In the US, the epidemic of opioid is a countrywide public health crisis. Several obstacles like problem in adhering to plans of treatment, access to prescribers and treatment, and social stigma are faced by individuals undergoing treatment. Sublocade™ is a partial agonist used in adults for treating moderate-to-severe opioid use disorder (OUD). It was previously recognized as RBP-6000. Indivior discovered and developed it, and submitted an application for a new drug in May 2017 to the US Food and Drug Administration (FDA). On October 2017, 18 votes were received in favor of Sublocade™ by FDA’s Drug Safety and Risk Management Advisory Committee and the Psychopharmacologic Drugs Advisory Committee. FDA approved the drug on November 2017 and it is planned to be launched in Q1 2018 in the US market by Indivior.
Mechanism of action
A partial agonist of mu-opioid receptor, namely buprenorphine, is the main component of Sublocade™. The mechanism of action of this drug is by the delivery of sustained plasma levels of buprenorphine, transmuting into high mu-opioid receptor present in the brain.
In clinical trials, the healthcare providers have given profile of systemic safety for Sublocade™, which is in line with the recognized safety profile of transmucosal buprenorphine, apart from reactions on the site of injection, which were reported by a small percentage of patients (16.5%). Fatigue, somnolence, sedation, headache, abnormal liver enzymes, vomiting, nausea, and constipation were some of the common adverse reactions. The reactions observed on the site of injection were not serious and one resulted in the treatment discontinuation study. The drug has a boxed warning noting that intravenous administration of this medication could lead to death or serious harm. Other precautions and warnings in the prescription include hepatic events, adrenal insufficiency, respiratory depression, risk of misuse, abuse, and addiction, and opioid withdrawal with sudden discontinuation.
Availability of medication
Sublocade™ should only be prepared and administered by healthcare providers. Moreover, it is subjected to a risk evaluation and mitigation strategy (REMS) program encompassing a limited system of distribution for ascertaining the administration of Sublocade™ only by a healthcare provider. Hence, generally a retail pharmacy cannot distribute Sublocade™.
Sublocade™ is available in doses of 100 mg and 300 mg to be administered subcutaneously. The availability of drug for subcutaneousinjection was announced by Indivior to treat moderate-to-severe OUD in patients having previously started treatment with a transmucosal buprenorphine-containing product with a dose adjustment for greater than or equal to 7 days. Sublocade™ has a recommended dose of 300 mg monthly (to be administered subcutaneously) after start and dose adjustment with transmuscosal buprenorphine. After initial 2 months, a monthly maintenance dose of 100 mg should be administered which may be increased to 300 mg monthly to those not presenting a satisfactory clinical response but tolerating a dose of 100 mg.
The administration of Sublocade™ should be restricted in patients with hypersensitivity to buprenorphine or any constituent of the ATRIGEL® delivery system. Strict monitoring of patients on CPY3A4 substrates and inhibitors should be performed for possibility of under- or over-dosing.