Buprenorphine/Naloxone (Zubsolv^®): A Review in Opioid Dependence

A new sublingual buprenorphine/naloxone tablet (hereafter referred to as buprenorphine/naloxone; Zubsolv^®), combining a long-acting partial µ receptor agonist and an opioid antagonist, is approved for the treatment of opioid dependence in adults and adolescents aged > 15 years. This formulation has a higher bioavailability, better taste and faster sublingual dissolve time than a reference sublingual buprenorphine/naloxone tablet (Suboxone^®), advantages that provide greater patient preference (potentially improving adherence) and importantly may reduce the risk of buprenorphine parenteral abuse by providing similar buprenorphine exposure at an ≈ 30% lower dosage than reference buprenorphine/naloxone. In large phase III trials of up to 28 days, buprenorphine/naloxone was associated with high treatment retention rates during the induction and stabilization phases, and also reduced opioid craving and opioid withdrawal symptoms. Although noninferiority of buprenorphine/naloxone to sublingual buprenorphine tablet during the 2-day induction phase was only shown in one of the two similarly designed trials, pooled analyses confirmed that treatment retention rates were similar in the buprenorphine/naloxone and buprenorphine groups. Where evaluated, noninferiority of buprenorphine/naloxone to sublingual buprenorphine/naloxone film (only approved in the USA) was also demonstrated at 15 days in the stabilization phase. During the 24-week extension study, buprenorphine/naloxone maintenance therapy sustained improvements in opioid craving and addiction severity scores. Buprenorphine/naloxone was generally well tolerated, displaying a tolerability profile that was generally consistent with that seen with reference buprenorphine/naloxone. In conclusion, with potentially greater patient preference and a lower potential for parenteral buprenorphine abuse than reference buprenorphine/naloxone, buprenorphine/naloxone expands the treatment options available for adults and adolescent (aged > 15 years) patients with opioid dependence.