Samidorphan
Small molecule targets OPRD1, OPRK1, OPRM1 via activation / inhibition
Trials 24 · a red edge is where a trial was stopped
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 18 trials | ||||||
| Phase 1 | NCT05547100 | Sep → Nov 2022 | — | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT04987658 | Jul 2021 → Aug 2023 | bipolar I disorder | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT02804568 | Jun → Aug 2016 | schizophrenia | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT02504463 | Jun → Sep 2015 | — | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT02413281 | Mar → Sep 2015 | — | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT02218021 | Aug → Nov 2014 | — | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01366001 | Aug 2011 → Feb 2012 | cocaine abuse | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00800319 | Dec 2008 → Feb 2009 | alcohol dependence | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 25 trials | ||||||
| Phase 2 | NCT02161718 | May 2014 → Jan 2017 | alcohol-related disorders, schizophrenia | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01903837 | Jun 2013 → Dec 2014 | schizophrenia | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01500200 | Dec 2011 → Mar 2013 | major depressive disorder | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01098435 | May 2010 → May 2011 | binge eating disorder | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT00981617 | Oct 2009 → Aug 2010 | alcohol dependence | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 310 trials | ||||||
| Phase 3 | NCT06649214 | Nov 2024 → Apr 2026 overdue | schizophrenia | Qilu Pharmaceutical Co., Ltd. | Not yet recruiting | No outcome recorded |
| Phase 3 | NCT05303064 | Jun 2022 → Sep 2026 expected | bipolar I disorder, schizophrenia | Alkermes, Inc. | Recruiting | No outcome recorded |
| Phase 3 | NCT04987229 | Oct 2021 → Sep 2027 expected | bipolar I disorder, schizophrenia | Alkermes, Inc. | Enrolling by invitation | No outcome recorded |
| Phase 3 | NCT03610048 | Aug 2018 → May 2020 | major depressive disorder | Alkermes, Inc. | Terminated | No outcome recorded |
| Phase 3 | NCT03201757 | Jun 2017 → Sep 2023 | bipolar I disorder, schizophrenia, schizophreniform disorder | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT03188185 | Jun 2017 → Feb 2020 | major depressive disorder | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT03187769 | Jun 2017 → Dec 2021 | bipolar I disorder, schizophrenia, schizophreniform disorder | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT02873208 | Aug 2016 → Oct 2019 | schizophrenia | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT02694328 | Mar 2016 → Nov 2018 | schizophrenia | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT02634346 | Dec 2015 → May 2017 | schizophrenia | Alkermes, Inc. | Completed | No outcome recorded |
| Phase 41 trial | ||||||
| Phase 4 | NCT06740890 | Jun 2025 → Apr 2027 expected | bipolar disorder, schizoaffective disorder, schizophrenia | New York State Psychiatric Institute | Recruiting | No outcome recorded |
Also used as a comparator or background therapy in 1 trial
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 1 | NCT01046539 Comparator | Jan → Mar 2010 | substance-related disorder | National Institute on Drug Abuse (NIDA) | Completed | No outcome recorded |
Evidence & citations 17 cited values
Every value below carries the sentence it was read from. 26 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Samidorphan | “BUP/SAM is a fixed-dose combination of buprenorphine, a partial μ-opioid receptor agonist and κ-opioid receptor antagonist, and samidorphan, a μ-opioid receptor antagonist...” PMID 30102427 ↗ Aug 201819“Efficacy and Safety of a Combination of Olanzapine and Samidorphan in Adult Patients With an Acute Exacerbation of Schizophrenia: Outcomes From the Randomized, Phase 3...” PMID 32141723 ↗ Mar 2020 “In ENLIGHTEN-2, combining olanzapine with the opioid receptor antagonist samidorphan (OLZ/SAM) mitigated olanzapine-associated weight gain.” PMID 36305696 ↗ Mar 2023 “Olanzapine will be gradually increased to a target dose of 10mg/samidorphan 5mg (Range: 5-20mg Olanzapine/samidorphan 5mg)” NCT04987658 ↗ “evaluated weight effects of combination olanzapine and samidorphan (OLZ/SAM) versus olanzapine in early-phase illness.” PMID 36946605 ↗ Mar 2023 “5 mg Olanzapine/10 mg Samidorphan dose approved for use in treatment for schizophrenia and bipolar I disorder” NCT05547100 ↗ “Coated bilayer tablet containing 10 mg, 15 mg or 20 mg olanzapine and 10 mg samidorphan” NCT02873208 ↗ “OLZ/SAM refers to the fixed dose combination of olanzapine and samidorphan.” NCT05303064 ↗ “Olanzapine and Samidorphan fixed dose coated tablet taken once daily” NCT04987229 ↗ “2 mg/2 mg of buprenorphine/samidorphan (the 2/2 dosage group)” PMID 26869247 ↗ Feb 2016 “Samidorphan + buprenorphine, administered sublingually” NCT03188185 ↗ “samidorphan + buprenorphine administered sublingually” NCT03610048 ↗ “10-mg samidorphan (a novel opioid system modulator)” PMID 30348514 ↗ Oct 2018 “Olanzapine + samidorphan, daily oral dosing” NCT03201757 ↗ |
| Known as | ALKS 33 | “A Study of [14c]-Samidorphan (Also Known as ALKS 33) in Healthy, Male Volunteers” NCT02504463 ↗ |
| Known as | ALKS 33: RDC-0313. | “ALKS 33: RDC-0313.” NCT01366001 ↗ |
| Known as | Low dose samidorphan (ALKS 33) | “Low dose samidorphan (ALKS 33)” NCT01903837 ↗ |
| Known as | RDC-0313 | “In collaboration with the National Institute on Drug Abuse (NIDA), Alkermes, Inc. is investigating a fixed-dose combination product consisting of ALKS 33 (also referred to as...” NCT01366001 ↗4“This study will evaluate the safety and efficacy of ALKS33 (RDC-0313) compared with placebo in adults with alcohol dependence.” NCT00981617 ↗ |
| Known as | RDC-0313-00 | ChEMBL registry synonym — accepted as the source's own label CHEMBL426084 ↗ |
| Known as | Samidorfano | ChEMBL registry synonym — accepted as the source's own label CHEMBL426084 ↗ |
| Known as | SAMIDORPHAN COMPONENT OF ALKS-5461 | ChEMBL registry synonym — accepted as the source's own label CHEMBL426084 ↗ |
| Known as | Samidorphan l-malate component of lybalvi | ChEMBL registry synonym — accepted as the source's own label CHEMBL426084 ↗ |
| Known as | Samidorphan malate | ChEMBL registry synonym — accepted as the source's own label CHEMBL426084 ↗ |
| Action | Activate | “Kappa opioid receptor partial agonist” CHEMBL426084 ↗1“Delta opioid receptor partial agonist” CHEMBL426084 ↗ |
| Action | Inhibit | “Mu opioid receptor antagonist” CHEMBL426084 ↗1“antagonist, samidorphan” PMID 26869247 ↗ Feb 2016 |
| Modality | Small molecule | — CHEMBL426084 ↗ |
| Route | Oral | “1 mg ALKS33 (RDC-0313) provided as capsules for daily oral administration” NCT00981617 ↗ |
| Target | OPRD1 | “Delta opioid receptor partial agonist” CHEMBL426084 ↗ |
| Target | OPRK1 | “Kappa opioid receptor partial agonist” CHEMBL426084 ↗ |
| Target | OPRM1 | “Mu opioid receptor antagonist” CHEMBL426084 ↗ |