Samidorphan
Identification
- Summary
Samidorphan is a novel opioid-system modulator, similar to naltrexone, that functions primarily as a μ-opioid receptor antagonist in vivo and is used primarily in combination with antipsychotics to reduce their metabolic dysfunction-associated adverse effects.
- Brand Names
- Lybalvi
- Generic Name
- Samidorphan
- DrugBank Accession Number
- DB12543
- Background
Olanzapine is an effective atypical antipsychotic that, like other antipsychotics, is associated with weight gain, metabolic dysfunction, and increased risk of type II diabetes.5,6 Samidorphan is a novel opioid antagonist structurally related to naltrexone, with a higher affinity for opioid receptors, more potent μ-opioid receptor antagonism, higher oral bioavailability, and a longer half-life, making it an attractive candidate for oral dosing.1,5,11 Although antipsychotic-induced weight gain is incompletely understood, it is thought that the opioid system plays a key role in feeding and metabolism, such that opioid antagonism may be expected to ameliorate these negative effects. Samidorphan has been shown in animal models and clinical trials to ameliorate olanzapine-induced weight gain and metabolic dysfunction.5,6
Samidorphan was first approved as a variety of fixed-dose combination tablets with olanzapine by the FDA on May 28, 2021, and is currently marketed under the trademark LYBALVI™ by Alkermes Inc.11
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 370.449
Monoisotopic: 370.189257325 - Chemical Formula
- C21H26N2O4
- Synonyms
- Samidorphan
- External IDs
- ALKS 33
- ALKS-33
- RDC-0313
- RDC-0313-00
Pharmacology
- Indication
Samidorphan is indicated in combination with olanzapine for the treatment of bipolar I disorder, either as an adjunct to lithium or valproate or as monotherapy for the acute treatment of manic or mixed episodes or as maintenance therapy, and for the treatment of schizophrenia in adults.11
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to manage Bipolar 1 disorder Combination Product in combination with: Olanzapine (DB00334) •••••••••••• ••••• •••••• Used as adjunct in combination to treat Bipolar disorder with manic or mixed episodes Combination Product in combination with: Olanzapine (DB00334) •••••••••••• ••••• •••••• Used in combination to treat Bipolar disorder with manic or mixed episodes Combination Product in combination with: Olanzapine (DB00334) •••••••••••• ••••• •••••• Used as adjunct in combination to treat Bipolar disorder with manic or mixed episodes Combination Product in combination with: Olanzapine (DB00334) •••••••••••• ••••• •••••• Used in combination to treat Schizophrenia Combination Product in combination with: Olanzapine (DB00334) •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Samidorphan, a novel opioid-system modulator, functions primarily as a μ-opioid receptor antagonist and as a κ/δ-opioid receptor partial agonist in vitro with an overall profile consistent with a μ-opioid receptor antagonist in vivo and is currently used to counteract olanzapine-induced adverse effects of weight gain and metabolic dysfunction.11 Samidorphin generally has a mild side effect profile. As an opioid antagonist, it can potentiate opioid withdrawal in dependent patients; it should not be administered within seven days from the last use of short-acting opioids and at least 14 days after cessation of long-acting opioids. Similarly, samidorphan use may lead to life-threatening opioid overdose, either in patients who attempt to overcome the samidorphan-induced opioid blockade or resume opioid use when therapy is interrupted or discontinued.11
Several other effects may be noted in combination with olanzapine, including increased risk for potentially fatal cerebrovascular events in elderly patients with dementia-related psychosis, neuroleptic malignant syndrome, hyperprolactinemia, and tardive dyskinesia. Olanzapine is associated with an increased risk of metabolic dysfunction, including hyperglycemia, type II diabetes, dyslipidemia, and weight gain. Patients may be at increased risk for orthostatic hypotension and syncope, particularly in patients with known cardiovascular/cerebrovascular disease. Leukopenia, neutropenia, and agranulocytosis may occur and should be monitored for; patients with a history of seizure should also be monitored. This combination may exhibit anticholinergic (antimuscarinic) effects. It should be used with caution with other anticholinergic drugs and in patients with urinary retention, prostatic hypertrophy, constipation, paralytic ileus, or related conditions. Serious allergic reactions such as Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) have been reported. Patients may be at increased risk of cognitive and motor impairment; caution while operating machinery is recommended.11
- Mechanism of action
Samidorphan is a novel naltrexone analogue containing a 3-carboxamido group that functions as an opioid receptor modulator, both in vitro and in vivo.1,11 Numerous in vitro studies have demonstrated that samidorphan binds with high affinity to the μ-, κ-, and δ-opioid receptors with Ki values of 0.052 ± 0.0044, 0.23 ± 0.018, and 2.7 ± 0.36 nM, respectively.2,3,4,11 Samidorphan acts as an antagonist at the μ-opioid receptor when it signals through Gαi proteins, a partial agonist when the receptor signals through GαoA, GαoB, and Gαz proteins, and essentially lacks β-arrestin-mediated signalling; samidorphan also acts as a partial agonist at both the κ- and δ-opioid receptors in vitro.2 In addition, both the major N-dealkylated and the major N-oxide human metabolites bind to the μ-, κ-, and δ-opioid receptors (Ki values of 0.26, 23, and 56, and 8, 110, and 280 nM, respectively); the former functions as a μ-opioid receptor agonist and the latter as an antagonist.11 Overall, samidorphan functions primarily as a μ-opioid antagonist in vivo.1
Olanzapine is an efficacious antipsychotic whose use is limited, in part, by known adverse effects mediated through metabolic dysfunction: hyperglycemia/diabetes mellitus, hyperlipidemia, and weight gain.1,5 The exact mechanisms behind this metabolic dysfunction are incompletely understood, but it is known that opioid signalling is involved in feeding and metabolism.5 Clinical studies have demonstrated that the addition of samidorphan to olanzapine helps mitigate its metabolic-related adverse effects; presumably, this is due to opioid receptor signalling, though the exact mechanism remains to be determined.1,6,5 The appropriateness of samidorphan in combination therapy is due in part to its relatively mild side effect profile and low abuse potential.6,7
Target Actions Organism AMu-type opioid receptor antagonistHumans UKappa-type opioid receptor partial agonistHumans UDelta-type opioid receptor partial agonistHumans - Absorption
Samidorphan pharmacokinetics are linear over the range of clinically relevant concentrations, and steady-state kinetics are reached by seven days with once-daily oral administration. Upon reaching steady-state, with a once-daily dose of 10 mg samidorphan combined with 20 mg olanzapine, samidorphan has a mean Cmax of 45.1 ± 11.4 ng/mL and an AUC24h of 364 ± 112 ng*h/mL. Samidorphan has an absolute oral bioavailability of 69% and a Tmax of 1-2 hours.8,9,11
Samidorphan pharmacokinetics are not significantly impacted by food; following a high-fat meal, the Cmax was 0.85 (90% CI 0.76, 0.94) and the AUC 1.03 (90% CI 1.0, 1.05) that for the fasted state.9,10,11
- Volume of distribution
Samidorphan following a single 10 mg oral dose had an apparent volume of distribution between 336.59 ± 75.42 and 557.6 ± 120.51 L, depending on age, gender, and concomitant food consumption.9
- Protein binding
Samidorphan is between 23 and 33 percent bound to plasma proteins.11
- Metabolism
Samidorphan is primarily metabolized by CYP3A4, with minor contributions from CYP3A5, CYP2C19, and CYP2C8.11 The main metabolism products are RDC-9986 (an N-dealkylated metabolite) and RDC-1066 (an N-oxide metabolite); although both metabolites have a nanomolar affinity for the μ-, κ-, and δ-opioid receptors, neither is thought to contribute to the pharmacological effects of samidorphan.11,12
- Route of elimination
Samidorphan is primarily renally excreted, with 67% of unchanged parent and metabolites eliminated in urine and another 16% in feces.11
- Half-life
- Clearance
- Adverse Effects
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- Toxicity
There is limited information regarding samidorphan overdose. During clinical trials for the combination of olanzapine and samidorphan, overdose was recognized in 7/861 patients, none of which were fatal. One patient who ingested 5.5- and 11-times the maximum daily dosage of olanzapine and samidorphan, respectively, was unresponsive and admitted to the hospital but stabilized within two days. As there are no known antidotes for overdose with this combination, symptomatic and supportive measures are recommended.11
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when 1,2-Benzodiazepine is combined with Samidorphan. Abametapir The serum concentration of Samidorphan can be increased when it is combined with Abametapir. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Samidorphan. Acetophenazine The risk or severity of CNS depression can be increased when Acetophenazine is combined with Samidorphan. Agomelatine The risk or severity of CNS depression can be increased when Agomelatine is combined with Samidorphan. - Food Interactions
- Take with or without food. Food has only a minor effect on samidorphan pharmacokinetics.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Samidorphan L-malate 0AJQ5N56E0 1204592-75-5 RARHXUAUPNYAJF-QSYGGRRVSA-N - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Lybalvi Samidorphan L-malate (10 mg/1) + Olanzapine (15 mg/1) Tablet, film coated Oral Alkermes, Inc. 2021-09-20 Not applicable US Lybalvi Samidorphan L-malate (10 mg/1) + Olanzapine (10 mg/1) Tablet, film coated Oral Alkermes, Inc. 2021-09-20 Not applicable US Lybalvi Samidorphan L-malate (10 mg/1) + Olanzapine (20 mg/1) Tablet, film coated Oral Alkermes, Inc. 2021-09-20 Not applicable US Lybalvi Samidorphan L-malate (10 mg/1) + Olanzapine (5 mg/1) Tablet, film coated Oral Alkermes, Inc. 2021-09-20 Not applicable US
Categories
- ATC Codes
- N05AH53 — Olanzapine and samidorphan
- Drug Categories
- Alkaloids
- Antipsychotic Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Diazepines, Oxazepines, Thiazepines and Oxepines
- Heterocyclic Compounds, Fused-Ring
- Morphinans
- Nervous System
- Opiate Alkaloids
- Opioid Antagonists
- Peripheral Nervous System Agents
- Phenanthrenes
- Psycholeptics
- Sensory System Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenanthrenes and derivatives
- Sub Class
- Not Available
- Direct Parent
- Phenanthrenes and derivatives
- Alternative Parents
- Naphthalenecarboxamides / Benzazocines / Isoquinolones and derivatives / Tetralins / Salicylic acid and derivatives / 1-hydroxy-4-unsubstituted benzenoids / Aralkylamines / Piperidines / Vinylogous acids / Tertiary alcohols show 10 more
- Substituents
- 1,2-aminoalcohol / 1-hydroxy-4-unsubstituted benzenoid / 2-naphthalenecarboxamide / 2-naphthalenecarboxylic acid or derivatives / Alcohol / Amine / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle show 25 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 7W2581Z5L8
- CAS number
- 852626-89-2
- InChI Key
- RYIDHLJADOKWFM-MAODMQOUSA-N
- InChI
- InChI=1S/C21H26N2O4/c22-19(26)15-4-3-13-9-16-21(27)6-5-14(24)10-20(21,17(13)18(15)25)7-8-23(16)11-12-1-2-12/h3-4,12,16,25,27H,1-2,5-11H2,(H2,22,26)/t16-,20-,21-/m1/s1
- IUPAC Name
- (1R,9R,10S)-17-(cyclopropylmethyl)-3,10-dihydroxy-13-oxo-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2,4,6-triene-4-carboxamide
- SMILES
- NC(=O)C1=CC=C2C[C@H]3N(CC4CC4)CC[C@@]4(CC(=O)CC[C@@]34O)C2=C1O
References
- Synthesis Reference
Wentland MP, Lu Q, Lou R, Bu Y, Knapp BI, Bidlack JM: Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2107-10. doi: 10.1016/j.bmcl.2005.02.032.
- General References
- Chaudhary AMD, Khan MF, Dhillon SS, Naveed S: A Review of Samidorphan: A Novel Opioid Antagonist. Cureus. 2019 Jul 15;11(7):e5139. doi: 10.7759/cureus.5139. [Article]
- Bidlack JM, Knapp BI, Deaver DR, Plotnikava M, Arnelle D, Wonsey AM, Fern Toh M, Pin SS, Namchuk MN: In Vitro Pharmacological Characterization of Buprenorphine, Samidorphan, and Combinations Being Developed as an Adjunctive Treatment of Major Depressive Disorder. J Pharmacol Exp Ther. 2018 Nov;367(2):267-281. doi: 10.1124/jpet.118.249839. Epub 2018 Aug 14. [Article]
- Wentland MP, Lu Q, Lou R, Bu Y, Knapp BI, Bidlack JM: Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2107-10. doi: 10.1016/j.bmcl.2005.02.032. [Article]
- Wentland MP, Lou R, Lu Q, Bu Y, Denhardt C, Jin J, Ganorkar R, VanAlstine MA, Guo C, Cohen DJ, Bidlack JM: Syntheses of novel high affinity ligands for opioid receptors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. doi: 10.1016/j.bmcl.2009.02.078. Epub 2009 Feb 25. [Article]
- Cunningham JI, Eyerman DJ, Todtenkopf MS, Dean RL, Deaver DR, Sanchez C, Namchuk M: Samidorphan mitigates olanzapine-induced weight gain and metabolic dysfunction in rats and non-human primates. J Psychopharmacol. 2019 Oct;33(10):1303-1316. doi: 10.1177/0269881119856850. Epub 2019 Jul 11. [Article]
- Martin WF, Correll CU, Weiden PJ, Jiang Y, Pathak S, DiPetrillo L, Silverman BL, Ehrich EW: Mitigation of Olanzapine-Induced Weight Gain With Samidorphan, an Opioid Antagonist: A Randomized Double-Blind Phase 2 Study in Patients With Schizophrenia. Am J Psychiatry. 2019 Jun 1;176(6):457-467. doi: 10.1176/appi.ajp.2018.18030280. Epub 2019 Mar 8. [Article]
- Pathak S, Vince B, Kelsh D, Setnik B, Nangia N, DiPetrillo L, Puhl MD, Sun L, Stanford AD, Ehrich E: Abuse Potential of Samidorphan: A Phase I, Oxycodone-, Pentazocine-, Naltrexone-, and Placebo-Controlled Study. J Clin Pharmacol. 2019 Feb;59(2):218-228. doi: 10.1002/jcph.1343. Epub 2018 Nov 26. [Article]
- Sun L, McDonnell D, von Moltke L: Pharmacokinetics and Short-term Safety of ALKS 3831, a Fixed-dose Combination of Olanzapine and Samidorphan, in Adult Subjects with Schizophrenia. Clin Ther. 2018 Nov;40(11):1845-1854.e2. doi: 10.1016/j.clinthera.2018.09.002. Epub 2018 Oct 20. [Article]
- Kumar V, Lu H, Hard M, von Moltke L: Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age. Drugs R D. 2019 Sep;19(3):277-287. doi: 10.1007/s40268-019-00280-5. [Article]
- Sun L, McDonnell D, Liu J, von Moltke L: Effect of Food on the Pharmacokinetics of a Combination of Olanzapine and Samidorphan. Clin Pharmacol Drug Dev. 2019 May;8(4):503-510. doi: 10.1002/cpdd.688. Epub 2019 Mar 28. [Article]
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- DEA Proposal: Removal of Samidorphan from Controlled Substance Schedule [Link]
- DEA: Removal of Samidorphan from Schedule II [Link]
- External Links
- PubChem Compound
- 11667832
- PubChem Substance
- 347828769
- ChemSpider
- 23259667
- BindingDB
- 50165049
- 2559612
- ChEMBL
- CHEMBL426084
- ZINC
- ZINC000028478244
- Wikipedia
- Samidorphan
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Recruiting Treatment Bipolar 1 Disorder / Schizophrenia 1 2 Completed Treatment Alcohol Dependency 1 2 Completed Treatment Alcohol Use Disorders (AUD) / Schizophrenia 1 2 Completed Treatment Binge Eating Disorder (BED) 1 2 Completed Treatment Schizophrenia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8778960 No 2014-07-15 2032-02-13 US US9126977 No 2015-09-08 2031-08-23 US US9517235 No 2016-12-13 2031-08-23 US US10716785 No 2020-07-21 2031-08-23 US US10300054 No 2019-05-28 2031-08-23 US US9119848 No 2015-09-01 2031-08-30 US US7956187 No 2011-06-07 2021-10-31 US US8252929 No 2012-08-28 2021-10-31 US US7262298 No 2007-08-28 2025-11-23 US US11185541 No 2021-11-30 2031-08-23 US US11241425 No 2011-08-23 2031-08-23 US US11351166 No 2011-08-23 2031-08-23 US US11707466 No 2021-11-12 2041-11-12 US US11793805 No 2011-08-23 2031-08-23 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 196.6-196.8 DEA water solubility freely soluble DEA pKa 8.3, 10.1 FDA Label - Predicted Properties
Property Value Source Water Solubility 0.629 mg/mL ALOGPS logP 1.09 ALOGPS logP 0.29 Chemaxon logS -2.8 ALOGPS pKa (Strongest Acidic) 7.92 Chemaxon pKa (Strongest Basic) 9.46 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 103.86 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 101.04 m3·mol-1 Chemaxon Polarizability 39.39 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-6bdc701626646b9d958f Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0uk9-0009000000-48bf7e94ae8bfedf3742 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0udr-0009000000-fbc3333cd2450f8aae0a Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-00or-1009000000-1500b2dd2eb97cc0c092 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0ab9-1429000000-4e5554594a235516f5eb Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-00ko-3049000000-fce3e5668c9ce64f4667 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 193.02089 predictedDeepCCS 1.0 (2019) [M+H]+ 195.41644 predictedDeepCCS 1.0 (2019) [M+Na]+ 201.3622 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- Curator comments
- Samidorphan binds the μ-opioid receptor with a Ki of 0.052 ± 0.0044 nM.
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- Curator comments
- Samidorphan binds the κ-opioid receptor with a Ki of 0.23 ± 0.018 nM.
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- Curator comments
- Samidorphan binds the δ-opioid receptor with a Ki of 2.7 ± 0.36 nM.
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
Drug created at October 20, 2016 22:47 / Updated at June 09, 2021 08:40