THX-160

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.