment option for cocaine dependence. Right now, there are currently no approved GPCR medical treatments. G-protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes. As cell surface receptors, they act like an inbox for messages in the form of light energy, peptides, lipids, sugars, and proteins.
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"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," said Fiona Marshall, Heptares' Chief Scientific Officer and co-founder. "We are using our structure-based design approaches to identify and optimize highly selective Orexin-1 antagonists, and with the help of this grant from NIDA we intend to progress these through to clinical development."
Implicated in moderating cravings for a number of substances, including cocaine, the Orexin-1 receptor is the obvious target for a potential antagonist. Such an antagonists of the receptor has proven to be effective in models of cocaine addiction and dependence, but has yet to be subject to actual clinical trials. Supported by the grant from NIDA, Heptares will develop an effective candidate antagonist in the form of a molecule and then take this molecule through pre-clinical development. The structure-based drug design technology of Heptares has led to the past engineering of drugs for highly validated, yet historically challenging PCRs.