Samidorphan
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| Elimination half-life | 7-9 hours[1] |
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| Formula | C21H26N2O4 |
| Molar mass | 370.441 g/mol g·mol−1 |
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Samidorphan (ALKS-33) is a selective opioid antagonist which blocks the μ-opioid receptor, but without blocking δ-opioid or κ-opioid receptors. It has been investigated for the treatment of alcoholism and cocaine addiction,[2][3] showing similar efficacy to naltrexone but possibly with reduced side effects.
However, it has attracted much more attention as part of the combination product ALKS-5461, where samidorphan is combined with the mixed μ-opioid agonist and κ-opioid antagonist opioid modulator buprenorphine, as an antidepressant. Buprenorphine has shown antidepressant effects in some human studies, thought to be because of its antagonist effects at the κ-opioid receptor, but has not been further developed for this application because of its μ-opioid agonist effects and consequent abuse potential. By combining buprenorphine with samidorphan to block the μ-opioid agonist effects, the combination acts more like a selective κ-opioid antagonist, and produces only antidepressant effects, without typical μ-opioid effects being evident.[4][5]
It is also being studied in combination with olanzapine, as ALKS-3831, for use in schizophenia.[6] It is hoped it will be effective while resulting in less weight gain. Phase 2 studies have begun.[7]
See also
References
- ^ Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers Clin Ther. 2015 Feb 1;37(2):338-48. doi: 10.1016/j.clinthera.2014.10.001. Epub 2014 Oct 29.
- ^ Hillemacher, T.; Heberlein, A.; Muschler, M. A.; Bleich, S.; Frieling, H. (2011). "Opioid modulators for alcohol dependence". Expert Opinion on Investigational Drugs. 20 (8): 1073–1086. doi:10.1517/13543784.2011.592139. PMID 21651459.
- ^ ALK33BUP-101: Safety and Pharmacodynamic Effects of ALKS 33-BUP Administered Alone and When Co-administered With Cocaine
- ^ ALKS 5461 drug found to reduce depressive symptoms in Phase 1/2 study
- ^ Investigational ALKS 5461 Channels ‘Opium Cure’ for Depression
- ^ "Will Alkermes' Antipsychotic ALKS-3831 Become Another Tredaptive?". Forbes. Jan 15, 2013.
- ^ "A Study of ALKS 3831 in Subjects With Schizophrenia and Alcohol Use Disorder".
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