Research and Development
THX-160: A Novel Pharmaceutical Formulation Containing a Specific CB2 Receptor Agonist for the Treatment of Pain
Studies suggest that cannabinoids may be useful in treating acute and chronic pain. The endocannabinoid system appears to have important regulatory functions throughout the human body. The system consists of the cannabinoid 1 and 2 (CB1 and CB2) receptors, the CB receptor ligands N‑arachidonoylethanolamine (anandamide or AEA) and 2‑arachidonoylglycerol (2‑AG) as well as the endocannabinoid-synthesizing and degrading enzymes. CB2 receptors have been shown to modulate acute pain, chronic inflammatory pain, post-surgical pain, cancer pain and pain associated with nerve injury.
To date, prescription opioids are considered to be the most effective treatment for moderate-to-severe pain, but their abuse has been identified by the U.S. Food and Drug Administration (FDA) and the Centers for Disease Control (CDC) as a significant public health issue. They produce tolerance, dependence, and are associated with major abuse liabilities. The respiratory depression associated with high doses has led to a catastrophic increase in the number of drug overdose deaths in the United States.
The utilization of the power of the endocannabinoid system, and especially the activation of the CB2 receptor, lead Therapix’s Chief Scientific Advisor, Professor Raphael Mechoulam to synthesize an innovative specific CB2 receptor agonist, HU-433. HU-433 is a key component in Therapix’s proprietary formulation THX-160 for the treatment of pain.
Therapix conducted a number of successful in-vivo studies evaluating the effect of THX-160 in animal models of pain perception. In the preclinical studies, THX-160 was well tolerated and did not cause any significant adverse clinical effects. In addition, preclinical efficacy studies in animals demonstrated the analgesic superiority of THX-160 over control and were comparable to high-dose morphine analgesic effects and in some instances exerted greater potency. The efficacy and safety of THX-160 was shown for both acute and chronic pain in these preclinical studies.