Drug intelligence / Profile preview

naltrexone + guanfacine

Development stage
Unknown
Lead developer
Baylor College of Medicine
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of naltrexone and guanfacine is a pharmaceutical therapy being investigated by the Baylor College of Medicine for the treatment of heroin dependence and the prevention of relapse in detoxified individuals. Naltrexone is a small molecule mu-opioid receptor antagonist that blocks the euphoric effects of opioids and reduces cravings. Guanfacine is an alpha-2A adrenergic receptor agonist, traditionally used as an antihypertensive, which is hypothesized to manage noradrenergic-mediated withdrawal symptoms and reduce stress-induced relapse. This specific combination was evaluated in a Phase 2 randomized, double-blind, placebo-controlled factorial study (NCT00218400) led by Dr. Thomas R. Kosten in St. Petersburg, Russian Federation.

Other names
naltrexone and guanfacine
02

Targets

KOR (Kappa opioid receptor)MOR (Mu opioid receptor)ADRA2A (α2A)DOR (Opioid Receptor Delta 1)

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