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
Thumb
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

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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

TargetActionsOrganism
AMu-type opioid receptor
antagonist
Humans
UKappa-type opioid receptor
partial agonist
Humans
UDelta-type opioid receptor
partial agonist
Humans
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

Samidorphan has a mean half-life of 7-11 hours.8,9,10,11

Clearance

Samidorphan has a mean clearance of 35-45 L/h.9,11

Adverse Effects
Adverseeffects
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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
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AbametapirThe serum concentration of Samidorphan can be increased when it is combined with Abametapir.
AbirateroneThe metabolism of Samidorphan can be decreased when combined with Abiraterone.
AlfentanilThe therapeutic efficacy of Alfentanil can be decreased when used in combination with Samidorphan.
AmiodaroneThe metabolism of Samidorphan can be decreased when combined with Amiodarone.
AmprenavirThe metabolism of Samidorphan can be decreased when combined with Amprenavir.
ApalutamideThe metabolism of Samidorphan can be increased when combined with Apalutamide.
AprepitantThe metabolism of Samidorphan can be decreased when combined with Aprepitant.
AtazanavirThe metabolism of Samidorphan can be decreased when combined with Atazanavir.
BenzhydrocodoneThe therapeutic efficacy of Benzhydrocodone can be decreased when used in combination with Samidorphan.
BerotralstatThe metabolism of Samidorphan can be decreased when combined with Berotralstat.
Interactions
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Food Interactions
  • Take with or without food. Food has only a minor effect on samidorphan pharmacokinetics.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Samidorphan L-malate0AJQ5N56E01204592-75-5RARHXUAUPNYAJF-QSYGGRRVSA-N
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
LybalviSamidorphan L-malate (10 mg/1) + Olanzapine (10 mg/1)Tablet, film coatedOralAlkermes, Inc.2021-09-20Not applicableUS flag
LybalviSamidorphan L-malate (10 mg/1) + Olanzapine (20 mg/1)Tablet, film coatedOralAlkermes, Inc.2021-09-20Not applicableUS flag
LybalviSamidorphan L-malate (10 mg/1) + Olanzapine (5 mg/1)Tablet, film coatedOralAlkermes, Inc.2021-09-20Not applicableUS flag
LybalviSamidorphan L-malate (10 mg/1) + Olanzapine (15 mg/1)Tablet, film coatedOralAlkermes, Inc.2021-09-20Not applicableUS flag

Categories

Drug Categories
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. 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]
  8. 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]
  9. 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]
  10. 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]
  11. FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]
  12. DEA Proposal: Removal of Samidorphan from Controlled Substance Schedule [Link]
  13. DEA: Removal of Samidorphan from Schedule II [Link]
PubChem Compound
11667832
PubChem Substance
347828769
ChemSpider
23259667
BindingDB
50165049
RxNav
2559612
ChEMBL
CHEMBL426084
ZINC
ZINC000028478244
Wikipedia
Samidorphan

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAlcohol Dependency1
2CompletedTreatmentAlcohol Use Disorders (AUD) / Schizophrenia1
2CompletedTreatmentBinge Eating Disorder (BED)1
2CompletedTreatmentSchizophrenia1
1CompletedNot AvailableCocaine Abuse1
1CompletedTreatmentAlcohol Dependency1
1CompletedTreatmentHealthy Subjects (HS)2
1CompletedTreatmentSubstance Related Disorders1
1, 2CompletedNot AvailableMajor Depressive Disorder (MDD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8778960No2014-07-152032-02-13US flag
US9126977No2015-09-082031-08-23US flag
US9517235No2016-12-132031-08-23US flag
US10716785No2020-07-212031-08-23US flag
US10300054No2019-05-282031-08-23US flag
US9119848No2015-09-012031-08-30US flag
US7956187No2011-06-072021-10-31US flag
US8252929No2012-08-282021-10-31US flag
US7262298No2007-08-282025-11-23US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)196.6-196.8DEA
water solubilityfreely solubleDEA
pKa8.3, 10.1FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.629 mg/mLALOGPS
logP1.09ALOGPS
logP0.29ChemAxon
logS-2.8ALOGPS
pKa (Strongest Acidic)7.92ChemAxon
pKa (Strongest Basic)9.46ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area103.86 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity101.04 m3·mol-1ChemAxon
Polarizability39.39 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets2
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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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. FDA Approved Drug Products: LYBALVI (olanzapine and samidorphan) tablets [Link]

Drug created on October 20, 2016 22:47 / Updated on June 09, 2021 08:40