FDA Approves First Once-Monthly Injectable Buprenorphine for Opioid Use Disorder

The Food and Drug Administration (FDA) has approved Sublocade, the first once-monthly injectable buprenorphine product for the treatment of moderate-to-severe opioid use disorder (OUD) in adults who have initiated treatment with a transmucosal (absorbed through mucus membrane) buprenorphine-containing product. Sublocade is indicated for patients who have been on a stable dose of buprenorphine treatment for a minimum of seven days and is meant to be used as part of a complete treatment program that includes counseling and psychosocial support.

“Sublocade provides a new treatment option for patients in recovery who may value the benefits of a once-monthly injection compared to other forms of buprenorphine,” the FDA stated in a press release.

The FDA approval of Sublocade was based in part on the results of two clinical studies of 848 adults who had a diagnosis of moderate-to-severe OUD and began treatment with buprenorphine/naloxone sublingual film (absorbed under the tongue). Sublocade provided sustained therapeutic plasma levels of buprenorphine over the one-month dosing interval, according to Indivior Inc., manufacturer of the medication.

In a 24-week phase 3 trial, researchers randomized patients to one of the following three regimens: six once-monthly Sublocade 300 mg doses; two once-monthly Sublocade 300 mg doses followed by four once-monthly 100 mg doses; or six once-monthly injections of placebo. According to Indivior, both dosage regimens of Sublocade were shown to be superior to placebo in achieving more illicit opioid-free weeks.

“The FDA is requiring postmarketing studies to assess which patients would benefit from a higher dosing regimen, to determine whether Sublocade can be safely initiated without a dose-stabilization period of sublingual buprenorphine, to assess the feasibility of administering Sublocade at a longer interdose interval than once monthly, and to determine a process for transitioning patients with long-term stability on a transmucosal buprenorphine dose to a monthly dose of Sublocade without the use of a higher dose for the first two months of treatment (loading dose),” the agency’s press release stated.

The most common side effects of Sublocade include constipation, nausea, vomiting, headache, drowsiness, injection site pain, itching (pruritus) at the injection site, and abnormal liver function tests. The safety and efficacy of Sublocade have not been established in children or adolescents under 17 years of age or adults over age of 65.

Sublocade features a boxed warning that notes the dangers of administering the drug intravenously instead of subcutaneously: “Sublocade forms a solid mass upon contact with body fluids and may cause occlusion, local tissue damage, and thrombo-embolic events, including threatening pulmonary emboli, if administered intravenously.”

The medication must be prescribed and dispensed as part of a Risk Evaluation and Mitigation Strategy to ensure that the product is not distributed directly to patients, the FDA noted.