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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:

None

Approvals:

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

FDA Adverse Event Reporting System (Female)

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	220.33	35.60	86	2916	42878	50559244
Fatigue	134.89	35.60	185	2817	707416	49894706
Headache	96.69	35.60	133	2869	506402	50095720
COVID-19	83.55	35.60	45	2957	46617	50555505
Dizziness	73.51	35.60	96	2906	346273	50255849
Unevaluable event	47.16	35.60	31	2971	46035	50556087
COVID-19 pneumonia	47.12	35.60	18	2984	8377	50593745
Balance disorder	43.66	35.60	35	2967	70555	50531567
Lymphocyte count decreased	43.24	35.60	24	2978	26283	50575839
Back pain	40.40	35.60	57	2945	219973	50382149
Hypoaesthesia	37.83	35.60	42	2960	127215	50474907
Migraine	37.60	35.60	33	2969	75247	50526875
Heart rate decreased	35.98	35.60	24	2978	36473	50565649

FDA Adverse Event Reporting System (Male)

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	88.68	43.81	25	681	11394	29562427
COVID-19	57.14	43.81	24	682	35990	29537831

FDA Adverse Event Reporting System (Geriatric)

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
Fatigue	150.18	42.38	171	2605	748559	63747397
Multiple sclerosis relapse	109.25	42.38	47	2729	41088	64454868
Headache	103.88	42.38	120	2656	529347	63966609
COVID-19	85.84	42.38	46	2730	65094	64430862
Dizziness	70.16	42.38	89	2687	430074	64065882
Back pain	63.17	42.38	65	2711	250106	64245850
Unevaluable event	48.45	42.38	29	2747	50460	64445496
Balance disorder	46.01	42.38	34	2742	83892	64412064
Hypoaesthesia	44.09	42.38	41	2735	139067	64356889
Heart rate decreased	43.63	42.38	28	2748	55039	64440917

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L04AA38	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents
MeSH PA	D000081243	Sphingosine 1 Phosphate Receptor Modulators

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

Disease	Relation	SNOMED_ID	DOID
Multiple sclerosis	indication	24700007	DOID:2377
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
Cerebrovascular accident	contraindication	230690007
Transient ischemic attack	contraindication	266257000	DOID:224

🐶 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)

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 0.46MG 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 0.92MG 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 0.23MG 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	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	10239846	Nov. 15, 2030	INDICATED FOR THE TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS

Orange Book exclusivity data (new drug applications)

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 0.46MG 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 0.92MG 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 0.23MG 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	March 25, 2025	NEW CHEMICAL ENTITY
EQ 0.92MG BASE	ZEPOSIA	CELGENE INTL	N209899	March 25, 2020	RX	CAPSULE	ORAL	March 25, 2025	NEW CHEMICAL ENTITY

Bioactivity Summary:

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

External reference:

ID	Source
Z80293URPV	UNII
C4278675	UMLSCUI
CHEMBL3707247	ChEMBL_ID
52938427	PUBCHEM_CID
DB12612	DRUGBANK_ID
CHEMBL3707246	ChEMBL_ID
D10968	KEGG_DRUG
8709	IUPHAR_LIGAND_ID
2288235	RXNORM
38279	MMSL
d09534	MMSL
870525003	SNOMEDCT_US
871794001	SNOMEDCT_US
871800005	SNOMEDCT_US
4039423	VANDF
4039424	VANDF
JEU	PDB_CHEM_ID
018313	NDDF
018314	NDDF
C000607776	MESH_SUPPLEMENTAL_RECORD_UI
10057	INN_ID
1618636-37-5	SECONDARY_CAS_RN

Pharmaceutical products:

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