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

Stem definitionDrug idCAS RN
immunomodulators, both stimulant/suppressive and stimulant 5383 1306760-87-1

Description:

MoleculeDescription

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:

DoseUnitRoute
0.92 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 20, 2020 EMA Bristol-Myers Squibb Pharma EEIG
March 25, 2020 FDA CELGENE INTL

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple sclerosis relapse 177.69 40.63 71 2587 44782 53301626
Fatigue 130.30 40.63 169 2489 730337 52616071
Headache 87.02 40.63 119 2539 536702 52809706
Dizziness 66.91 40.63 87 2571 372172 52974236
COVID-19 61.44 40.63 32 2626 36856 53309552
COVID-19 pneumonia 52.89 40.63 18 2640 7185 53339223
Unevaluable event 50.09 40.63 31 2627 49467 53296941
Multiple sclerosis 43.61 40.63 23 2635 27130 53319278
Balance disorder 43.49 40.63 33 2625 73174 53273234

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
COVID-19 50.04 45.57 19 514 31996 32480997
Multiple sclerosis relapse 46.34 45.57 14 519 11767 32501226

Pharmacologic Action:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.46 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sphingosine 1-phosphate receptor 1 GPCR AGONIST EC50 9.39 SCIENTIFIC LITERATURE DRUG LABEL
Sphingosine 1-phosphate receptor 5 GPCR AGONIST EC50 7.96 SCIENTIFIC LITERATURE DRUG LABEL
Sphingosine 1-phosphate receptor 4 GPCR EC50 5.38 CHEMBL
Sphingosine 1-phosphate receptor 3 GPCR EC50 5 CHEMBL
Sphingosine 1-phosphate receptor 2 GPCR EC50 5.02 CHEMBL

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ZEPOSIA HUMAN PRESCRIPTION DRUG LABEL 1 59572-820 CAPSULE 0.92 mg ORAL NDA 29 sections