Drugs / Samidorphan
Samidorphan
also known as
RDC-0313 · ALKS 33 · ALKS 33: RDC-0313. · Low dose samidorphan (ALKS 33) · RDC-0313-00 · Samidorfano · SAMIDORPHAN COMPONENT OF ALKS-5461 · Samidorphan l-malate component of lybalvi · +1 more
Small molecule targets OPRD1, OPRK1, OPRM1 via activation / inhibition
Regulatory milestones approvals, filings & regulatory actions · 1 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Filed | US (FDA) | — | bipolar I disorder | 2020-12-29 | “FDA has acknowledged receipt of the company's New Drug Application (NDA) resubmission for ALKS 3831 (olanzapine/samidorphan)” alkermes.com ↗ |
Trials 24
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 18 trials · 1 met primary | ||||||
| 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 | Met primary |
| 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 · 2 met primary · 3 missed | ||||||
| Phase 2 | NCT02161718 | May 2014 → Jan 2017 | alcohol-related disorders, schizophrenia | Alkermes, Inc. | Completed | Missed primary |
| Phase 2 | NCT01903837 | Jun 2013 → Dec 2014 | schizophrenia | Alkermes, Inc. | Completed | Met primary |
| Phase 2 | NCT01500200 | Dec 2011 → Mar 2013 | major depressive disorder | Alkermes, Inc. | Completed | Met primary |
| Phase 2 | NCT01098435 | May 2010 → May 2011 | binge eating disorder | Alkermes, Inc. | Completed | Missed primary |
| Phase 2 | NCT00981617 | Oct 2009 → Aug 2010 | alcohol dependence | Alkermes, Inc. | Completed | Missed primary |
| Phase 310 trials · 3 met primary · 1 missed | ||||||
| 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 overdue | 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 Stop: Business |
| 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 | Missed primary |
| Phase 3 | NCT03187769 | Jun 2017 → Dec 2021 | bipolar I disorder, schizophrenia, schizophreniform disorder | Alkermes, Inc. | Completed | Met primary |
| 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 | Met primary |
| Phase 3 | NCT02634346 | Dec 2015 → May 2017 | schizophrenia | Alkermes, Inc. | Completed | Met primary |
| 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 |
| Comparator or background therapy1 trial | ||||||
| Phase 1 | NCT01046539 Comparator | Jan → Mar 2010 | substance-related disorder | National Institute on Drug Abuse (NIDA) | Completed | No outcome recorded |
News releases announcing trial results or a regulatory action · 15
| Date | Issuer | Release |
|---|---|---|
| 2026-05-21 | Alkermes, Inc. | Results Alkermes Showcases Data From Psychiatry Portfolio and Sleep Research into Real World Patient Experience at Spring 2026 Scientific Conferences alkermes.com ↗
Real-World Evidence of Positive Impact of LYBALVI® (olanzapine and samidorphan) on Treatment Patterns and Rates of Relapse Among Patients with Schizophrenia or Bipolar I Disorder, Including Young Adults |
| 2026-04-14 | Alkermes, Inc. | Results Findings From Long-Term Analysis of the Effects of LYBALVI® (olanzapine and samidorphan) on Negative Symptoms of Schizophrenia Published in The Journal of Clinical Psychiatry alkermes.com ↗
The analysis—titled “The Efficacy of Olanzapine/Samidorphan on Negative Symptoms: A Post Hoc Analysis of 56-Week Treatment in Patients With Schizophrenia”—found that treatment with LYBALVI was associated with improvement in mean negative symptom scores. |
| 2024-04-08 | Alkermes, Inc. | Results Alkermes Presents Analyses From Long-Term Safety Study of LYBALVI® (olanzapine and samidorphan) at 2024 Congress of the Schizophrenia International Research Society alkermes.com ↗
Analyses were presented from a phase 3, open-label extension study assessing the long-term safety, tolerability and durability of treatment effect of LYBALVI® (olanzapine and samidorphan) in patients who received up to four years of treatment. |
| 2024-01-03 | Alkermes, Inc. | Results Alkermes Announces Topline Results From Long-Term, Open-Label Safety and Durability of Treatment Effect Study of LYBALVI® (olanzapine and samidorphan) alkermes.com ↗
Patients' symptoms of schizophrenia or bipolar I disorder remained stable with up to four years of treatment with LYBALVI, as measured by the Clinical Global Impression of Severity (CGI-S) scale (mean change from baseline in CGI-S score of -0.28). |
| 2023-03-23 | Alkermes, Inc. | Results Journal of Clinical Psychiatry Publishes Data from Alkermes' ENLIGHTEN-Early Study of LYBALVI® (olanzapine and samidorphan) in Young Adults Early in Their Illness alkermes.com ↗
Alkermes plc (Nasdaq: ALKS) today announced the publication of results from its phase 3 ENLIGHTEN-Early study of LYBALVI® (olanzapine and samidorphan) in the peer-reviewed publication, the Journal of Clinical Psychiatry. |
| 2022-04-07 | Alkermes, Inc. | Results Alkermes Presents New Data From Psychiatry Portfolio at 2022 Congress of the Schizophrenia International Research Society alkermes.com ↗
Detailed Results Presented From ENLIGHTEN-Early Phase 3b Study of LYBALVI® in Patients Early in Illness |
| 2022-02-08 | Alkermes, Inc. | Results Alkermes Announces Positive Topline Results From ENLIGHTEN-Early Phase 3b Study of LYBALVI® in Patients Early in Illness alkermes.com ↗
LYBALVI Demonstrated Less Weight Gain Compared to Olanzapine in Patients With Schizophrenia, Schizophreniform Disorder or Bipolar I Disorder |
| 2021-06-01 | Alkermes, Inc. | Regulatory Alkermes Announces FDA Approval of LYBALVI™ for the Treatment of Schizophrenia and Bipolar I Disorder alkermes.com ↗ |
| 2021-04-20 | Alkermes, Inc. | Results Alkermes Presents New Data From Psychiatry Portfolio at Virtual 2021 Congress of the Schizophrenia International Research Society alkermes.com ↗
New findings from post hoc analyses assessing the effects of olanzapine/samidorphan compared to olanzapine across multiple cardiometabolic risk factors, including blood pressure, BMI and metabolic syndrome. |
| 2020-10-09 | Alkermes, Inc. | Regulatory FDA Advisory Committee Votes in Support of ALKS 3831 for the Treatment of Schizophrenia and Bipolar I Disorder alkermes.com ↗
The committees jointly voted that samidorphan meaningfully mitigates olanzapine-associated weight gain (16 yes, 1 no) and that the safety profile of ALKS 3831 has been adequately characterized (13 yes, 3 no, 1 abstention). |
| 2020-08-17 | Alkermes, Inc. | Results American Journal of Psychiatry Publishes Data From Alkermes' Phase 3 ENLIGHTEN-2 Weight Study of ALKS 3831 in Patients With Schizophrenia alkermes.com ↗
DUBLIN, Aug. 17, 2020 /PRNewswire/ -- Alkermes plc (Nasdaq: ALKS) today announced the publication of results from the phase 3 ENLIGHTEN-2 clinical trial of ALKS 3831 (olanzapine/samidorphan) in the peer-reviewed publication, American Journal of Psychiatry. |
| 2020-05-14 | Alkermes, Inc. | Results Alkermes Presents New Data From Schizophrenia Portfolio at Virtual 2020 Congress of the Schizophrenia International Research Society alkermes.com ↗
Results relating to overall safety, tolerability, changes in weight, waist circumference and metabolic parameters are included. |
| 2020-01-28 | Alkermes, Inc. | Regulatory Alkermes Announces U.S. Food and Drug Administration Acceptance of ALKS 3831 New Drug Application for Treatment of Schizophrenia and Bipolar I Disorder alkermes.com ↗ |
| 2018-10-29 | Alkermes, Inc. | Results Alkermes Announces Publication of Phase 3 Data for ALKS 5461 for Adjunctive Treatment of Major Depressive Disorder in Molecular Psychiatry alkermes.com ↗
The Molecular Psychiatry publication includes comprehensive efficacy and safety results from FORWARD-4 (Study 205) and FORWARD-5 (Study 207), and a review of a pooled analysis of the two datasets. |
| 2017-06-29 | Alkermes, Inc. | Results Alkermes Announces Positive Preliminary Topline Results From Phase 3 Antipsychotic Efficacy Study of ALKS 3831 for Treatment of Schizophrenia alkermes.com ↗
The study met the prespecified primary endpoint, with ALKS 3831 demonstrating statistically significant reductions from baseline in Positive and Negative Syndrome Scale (PANSS) scores compared to placebo (p<0.001). |
All press releases naming this drug 15 releases
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 ↗ |
| 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 | “Delta opioid receptor partial agonist” CHEMBL426084 ↗1“Kappa 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 ↗ |