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:

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

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 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
Unevaluable event 40.57 35.80 31 4237 51355 63433399
Hypoaesthesia 40.34 35.80 53 4215 168340 63316414
COVID-19 pneumonia 38.81 35.80 19 4249 14190 63470564
Memory impairment 38.57 35.80 41 4227 104217 63380537
Product dose omission issue 36.23 35.80 60 4208 234253 63250501

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 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

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
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
Drug ineffective 51.10 37.95 153 4279 1080760 78659196
Product dose omission issue 45.37 37.95 62 4370 247475 79492481
Memory impairment 42.73 37.95 41 4391 111693 79628263
Heart rate decreased 41.41 37.95 33 4399 70283 79669673
Unevaluable event 39.11 37.95 29 4403 55556 79684400
Lymphocyte count decreased 38.59 37.95 27 4405 47262 79692694

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
FDA MoA N0000181815 Sphingosine 1-Phosphate Receptor Modulators
FDA EPC N0000181816 Sphingosine 1-phosphate Receptor Modulator

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

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

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
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