ozanimod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.479 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 9.376 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 12.764 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 3.597 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 1.950 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 6.960 % High 1
herg hERG pIC50 5.426 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.573 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.093 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 2.220 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK9,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MET,PDK1,PDK2,PDK4,PIK3CA,PRKDC 18
kinase-selectivity-class EIF2AK3,PDK4 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 27.416 High 1
mh-clint Mouse hepatocyte intrinsic clearance 7.998 High 1
mppb Mouse plasma protein binding (% unbound) 1.610 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 53.951 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 3.260 % High 1
rh-clint Rat hepatocyte intrinsic clearance 12.764 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 4.850 % High 1
rppb Rat plasma protein binding (% unbound) 1.700 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 64.863 uM High 1

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 1366.20 26.18 380 6527 51925 90569615
Fatigue 235.03 26.18 356 6551 1153667 89467873
Headache 149.43 26.18 248 6659 862498 89759042
Lymphopenia 140.24 26.18 56 6851 22825 90598715
Lymphocyte count decreased 132.75 26.18 61 6846 34989 90586551
Disturbance in attention 109.97 26.18 59 6848 47050 90574490
Dizziness 95.68 26.18 165 6742 589119 90032421
Back pain 62.34 26.18 97 6810 317078 90304462
COVID-19 61.67 26.18 70 6837 168773 90452767
Balance disorder 60.89 26.18 54 6853 97026 90524514
Stress 50.48 26.18 45 6862 81350 90540190
Product dose omission issue 50.18 26.18 84 6823 291603 90329937
Visual impairment 41.86 26.18 51 6856 132314 90489226
Adverse event 40.01 26.18 47 6860 117371 90504169
Heart rate decreased 38.06 26.18 32 6875 53473 90568067
Unevaluable event 35.35 26.18 31 6876 54817 90566723
COVID-19 pneumonia 32.16 26.18 19 6888 18158 90603382
Urinary incontinence 32.07 26.18 25 6882 37541 90583999
Blood pressure increased 31.50 26.18 55 6852 197162 90424378
Depression 31.26 26.18 70 6837 300531 90321009
White blood cell count decreased 29.85 26.18 49 6858 167060 90454480
Hypoaesthesia 29.19 26.18 70 6837 314140 90307400
Migraine 28.99 26.18 52 6855 190340 90431200
Vision blurred 27.80 26.18 38 6869 110255 90511285
Drug ineffective 27.21 26.18 189 6718 1384109 89237431
Neuralgia 26.97 26.18 21 6886 31479 90590061
Bladder disorder 26.54 26.18 14 6893 10758 90610782

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 344.48 37.37 91 2244 14173 42604827
Fatigue 101.36 37.37 121 2214 435520 42183480
Drug ineffective 91.53 37.37 139 2196 630058 41988942
Angiolymphoid hyperplasia with eosinophilia 61.76 37.37 10 2325 130 42618870

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 1495.92 31.18 400 7563 49840 110531496
Fatigue 315.66 31.18 409 7554 1215549 109365787
Headache 169.50 31.18 258 7705 882119 109699217
Disturbance in attention 144.22 31.18 76 7887 61919 110519417
Lymphopenia 128.08 31.18 61 7902 40109 110541227
Back pain 90.59 31.18 122 7841 370874 110210462
Dizziness 89.54 31.18 171 7792 698022 109883314
Drug ineffective 83.01 31.18 268 7695 1520272 109061064
Lymphocyte count decreased 74.08 31.18 48 7915 57195 110524141
Balance disorder 60.74 31.18 57 7906 116503 110464833
Product dose omission issue 59.72 31.18 93 7870 321689 110259647
Angiolymphoid hyperplasia with eosinophilia 58.94 31.18 10 7953 131 110581205
COVID-19 58.81 31.18 80 7883 244980 110336356
Adverse event 58.21 31.18 54 7909 108755 110472581
Stress 50.11 31.18 49 7914 105299 110476037
Urinary incontinence 49.17 31.18 35 7928 48552 110532784
Visual impairment 46.91 31.18 53 7910 134375 110446961
Heart rate decreased 46.06 31.18 42 7921 82714 110498622
Vision blurred 45.25 31.18 51 7912 128971 110452365
Hypoaesthesia 45.15 31.18 81 7882 314142 110267194
Depression 39.58 31.18 77 7886 317258 110264078
Feeling of despair 33.66 31.18 12 7951 3786 110577550
Migraine 32.33 31.18 50 7913 171602 110409734

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AE02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Sphingosine-1-phosphate (S1P) receptor modulators
MeSH PA D000081243 Sphingosine 1 Phosphate Receptor Modulators
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
FDA MoA N0000181815 Sphingosine 1-Phosphate Receptor Modulators
FDA EPC N0000181816 Sphingosine 1-phosphate Receptor Modulator
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:67079 anti-inflammatory agent

Related Drugs by ATC class:

L04AE Sphingosine-1-phosphate (S1P) receptor modulators 4 drugs
etrasimodfingolimodponesimodsiponimod

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 BRISTOL 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 BRISTOL 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 BRISTOL 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 BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 10239846 Nov. 15, 2030 TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC) IN ADULTS
EQ 0.46MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 10239846 Nov. 15, 2030 TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC) IN ADULTS
EQ 0.92MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 10239846 Nov. 15, 2030 TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC) IN ADULTS
EQ 0.23MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 8481573 March 24, 2033 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 BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 8481573 March 24, 2033 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 BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 8481573 March 24, 2033 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 BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 11680050 Sept. 30, 2038 TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC) IN ADULTS
EQ 0.23MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 11680050 Sept. 30, 2038 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 BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 11680050 Sept. 30, 2038 TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC) IN ADULTS
EQ 0.46MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 11680050 Sept. 30, 2038 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 BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 11680050 Sept. 30, 2038 TREATMENT OF MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UC) IN ADULTS
EQ 0.92MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL 11680050 Sept. 30, 2038 TREATMENT OF RELAPSING FORMS OF MULTIPLE SCLEROSIS (MS), TO INCLUDE CLINICALLY ISOLATED SYNDROME, RELAPSING-REMITTING DISEASE, AND ACTIVE SECONDARY PROGRESSIVE DISEASE, IN ADULTS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.23MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL Aug. 30, 2027 INFORMATION ADDED TO THE LABELING TO INCLUDE RESULTS FROM A STUDY TO FULFILL POST MARKETING REQUIREMENT 3809-5
EQ 0.46MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL Aug. 30, 2027 INFORMATION ADDED TO THE LABELING TO INCLUDE RESULTS FROM A STUDY TO FULFILL POST MARKETING REQUIREMENT 3809-5
EQ 0.92MG BASE ZEPOSIA BRISTOL N209899 March 25, 2020 RX CAPSULE ORAL Aug. 30, 2027 INFORMATION ADDED TO THE LABELING TO INCLUDE RESULTS FROM A STUDY TO FULFILL POST MARKETING REQUIREMENT 3809-5

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
CHEBI:234516 CHEBI
CHEMBL3707247 ChEMBL_ID
52938427 PUBCHEM_CID
DB12612 DRUGBANK_ID
CHEMBL3707246 ChEMBL_ID
10057 INN_ID
C000607776 MESH_SUPPLEMENTAL_RECORD_UI
D10968 KEGG_DRUG
8709 IUPHAR_LIGAND_ID
870525003 SNOMEDCT_US
871794001 SNOMEDCT_US
871800005 SNOMEDCT_US
JEU PDB_CHEM_ID
38279 MMSL
d09534 MMSL
018313 NDDF
018314 NDDF
2288235 RXNORM
Z80293URPV INXIGHT DRUGS

Pharmaceutical products:

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