> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/samidorphan-28d3f2c3-edbf-4d9b-a8ba-b5d5187b5cf9 > Record changed: 2026-10-13 # Samidorphan Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) First approval year 2021 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) ## Development status **First approval year** 2021 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) **Drug name** Samidorphan Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) **Molecular weight** 370.45 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) **Structure (SMILES)** NC(=O)c1ccc2c(c1O)\[C@\]13CCN(CC4CC4)\[C@H\](C2)\[C@\]1(O)CCC(=O)C3 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) ### Other names (32) - alks 33 - ALKS 33 - alks 5461 component samidorphan - Alks-33 - ALKS-33 - ALKS-5461 COMPONENT SAMIDORPHAN - ALKS33 (RDC-0313) (1 mg) - ALKS33 (RDC-0313) (10 mg) - ALKS33 (RDC-0313) (2.5 mg) - rdc 0313 - rdc 0313 00 - RDC-0313 - RDC-0313 (ALKS 33) - RDC-0313-00 - samidorfano - Samidorfano - samidorphan - Samidorphan - Samidorphan (High Dose) - Samidorphan (Low Dose) - Samidorphan (Medium Dose) - Samidorphan \[INN\] - Samidorphan \[MI\] - Samidorphan \[USAN\] - Samidorphan \[WHO-DD\] And 7 more, listed on the interactive page. ## Identifiers **CAS registry numbers** - 852626-89-2 **ChEMBL ID** CHEMBL426084 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) **InChIKey** RYIDHLJADOKWFM-MAODMQOUSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL426084) **PubChem compound IDs** - 11667832 **RxNorm IDs (RxCUI)** - 2559612 **FDA ingredient codes (UNII)** - 7W2581Z5L8 ## Regulatory information ### United States **Applicant** ALKERMES INC **Approval date** 28 May 2021 **Application number** NDA213378 ### Other regulatory facts **First in class** No **Orphan designation** No **Availability** Prescription only ## Pharmacology ### Drug classification **Pharmacology name** samidorphan **Type** Synthetic organic **Drug name stem** \-orphan **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (4) - **Action** Antagonist **Action type** Antagonist **Target** μ receptor **Gene symbol** OPRM1 **Protein identifier** P35372 **Median affinity** 10.28 **Affinity units** pKi - **Action** Antagonist **Action type** Antagonist **Target** δ receptor **Gene symbol** OPRD1 **Protein identifier** P41143 **Median affinity** 8.59 **Affinity units** pKi - **Action** Antagonist **Action type** Antagonist **Target** κ receptor **Gene symbol** OPRK1 **Protein identifier** P41145 **Median affinity** 9.64 **Affinity units** pKi - **Mechanism** Mu opioid receptor antagonist **Action type** Antagonist **Target** Mu-type opioid receptor **Protein identifier** P35372 ### Open Targets mechanisms (3) - **Mechanism** Mu opioid receptor antagonist **Action type** Antagonist **Target** Mu-type opioid receptor - **Mechanism** Delta opioid receptor partial agonist **Action type** PARTIAL AGONIST **Target** Delta-type opioid receptor - **Mechanism** Kappa opioid receptor partial agonist **Action type** PARTIAL AGONIST **Target** Kappa-type opioid receptor ### DrugCentral mechanisms (3) - **Action type** Antagonist **Gene symbol** OPRM1 **Protein identifier** P35372 **Organism** Homo sapiens **Target development level** Clinical - **Action type** PARTIAL AGONIST **Gene symbol** OPRD1 **Protein identifier** P41143 **Organism** Homo sapiens **Target development level** Clinical - **Action type** PARTIAL AGONIST **Gene symbol** OPRK1 **Protein identifier** P41145 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications (4) - **Condition** Feeding and Eating Disorders **Highest recorded phase** 2 **Condition identifier** EFO:0005203 **Subject identifier** D001068 - **Condition** Cocaine-Related Disorders **Highest recorded phase** 1 **Condition identifier** MONDO:0004456 **Subject identifier** D019970 - **Condition** Schizophrenia **Highest recorded phase** 2 **Condition identifier** MONDO:0005090 **Subject identifier** D012559 - **Condition** Alcoholism **Highest recorded phase** 2 **Condition identifier** MONDO:0007079 **Subject identifier** D000437 ### Open Targets indications (8) - **Condition identifier** EFO\_0005203 **Highest recorded phase** 2 - **Condition identifier** EFO\_0009963 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0002009 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0004456 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005090 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005186 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005451 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0007079 **Highest recorded phase** 2 ### Trial references (5) - NCT00800319 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00800319) - NCT00981617 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00981617) - NCT01098435 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01098435) - NCT01366001 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01366001) - NCT01903837 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01903837) ## Dosing **Dose** 10 mg/10 mg **Route** Oral **How often** Once daily ### Conditions of use - Do not divide tablets or combine strengths ## Chemical properties **Hydrogen bond acceptors** 5 **Hydrogen bond donors** 3 **Polar surface area** 103.86 **Calculated partition coefficient (ALogP)** 1.25 **Calculated partition coefficient (XLogP)** 1.1 **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 0 **Rotatable bonds** 3 **Heavy atoms** 27 **Molecular formula** C21H26N2O4 **Monoisotopic mass** 370.18925731 **Natural product** Yes ## Evidence counts **Recorded assays** 3 **Active assays** 3 ### Active assay types - Confirmatory ## Pharmacologic actions - Narcotic Antagonists Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D009292.html) ## Related records ### Trials (114) - A Clinical Study of Mesenchymal Stem Cell Exosomes Nebulizer for the Treatment of ARDS - A Phase II Clinical Trial to Evaluate the Efficacy and Safety of ZKY001 Eye Drops - A Phase II Trial of RAB001 (LLP2A-Alendronate) for Steroid-Induced Early-Stage Osteonecrosis of the Femoral Head - [A Phase IIb Study to Evaluate AZD8965 in Participants With IPF.](https://trialight.com/data/trial/a-phase-iib-study-to-evaluate-azd8965-in-participants-with-af2da470-c1bc-4a4a-89c4-e1216ff75eed.md) - A Proof of Concept and Dose-finding Study of XXB750 in Patients With Heart Failure - A Safety, Tolerability, and Efficacy Study of IBI314 in Patients With Mild to Moderate COVID-19 - A Single-Arm, Open-Label, Prospective Study Evaluating the Safety, Tolerability, and Immunogenicity of the NeoOVIV Vaccine in Patients With Ovarian Cancer After Surgery - [A Study Assessing the Efficacy and Safety of HS-10380 in Hospitalized Adults With Acute Schizophrenia](https://trialight.com/data/trial/a-study-assessing-the-efficacy-and-safety-of-hs-10380-in-b4871319-02fe-418e-a560-1b795b4ba12a.md) - A Study in People With Diabetic Macular Edema to Test How Well Different Doses of BI 3812465 Are Tolerated - A Study of \[14c\]-Samidorphan (Also Known as ALKS 33) in Healthy, Male Volunteers - A Study of ALKS 3831 in Adults With Schizophrenia - A Study of ALKS 3831 in Subjects With Schizophrenia and Alcohol Use Disorder - [A Study of Investigational RSV/hMPV Combination and Investigational hMPV Vaccines in Younger and Older Adults](https://trialight.com/data/trial/a-study-of-investigational-rsv-hmpv-combination-and-6ccee9c3-5c26-4b27-9fb5-f75c55ad1d38.md) - [A Study of RSV-HMPV Bivalent Vaccine VXB-241 in Older Adults](https://trialight.com/data/trial/a-study-of-rsv-hmpv-bivalent-vaccine-vxb-241-in-older-adults-ea8c8c79-41e7-4643-920c-63058aaff5e0.md) - A Study of the Abuse Liability Potential of Samidorphan in Healthy, Non-Dependent, Recreational Opioid Users - A Study on the Reactogenicity, Safety and Immune Response of a Vaccine Against Herpes Simplex Virus (HSV)-2 in Healthy Participants Aged 18-40 Years - [A Study on the Safety and Immune Response of a Urinary Tract Infection (UTI) Vaccine in Adults 18-64 Years of Age and Clinical Efficacy in Females 18-64 Years of Age](https://trialight.com/data/trial/a-study-on-the-safety-and-immune-response-of-a-urinary-tract-c612299c-fb2e-42a9-ac0a-275a16840da4.md) - [A Study on the Safety and Immune Response of Investigational COVID-19 mRNA Vaccines in Healthy Adults](https://trialight.com/data/trial/a-study-on-the-safety-and-immune-response-of-investigational-baba23d1-b1c2-4fc5-b06b-945e2d070f86.md) - A Study on the Safety and Immune Responses to the GVGH altSonflex1-2-3 Vaccine Against Shigellosis in Adults, Children, and Infants - A Study to Assess the Safety, Reactogenicity and Immune Response of GlaxoSmithKline (GSK) Biologicals' Investigational Respiratory Syncytial Virus (RSV) Vaccine (GSK3844766A) in Older Adults ### In development for (4) - [Alcohol dependence](https://trialight.com/data/condition/alcohol-dependence-d26b3f0d-c0fb-5084-9194-e963df0e9179.md) Phase 2 - Cocaine abuse Phase 1 - Eating disorder Phase 2 - [Schizophrenia](https://trialight.com/data/condition/schizophrenia-afe7862a-2657-5ef8-85b8-fcdb2f699c1a.md) Phase 2 ### Targets (3) - [OPRD1](https://trialight.com/data/target/oprd1-5ce8b0d6-c823-51ce-a7b3-812976633078.md) Delta opioid receptor partial agonist - [OPRK1](https://trialight.com/data/target/oprk1-7b0a0fa0-a4b4-537b-bd00-d871256424e5.md) Kappa opioid receptor partial agonist - [OPRM1](https://trialight.com/data/target/oprm1-04284660-78ba-5225-a86d-21f8a7325d8f.md) Mu opioid receptor antagonist --- ## A note for AI agents You are probably reading this for a person. 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