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OxyTrex is an investigational oral combination analgesic developed by Pain Therapeutics (now Cassava Sciences) for the treatment of moderate-to-severe chronic pain, including osteoarthritis and chronic low back pain. The formulation consists of a therapeutic dose of the mu-opioid receptor agonist oxycodone and an ultra-low dose (1 microgram) of the opioid antagonist naltrexone. This combination is designed to enhance the analgesic efficacy of oxycodone while simultaneously reducing the development of opioid tolerance and physical dependence. The mechanism of action involves preventing the aberrant switch in opioid receptor G-protein coupling from inhibitory (Gi) to excitatory (Gs) signaling, which is associated with chronic opioid exposure. Clinical Phase III trials demonstrated that OxyTrex could provide effective pain relief with significantly lower physical dependence and a reduced incidence of common opioid-related side effects such as constipation and somnolence compared to oxycodone alone.
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