ozanimod 🐶 Veterinary Use | 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 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 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 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 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
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:

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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