Dinalbuphine sebacate
Dinalbuphine sebacate, also known as nalbuphine sebacate or as sebacoyl dinalbuphine ester and sold under the brand name Naldebain, is a non-controlled opioid analgesic which is used as a 7-day long-acting injection in the treatment of moderate to severe postoperative pain. It was developed by Lumosa Therapeutics and was approved in Taiwan in the spring of 2017; development is ongoing in the United States. The compound is a diester of nalbuphine joined via a sebacic acid linker, and acts as a long-lasting prodrug of nalbuphine via slow hydrolysis. It was developed to extend the duration of action of nalbuphine, which has a short duration and requires frequent injections. Whereas nalbuphine must be injected every 4 to 6 hours, a single injection of DNS lasts for up to 7 to 10 days. Nalbuphine, and hence DNS, acts as a mixed agonist/antagonist opioid modulator, or more specifically as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor and as a high-efficacy partial agonist of the κ-opioid receptor.
