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ozanimod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
immunomodulators, both stimulant/suppressive and stimulant	5383	1306760-87-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ozanimod RPC1063 RPC-1063 ozanimod hydrochloride	Ozanimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1 and 5. Ozanimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which ozanimod exerts therapeutic effects in multiple sclerosis is unknown but may involve the reduction of lymphocyte migration into the central nervous system Molecular weight: 404.47 Formula: C23H24N4O3 CLOGP: 3.44 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 104.20 ALOGS: -3.40 ROTB: 7 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ozanimod
RPC1063
RPC-1063
ozanimod hydrochloride

Ozanimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1 and 5. Ozanimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which ozanimod exerts therapeutic effects in multiple sclerosis is unknown but may involve the reduction of lymphocyte migration into the central nervous system

Molecular weight: 404.47
Formula: C23H24N4O3
CLOGP: 3.44
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 104.20
ALOGS: -3.40
ROTB: 7

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.92	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
March 25, 2020	FDA	CELGENE INTL
May 20, 2020	EMA	Bristol-Myers Squibb Pharma EEIG

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	508.81	35.80	170	4098	48308	63436446
Fatigue	139.26	35.80	227	4041	887801	62596953
Headache	131.80	35.80	185	4083	633056	62851698
Dizziness	89.54	35.80	126	4142	429799	63054955
Lymphopenia	80.16	35.80	34	4234	18293	63466461
Lymphocyte count decreased	66.75	35.80	35	4233	30222	63454532
COVID-19	59.72	35.80	54	4214	113049	63371705
Balance disorder	51.96	35.80	44	4224	84378	63400376
Back pain	51.20	35.80	75	4193	264070	63220684
Migraine	48.08	35.80	46	4222	103300	63381454

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	174.49	45.82	48	1228	13085	34942570
Drug ineffective	80.60	45.82	90	1186	456661	34498994
Fatigue	53.23	45.82	66	1210	370587	34585068
COVID-19	46.34	45.82	31	1245	77519	34878136

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Multiple sclerosis relapse	476.45	37.95	153	4279	46380	79693576
Fatigue	173.41	37.95	233	4199	929494	78810462
Headache	148.38	37.95	181	4251	653591	79086365
Dizziness	92.79	37.95	129	4303	526312	79213644
Lymphopenia	88.24	37.95	40	4392	30517	79709439
Back pain	74.65	37.95	88	4344	304092	79435864
COVID-19	68.39	37.95	62	4370	157612	79582344
Migraine	55.75	37.95	43	4389	87450	79652506
Hypoaesthesia	54.37	37.95	58	4374	179294	79560662
Balance disorder	53.20	37.95	44	4388	98813	79641143

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AA38	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
FDA EPC	N0000181816	Sphingosine 1-phosphate Receptor Modulator
FDA MoA	N0000181815	Sphingosine 1-Phosphate Receptor Modulators
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents
MeSH PA	D000081243	Sphingosine 1 Phosphate Receptor Modulators

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Multiple sclerosis	indication	24700007	DOID:2377
Ulcerative colitis	indication	64766004	DOID:8577
Relapsing remitting multiple sclerosis	indication	426373005	DOID:2378
Preinfarction syndrome	contraindication	4557003
Myocardial infarction	contraindication	22298006	DOID:5844
Mobitz type II atrioventricular block	contraindication	28189009	DOID:11312
Sick sinus syndrome	contraindication	36083008	DOID:13884
Sinoatrial block	contraindication	65778007
Sleep apnea	contraindication	73430006	DOID:0050847
Heart failure	contraindication	84114007	DOID:6000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.46	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.23MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	8481573	May 14, 2029	TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
EQ 0.23MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	9382217	May 14, 2029	TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
EQ 0.23MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	10239846	Nov. 15, 2030	INDICATED FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS
EQ 0.46MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	8481573	May 14, 2029	TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
EQ 0.46MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	9382217	May 14, 2029	TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
EQ 0.46MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	10239846	Nov. 15, 2030	INDICATED FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS
EQ 0.92MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	8481573	May 14, 2029	TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
EQ 0.92MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	9382217	May 14, 2029	TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS
EQ 0.92MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	10239846	Nov. 15, 2030	INDICATED FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 0.23MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	May 27, 2024	FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS IN ADULT PATIENTS
EQ 0.23MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	March 25, 2025	NEW CHEMICAL ENTITY
EQ 0.46MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	May 27, 2024	FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS IN ADULT PATIENTS
EQ 0.46MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	March 25, 2025	NEW CHEMICAL ENTITY
EQ 0.92MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	May 27, 2024	FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS IN ADULT PATIENTS
EQ 0.92MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	March 25, 2025	NEW CHEMICAL ENTITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sphingosine 1-phosphate receptor 1	GPCR	P21453	S1PR1_HUMAN	AGONIST	EC50	9.39	SCIENTIFIC LITERATURE	DRUG LABEL
Sphingosine 1-phosphate receptor 5	GPCR	Q9H228	S1PR5_HUMAN	AGONIST	EC50	7.96	SCIENTIFIC LITERATURE	DRUG LABEL
Sphingosine 1-phosphate receptor 4	GPCR	O95977	S1PR4_HUMAN		EC50	5.38	CHEMBL
Sphingosine 1-phosphate receptor 3	GPCR	Q99500	S1PR3_HUMAN		EC50	5	CHEMBL
Sphingosine 1-phosphate receptor 2	GPCR	O95136	S1PR2_HUMAN		EC50	5.02	CHEMBL

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External reference:

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ID	Source
018313	NDDF
018314	NDDF
10057	INN_ID
1618636-37-5	SECONDARY_CAS_RN
2288235	RXNORM
38279	MMSL
4039423	VANDF
4039424	VANDF
52938427	PUBCHEM_CID
870525003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ZEPOSIA	HUMAN PRESCRIPTION DRUG LABEL	1	59572-820	CAPSULE	0.92 mg	ORAL	NDA	29 sections
ZEPOSIA	HUMAN PRESCRIPTION DRUG LABEL	1	59572-820	CAPSULE	0.92 mg	ORAL	NDA	29 sections
ZEPOSIA	HUMAN PRESCRIPTION DRUG LABEL	1	59572-820	CAPSULE	0.92 mg	ORAL	NDA	29 sections
ZEPOSIA	HUMAN PRESCRIPTION DRUG LABEL	1	59572-820	CAPSULE	0.92 mg	ORAL	NDA	29 sections

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