Samidorphan

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H26N2O4
Molecular Weight	370.4421
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC(=O)C1=CC=C2C[C@H]3N(CC4CC4)CC[C@@]5(CC(=O)CC[C@@]35O)C2=C1O

InChI

InChIKey=RYIDHLJADOKWFM-MAODMQOUSA-N

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

HIDE SMILES / InChI

Molecular Formula	C21H26N2O4
Molecular Weight	370.4421
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf |https://pubmed.ncbi.nlm.nih.gov/34304374 | https://pubmed.ncbi.nlm.nih.gov/35040357

Samidorphan, which was developed by Alkermes, is an opioid receptor antagonist that has been co-formulated with olanzapine into a single-dose oral tablet to mitigate the risk of weight gain while providing the therapeutic effect of olanzapine. In June 2021, the Food and Drug Administration (FDA) approved Lybalvi (olanzapine/samidorphan) for indications including treatment of adults with schizophrenia and/or bipolar I disorder (acute manic episodes or acute episodes with mixed features).

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Potency
Mu opioid receptor 231 Target ID: CHEMBL233 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf	Antagonist 2849	0.052 nM [Ki]
Kappa opioid receptor 115 Target ID: CHEMBL237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf	Partial Agonist 297	0.23 nM [Ki]
Delta opioid receptor 81 Target ID: CHEMBL236 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf	Partial Agonist 297	2.7 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 305 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf	Primary		Approved 8583	Lybalvi Approved Use Schizophrenia in adults Launch Date 2021
Bipolar I disorder 19 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf	Primary		Approved 8583	Lybalvi Approved Use Bipolar I disorder in adults; Acute treatment of manic or mixed episodes as monotherapy and as adjunct to lithium or valproate; Maintenance monotherapy treatment Launch Date 2021

C_max

Value	Dose	Co-administered	Analyte	Population
45.1 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=25	10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE	OLANZAPINE	SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
11.2 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
4.1 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	2 mg single, sublingual dose: 2 mg route of administration: Sublingual experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
4.1 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
27.8 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
13.3 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=306	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
16.291 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=275	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: OLANZAPINE	OLANZAPINE	SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
364 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=25	10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE	OLANZAPINE	SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
27.7 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
41.3 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	2 mg single, sublingual dose: 2 mg route of administration: Sublingual experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
39.9 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
246 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=307	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
113.1 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=306	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
627.907 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=275	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: OLANZAPINE	OLANZAPINE	SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
11 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=25	10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE	OLANZAPINE	SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
67% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=25	10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE	OLANZAPINE	SAMIDORPHAN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
20 mg 1 times / day multiple, oral Highest studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf	Disc. AE: Hypertension, Anxiety... AEs leading to discontinuation/dose reduction: Hypertension (1 pt) Anxiety (1 pt) Dizziness (1 pt) Irritability (1 pt) Malaise (1 pt) Suicidal ideation (2 pt) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf
10 mg 1 times / day multiple, oral Studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf	Disc. AE: Schizophrenia, Liver function test abnormal... AEs leading to discontinuation/dose reduction: Schizophrenia (serious, 1%) Liver function test abnormal (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf
10 mg 1 times / day multiple, oral Studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf	Disc. AE: Somnolence, Neutrophil count decreased... AEs leading to discontinuation/dose reduction: Somnolence (2%) Neutrophil count decreased (1%) Weight increased (1%) Glycosylated hemoglobin increased (1%) Schizophrenia (1%) Drug abuse (1%) Liver function test abnormal (1%) Fatigue (<1%) Mental status changes (<1%) Headache (<1%) Vomiting (<1%) Rash (<1%) Blood creatine phosphokinase increased (<1%) Rectal hemorrhage (<1%) Blood creatine increased (<1%) Pleural effusion (<1%) Priapism (<1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf
30 mg 1 times / day multiple, oral Studied dose Dose: 30 mg, 1 times / day Route: oral Route: multiple Dose: 30 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30476361/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30476361/	Disc. AE: Adverse event... AEs leading to discontinuation/dose reduction: Adverse event (0%) Sources: https://pubmed.ncbi.nlm.nih.gov/30476361/
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000OtherR.pdf#page=139	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000OtherR.pdf#page=139	Disc. AE: Viral gastroenteritis, Intentional overdose... Other AEs: Blood insulin increased... AEs leading to discontinuation/dose reduction: Viral gastroenteritis (1 pt) Intentional overdose (1 pt) Dizziness (1 pt) Blood glucose increased (1 pt) Suicide attempt (1 pt) Other AEs: Blood insulin increased (1 pt) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000OtherR.pdf#page=139
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000OtherR.pdf#page=139	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000OtherR.pdf#page=139	Disc. AE: Electrocardiogram change, Nausea... AEs leading to discontinuation/dose reduction: Electrocardiogram change (1 pt) Nausea (1 pt) Pleural effusion (1 pt) Dyslipidemia (1 pt) Dizziness (1 pt) Seizure (1 pt) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000OtherR.pdf#page=139

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 substrate 1946 inhibitor 2252	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 2057 CYP1A2 2153 OAT1 725 OATP1B3 961 P-gp 1741 CYP2B6 926 OCT2 779 CYP2C8 1057 CYP3A5 136 BCRP 910 OATP1B1 1079 OAT3 747	CYP2C8 810 CYP3A5 446 CYP2C19 1119 CYP1A2 1197 OATP1B1 503 OATP1B3 435 P-gp 2052	CYP1A2 832 CYP2B6 669 CYP3A5 92

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP3A5 201	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
CYP3A5 201	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no	(co-administration study) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 Page: 21 \| 260	major
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=272 Page: 21 \| 260 \| 272 \| 274	major	yes (co-administration study) Comment: Rifampicin decreased AUCinf by 73%, Itraconazole was shown to have only marginal increase (~16% increase in Cmax and ~45% increase in AUC) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=272 Page: 21 \| 260 \| 272 \| 274
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 Page: 21 \| 260	minor
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 Page: 21 \| 260	minor
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=274 Page: 274.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/213378s000lbl.pdf#page=29 Page: 29.0	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=336 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=19 Page: 336 \| 19
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=336\| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=19 Page: 336 \| 19		RDC-9986 2

PubMed

Title	Date	PubMed
Effects of the Opioid System Modulator, Samidorphan, on Measures of Alcohol Consumption and Patient-Reported Outcomes in Adults with Alcohol Dependence.	2018 Oct	30055046

Patents

Sample Use Guides

In Vivo Use Guide

Schizophrenia: the recommended dosage is 10 mg/10 mg, 15 mg/10 mg (contains 15 mg of olanzapine and 10 mg of samidorphan), or 20 mg/10 mg (contains 20 mg of olanzapine and 10 mg of samidorphan) once daily.

Route of Administration: Oral

In Vitro Use Guide

Using membranes from hMOR-, hKOR and hDOR- CHO cells, competition binding experiments showed that Samidorphan had the highest affinity for the MOR with a Ki value of 0.052 ± 0.0044 nM. [3H]SAM had the highest affinity for the MOR with Kd values of 0.046 ± 0.0027 nM and 0.044 ± 0.0051 nM in TrisHCl and GP buffers, respectively.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:59:32 GMT 2025` Edited by `admin` on `Mon Mar 31 20:59:32 GMT 2025`
Record UNII	7W2581Z5L8
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

Samidorphan [INN]

Preferred Name

English

Samidorphan

Official Name

English

ALKS-5461 COMPONENT SAMIDORPHAN

Code

English

Samidorphan [WHO-DD]

Common Name

English

ALKS-33

Code

English

Morphinan-3-carboxamide, 17-(cyclopropylmethyl)-4,14-dihydroxy-6-oxo-

Systematic Name

English

Samidorphan [USAN]

Common Name

English

RDC-0313

Code

English

17-(Cyclopropylmethyl)-4,14-dihydroxy-6-oxomorphinan-3-carboxamide

Systematic Name

English

RDC-0313-00

Code

English

ALKS 33

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C681