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This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C23H24N4O3
Molecular Weight 404.4617
Optical Activity ( - )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Ozanimod

SMILES

CC(C)OC1=CC=C(C=C1C#N)C2=NC(=NO2)C3=C4CC[C@H](NCCO)C4=CC=C3

InChI

InChIKey=XRVDGNKRPOAQTN-FQEVSTJZSA-N
InChI=1S/C23H24N4O3/c1-14(2)29-21-9-6-15(12-16(21)13-24)23-26-22(27-30-23)19-5-3-4-18-17(19)7-8-20(18)25-10-11-28/h3-6,9,12,14,20,25,28H,7-8,10-11H2,1-2H3/t20-/m0/s1

HIDE SMILES / InChI
Molecular Formula C23H24N4O3
Molecular Weight 404.4617
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Ozanimod (previously known as RPC-1063) is a selective immune-inflammatory modulator of the G protein-coupled receptors sphingosine 1-phosphate 1 and 5, which are part of the sphingosine 1-phosphate (S1P) receptor family. Treatment with S1P receptor modulators interferes with S1P signaling and blocks the response of lymphocytes (a type of white blood cell) to exit signals from the lymph nodes, sequestering them within the nodes. The result is a downward modulation of circulating lymphocytes and anti-inflammatory activity by inhibiting cell migration to sites of inflammation. Ozanimod is currently in phase III clinical trials for the treatment of relapsing multiple sclerosis (RMS) and ulcerative colitis, and also in phase II clinical trials to determine whether it is effective in the treatment of Crohn's disease.

CNS Activity

CNS Penetrant
2588
Curator's Comment: effectively crossing the blood–brain barrier resulting in exposure in the brain

Originator

Approval Year

2020
691
Targets

Targets

Primary TargetPharmacologyConditionPotency
Sphingosine 1-phosphate receptor 1
7
Target ID: P21453
Gene ID: 1901.0
Gene Symbol: S1PR1
Target Organism: Homo sapiens (Human)
Agonist
2752
 0.41 nM [EC50]
Sphingosine 1-phosphate receptor 5
5
Target ID: Q9H228
Gene ID: 53637.0
Gene Symbol: S1PR5
Target Organism: Homo sapiens (Human)
Agonist
2752
 11.0 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase III
665
Unknown

Approved Use

Unknown
Primary
Phase III
665
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.409 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28398597
1.5 mg 1 times / day steady-state, oral
dose: 1.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OZANIMOD plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
7.66 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28398597
1.5 mg 1 times / day steady-state, oral
dose: 1.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OZANIMOD plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
21.4 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28398597
1.5 mg 1 times / day steady-state, oral
dose: 1.5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OZANIMOD plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Other AEs: Nasopharyngitis, Headache...
Other AEs:
Nasopharyngitis (9.7%)
Headache (6%)
Upper respiratory tract infection (6.8%)
Alanine aminotransferase increased (2.6%)
Back pain (2.2%)
Gamma-glutamyltransferase increased (2.2%)
Respiratory tract infection viral (2.2%)
Urinary tract infection (1.8%)
Hypercholesterolaemia (1.3%)
Hypertension (2.4%)
Pharyngitis (1.3%)
Rhinitis (1.8%)
Upper abdominal pain (2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Other AEs: Nasopharyngitis, Headache...
Other AEs:
Nasopharyngitis (6.7%)
Headache (7.6%)
Upper respiratory tract infection (4%)
Alanine aminotransferase increased (4.7%)
Back pain (3.8%)
Gamma-glutamyltransferase increased (3.3%)
Respiratory tract infection viral (3.3%)
Urinary tract infection (3.8%)
Hypercholesterolaemia (2.5%)
Hypertension (1.3%)
Pharyngitis (2.5%)
Rhinitis (2%)
Upper abdominal pain (1.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Other AEs: Upper respiratory infection, Transaminases increased...
Other AEs:
Upper respiratory infection (26%)
Transaminases increased (10%)
Orthostatic hypotension (4%)
Urinary tract infection (4%)
Back pain (4%)
Hypertension (4%)
Abdominal pain upper (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
0.92 mg 1 times / day multiple, oral
Recommended
Dose: 0.92 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.92 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Disc. AE: Hepatic enzymes increased...
AEs leading to
discontinuation/dose reduction:
Hepatic enzymes increased (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Hypercholesterolaemia 1.3%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Pharyngitis 1.3%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Rhinitis 1.8%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Urinary tract infection 1.8%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Upper abdominal pain 2%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Back pain 2.2%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Gamma-glutamyltransferase increased 2.2%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Respiratory tract infection viral 2.2%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Hypertension 2.4%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Alanine aminotransferase increased 2.6%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Headache 6%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Upper respiratory tract infection 6.8%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Nasopharyngitis 9.7%
0.5 mg 1 times / day multiple, oral
Recommended
Dose: 0.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Hypertension 1.3%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Upper abdominal pain 1.3%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Rhinitis 2%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Hypercholesterolaemia 2.5%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Pharyngitis 2.5%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Gamma-glutamyltransferase increased 3.3%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Respiratory tract infection viral 3.3%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Back pain 3.8%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Urinary tract infection 3.8%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Upper respiratory tract infection 4%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Alanine aminotransferase increased 4.7%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Nasopharyngitis 6.7%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Headache 7.6%
1 mg 1 times / day multiple, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
unhealthy, 18 - 55 years
Health Status: unhealthy
Age Group: 18 - 55 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31492651/
Transaminases increased 10%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Abdominal pain upper 2%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Upper respiratory infection 26%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Back pain 4%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Hypertension 4%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Orthostatic hypotension 4%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Urinary tract infection 4%
0.84 mg 1 times / day multiple, oral
Recommended
Dose: 0.84 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.84 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Hepatic enzymes increased 1%
Disc. AE
0.92 mg 1 times / day multiple, oral
Recommended
Dose: 0.92 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.92 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
unhealthy, mean age 35.4 years
Health Status: unhealthy
Age Group: mean age 35.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209899s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946
inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2B6
926

CYP2C19
2057

CYP2C8
1057

CYP3A
227

P-gp
1741

OATP1B1
1079

OATP1B3
961

OAT1
725

OAT3
747

MATE2
267

BCRP
910
alcohol dehydrogenase
7

ALDH
6

AKR1C1
22

AKR1C2
12

11-beta-HSD
3

3-beta-HSD
3

CYP1A1
389

P-gp
2052

BCRP
697

CYP2C8
810
CYP1A2
832

CYP2B6
669

CYP3A
142
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no
CYP1A2
2333
 no
CC1084037
2
CYP1A2
2333
 no
CC112273
2
CYP1A2
2333
 no
CYP1A2
2333
 no
CC1084037
2
CYP1A2
2333
 no
CC112273
2
CYP2B6
1160
 no
CYP2B6
1160
 no
CC1084037
2
CYP2B6
1160
 no
CC112273
2
CYP2B6
1160
 no
CYP2B6
1160
 no
CC1084037
2
CYP2B6
1160
 no
CC112273
2
CYP2C19
2141
 no
CYP2C19
2141
 no
CC1084037
2
CYP2C19
2141
 no
CC112273
2
CYP2C8
1117
 no
CYP2C8
1117
 no
CC1084037
2
CYP2C8
1117
 no
CC112273
2
CYP2C9
2497
 no
CYP2C9
2497
 no
CC1084037
2
CYP2C9
2497
 no
CC112273
2
CYP2D6
2546
 no
CYP2D6
2546
 no
CC1084037
2
CYP2D6
2546
 no
CC112273
2
CYP3A
317
 no
CYP3A
317
 no
CC1084037
2
CYP3A
317
 no
CC112273
2
CYP3A
317
 no
CYP3A
317
 no
CC1084037
2
CYP3A
317
 no
CC112273
2
MATE2
267
 no
MATE2
267
 no
CC1084037
2
MATE2
267
 no
CC112273
2
OAT1
730
 no
OAT1
730
 no
CC1084037
2
OAT1
730
 no
CC112273
2
OAT3
749
 no
OAT3
749
 no
CC1084037
2
OAT3
749
 no
CC112273
2
OATP1B1
1095
 no
OATP1B1
1095
 no
CC1084037
2
OATP1B1
1095
 no
CC112273
2
OATP1B3
970
 no
OATP1B3
970
 no
CC1084037
2
OATP1B3
970
 no
CC112273
2
P-gp
1932
 no
P-gp
1932
 no
CC1084037
2
P-gp
1932
 no
CC112273
2
BCRP
985
 yes [IC50 22.8 uM]
CC112273
2
unlikely
Comment: At clinically relevant concentrations of CC112273 and CC1084037, inhibition of BCRP is not expected
Page: 17.0
BCRP
985
 yes [IC50 25.2 uM]
CC1084037
2
unlikely
Comment: At clinically relevant concentrations of CC112273 and CC1084037, inhibition of BCRP is not expected
Page: 17.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
2052
 likely
ALDH
6
 major
alcohol dehydrogenase
7
 major
BCRP
697
 no
CC1084037
2
BCRP
697
 no
CC112273
2
P-gp
2052
 no
CC1084037
2
P-gp
2052
 no
CC112273
2
11-beta-HSD
3
 yes
CC1084037
2
3-beta-HSD
3
 yes
CC1084037
2
AKR1C1
22
 yes
CC1084037
2
AKR1C2
12
 yes
CC1084037
2
BCRP
697
 yes
RP101988
2
CYP1A1
389
 yes
P-gp
2052
 yes
RP101988
2
CYP2C8
810
 yes
CC112273
2
yes (co-administration study)
Comment: Co-administration of gemfibrozil (a strong inhibitor of CYP2C8) 600 mg twice daily at steady state and a single dose of ozanimod 0.46 mg resulted in no clinically meaningful changes in exposure (AUC) of ozanimod and increased exposure (AUC) of active metabolites CC112273 and CC1084037 by approximately 47% and 69%, respectively
Page: 31.0
CYP3A4
1946
 yes
yes (co-administration study)
Comment: Coadministration of itraconazole (a strong inhibitor of CYP3A4) twice daily at steady state and a single dose of ozanimod 0.46 mg had no significant effect on ozanimod Cmax and AUCinf. Itraconazole decreased the Cmax of the major metabolites CC112273 and approximately 21% and 22%, respectivelyCC1084037 by
Page: 11.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
hERG
2263
CC112273
2
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA000UPT
https://www.aablocks.com/goods/Goods/detail?id=AA000UPT
Aaron Chemicals
AR000VHL
http://www.aaronchem.com/1306760-87-1
abcr GmbH
AB459325
http://www.abcr.com/shop/en/AB459325
AbMole Bioscience
M5244
http://www.abmole.com/products/ozanimod.html
Achemtek
0102-032368
http://www.achemtek.com/1306760-87-1-3
Acorn PharmaTech
ACN-037518
http://www.acornpharmatech.com/
Adooq BioScience
A15819
https://www.adooq.com/rpc1063.html
BioChemPartner
BCP16513
http://www.biochempartner.com/1306760-87-1-BCP16513
BioCrick
BCC6533
http://www.biocrick.com/Ozanimod-RPC1063-BCC6533.html
Chem Scene
CS-5070
http://www.chemscene.com/1306760-87-1.html
Chemspace
CSSB00025715463
https://chem-space.com/CSSB00025715463
DC Chemicals
DC8281
http://www.dcchemicals.com/product_show-Ozanimod_RPC1063_.html
eNovation Chemicals
D567265
https://www.enovationchem.com/ProductDetails.asp?ProductID=D567265
eNovation Chemicals
D580258
https://www.enovationchem.com/ProductDetails.asp?ProductID=D580258
eNovation Chemicals
Y0975701
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0975701
eNovation Chemicals
Y1040763
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1040763
Excenen
EX-A1316
http://www.excenen.com/searchresultlist.php?id=1306760-87-1
iChemical
EBD3724513
http://www.ichemical.com/products/1306760-87-1.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network
LN01344430
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01344430
MedChem Express
HY-12288
https://www.medchemexpress.com/Ozanimod.html
Smolecule
S538448
http://www.smolecule.com/products/s538448
Synblock Inc
SB16927
http://www.synblock.com/product/1306760-87-1.html
THE BioTek
bt-278101
https://www.thebiotek.com/product/inhibitors/bt-278101
PubMed

PubMed

TitleDatePubMed
Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.
2016 Jun
Ozanimod Induction and Maintenance Treatment for Ulcerative Colitis.
2016 May 5
Patents

Patents

20110172202
2

Sample Use Guides

In Vivo Use Guide
Multiple Sclerosis: 1 mg RPC1063 (Ozanimod) oral capsule daily
Route of Administration: Oral
In Vitro Use Guide
Ozanimod (RPC1063) is a specific agonist for sphingosine-1-phosphate receptor subtypes 1 (S1P1) and S1P5 receptors. The EC50 values were 0.16 nM and 0.41 nM for S1P1 receptors in the inhibition of cAMP generation and [35S]-GTPγS binding. The 83% Emax value of ozanimod against S1P5 receptor was 11 nM. RPC1063 demonstrated a dose‐dependent effect on S1P1 receptor re‐expression on the cell surface, with near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM in S1P1 receptor-HEK293T cells after 1 h incubation.
Substance Class Chemical
Created
by admin
on Mon Mar 31 19:01:23 GMT 2025
Edited
by admin
on Mon Mar 31 19:01:23 GMT 2025
Record UNII
Z80293URPV
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
Ozanimod
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
Ozanimod [INN]
Preferred Name English
RPC-1063
Code English
Benzonitrile, 5-[3-[(1S)-2,3-dihydro-1-[(2-hydroxyethyl)amino]-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)-
Systematic Name English
Ozanimod [USAN]
Common Name English
Ozanimod [WHO-DD]
Common Name English
RPC1063
Code English
Ozanimod [MI]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 499515
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
WHO-ATC L04AA38
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
FDA ORPHAN DRUG 611517
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
Code System Code Type Description
DRUG CENTRAL
5383
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
MERCK INDEX
m12197
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
DRUG BANK
DB12612
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
NCI_THESAURUS
C170279
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
LACTMED
Ozanimod
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
DAILYMED
Z80293URPV
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
SMS_ID
100000167014
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
WIKIPEDIA
Ozanimod
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
FDA UNII
Z80293URPV
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
PUBCHEM
52938427
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
USAN
CD-21
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
INN
10057
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
EVMPD
SUB181335
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
EPA CompTox
DTXSID501026488
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
CAS
1306760-87-1
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
RXCUI
2288236
Created by admin on Mon Mar 31 19:01:23 GMT 2025 , Edited by admin on Mon Mar 31 19:01:23 GMT 2025
PRIMARY
Related Record Type Details
SPHINGOSINE 1-PHOSPHATE RECEPTOR 1
TARGET -> AGONIST
SELECTIVE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Structure of Ozanimod
EXCRETED UNCHANGED
Ozanimod was not present in feces. Ozanimod concentration in urine was negligible.
FECAL; URINE
Structure of Ozanimod hydrochloride
SALT/SOLVATE -> PARENT
AMINE OXIDASE (FLAVIN-CONTAINING) B
METABOLIC ENZYME -> SUBSTRATE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
ARYLAMINE N-ACETYLTRANSFERASE 2
METABOLIC ENZYME -> SUBSTRATE
SPHINGOSINE 1-PHOSPHATE RECEPTOR 5
TARGET -> AGONIST
SELECTIVE
Structure of Ozanimod hydrochloride
SALT/SOLVATE -> PARENT
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of RP-101075
METABOLITE ACTIVE -> PARENT
PLASMA
Structure of RP-112273
METABOLITE ACTIVE -> PARENT
MAJOR
PLASMA
Structure of RP-112374
METABOLITE -> PARENT
FECAL
Structure of PR-101442
METABOLITE ACTIVE -> PARENT
PLASMA
Structure of (2S,3S,4S,5R,6S)-6-(3-CYANO-4-HYDROXY-BENZOYL)OXY-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
METABOLITE INACTIVE -> PARENT
URINE
Structure of RP-112533
METABOLITE INACTIVE -> PARENT
MAJOR
FECAL
Structure of PR-101988
METABOLITE ACTIVE -> PARENT
PLASMA; URINE
Structure of RP-101124
METABOLITE INACTIVE -> PARENT
FECAL; PLASMA; URINE
Structure of RP-112480
METABOLITE INACTIVE -> PARENT
MAJOR
FECAL
Structure of RP-100798
METABOLITE ACTIVE -> PARENT
PLASMA
Structure of RP-112479
METABOLITE -> PARENT
FECAL
Structure of RP-112402
METABOLITE INACTIVE -> PARENT
MAJOR
URINE
Related Record Type Details
Structure of Ozanimod
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC AT STEADY-STATE

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