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Heroin Addiction and Related Clinical Problems: 2021, 23, N5 (pages: 25 - 36)

RBP-6000: a rationally designed prolonged-release buprenorphine formulation

Wiest K., Shaya G., Somaini L., and Greenwald M.

Summary: Background. RBP-6000 (Sublocade®; Subutex Prolonged Release Solution for Injection®) is a monthly prolonged-release subcutaneous formulation of buprenorphine that has been rationally designed to achieve sustained mu-opioid receptor (MOR) occupancy at levels that suppress withdrawal symptoms, drug-liking and craving, which drive addiction. Method. This review summarises relevant publications identified through online searches. Results. Effective opioid blockade with RBP-6000 was demonstrated in a phase 2 study. Safety and efficacy were demonstrated in a 6-month randomised double-blind placebo-controlled study and a 12-month open-label study. Target buprenorphine plasma concentrations (2–3 ng/mL) that achieve ≥70% MOR occupancy were reached from treatment initiation and sustained throughout the monthly maintenance dosing interval, reducing opioid use, controlling opioid craving and suppressing withdrawal symptoms. In a 6-month open-label extension, opioid abstinence rates increased with treatment duration. Quality of life, employment, social engagement and treatment satisfaction all improved. Hospitalisations, days in hospital and emergency admissions were reduced. The safety profile of RBP-6000 was consistent with that of transmucosal buprenorphine, except for injection site reactions. The 24-month RECOVER study, which followed participants transitioning from phase 3 into the real-world setting, confirmed that improvements in abstinence and psychosocial outcomes were maintained after patients stopped RBP-6000, especially for those who had received ≥12 months' treatment. Conclusion. Once-monthly RBP-6000 provides sustained opioid blockade, aiding long-term abstinence from opioid use and supporting recovery and a return to a meaningful life. Monthly administration by a health professional removes the burden and stigma of daily supervised treatment whilst maintaining the therapeutic alliance and avoiding diversion and misuse.