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
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
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 |
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 | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL233 |
0.052 nM [Ki] | ||
Target ID: CHEMBL237 |
0.23 nM [Ki] | ||
Target ID: CHEMBL236 |
2.7 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Lybalvi Approved UseSchizophrenia in adults Launch Date2021 |
|||
Primary | Lybalvi Approved UseBipolar I disorder in adults; Acute treatment of manic or mixed episodes as monotherapy and as adjunct to lithium or valproate; Maintenance monotherapy treatment Launch Date2021 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
45.1 ng/mL |
10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE |
SAMIDORPHAN plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
11.2 ng/mL |
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 |
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 |
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 |
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 |
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 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: 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 |
10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE |
SAMIDORPHAN plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
27.7 ng × h/mL |
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 |
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 |
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 |
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 |
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 |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: OLANZAPINE |
SAMIDORPHAN plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11 h |
10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: OLANZAPINE |
SAMIDORPHAN plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
67% |
10 mg 11 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: 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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Hypertension, Anxiety... AEs leading to discontinuation/dose reduction: Hypertension (1 pt) Sources: Anxiety (1 pt) Dizziness (1 pt) Irritability (1 pt) Malaise (1 pt) Suicidal ideation (2 pt) |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Schizophrenia, Liver function test abnormal... AEs leading to discontinuation/dose reduction: Schizophrenia (serious, 1%) Sources: Liver function test abnormal (1%) |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Somnolence, Neutrophil count decreased... AEs leading to discontinuation/dose reduction: Somnolence (2%) Sources: 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%) |
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: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Adverse event... AEs leading to discontinuation/dose reduction: Adverse event (0%) Sources: |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Viral gastroenteritis, Intentional overdose... Other AEs: Blood insulin increased... AEs leading to discontinuation/dose reduction: Viral gastroenteritis (1 pt) Other AEs:Intentional overdose (1 pt) Dizziness (1 pt) Blood glucose increased (1 pt) Suicide attempt (1 pt) Blood insulin increased (1 pt) Sources: |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Electrocardiogram change, Nausea... AEs leading to discontinuation/dose reduction: Electrocardiogram change (1 pt) Sources: Nausea (1 pt) Pleural effusion (1 pt) Dyslipidemia (1 pt) Dizziness (1 pt) Seizure (1 pt) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Anxiety | 1 pt Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Dizziness | 1 pt Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Hypertension | 1 pt Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Irritability | 1 pt Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Malaise | 1 pt Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Suicidal ideation | 2 pt Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Liver function test abnormal | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Schizophrenia | serious, 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Drug abuse | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Glycosylated hemoglobin increased | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Liver function test abnormal | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Neutrophil count decreased | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Schizophrenia | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Weight increased | 1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Somnolence | 2% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Blood creatine increased | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Blood creatine phosphokinase increased | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Fatigue | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Headache | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Mental status changes | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Pleural effusion | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Priapism | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Rash | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Rectal hemorrhage | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Vomiting | <1% Disc. AE |
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: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Adverse event | 0% Disc. AE |
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: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Blood insulin increased | 1 pt | 10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Blood glucose increased | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Dizziness | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Intentional overdose | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Suicide attempt | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Viral gastroenteritis | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Dizziness | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Dyslipidemia | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Electrocardiogram change | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Nausea | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Pleural effusion | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Seizure | 1 pt Disc. AE |
10 mg multiple, oral Recommended Dose: 10 mg Route: oral Route: multiple Dose: 10 mg Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
Page: 29.0 |
no | |||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Page: 29.0 |
no | (co-administration study) Page: 29.0 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 Page: 21 | 260 |
major | |||
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) Page: 21 | 260 | 272 | 274 |
|||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 Page: 21 | 260 |
minor | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/213378Orig1Orig2s000MultidisciplineR.pdf#page=21 Page: 21 | 260 |
minor | |||
no | ||||
Page: 29.0 |
no | |||
no | ||||
Page: 29.0 |
no |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
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
Sources: https://pubmed.ncbi.nlm.nih.gov/30108159
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
Edited
Mon Mar 31 20:59:32 GMT 2025
by
admin
on
Mon Mar 31 20:59:32 GMT 2025
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Record UNII |
7W2581Z5L8
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C681
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SAMIDORPHAN
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TARGET->PARTIAL AGONIST |
weak partial agonist
BINDING
Ki
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TARGET -> INHIBITOR |
could have very weak partial agonist activity
BINDING
Ki
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TARGET->PARTIAL AGONIST |
BINDING
Ki
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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