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

By John Lavitt 10/06/15

Doctors are pushing for a naloxone-like medication to treat cocaine dependence.

Doctors are pushing for a naloxone-like medication to treat cocaine dependence.

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.

"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.

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Growing up in Manhattan as a stutterer, John Lavitt discovered that writing was the best way to express himself when the words would not come. After graduating with honors from Brown University, he lived on the Greek island of Patmos, studying with his mentor, the late American poet Robert Lax. As a writer, John’s published work includes three articles in Chicken Soup For The Soul volumes and poems in multiple poetry journals and compilations. Active in recovery, John has been the Treatment Professional News Editor for The Fix. Since 2015, he has published over 500 articles on the addiction and recovery news website. Today, he lives in Los Angeles, trying his best to be happy and creative. Find John on Facebook, Twitter, and LinkedIn.