Details of the Drug

General Information of Drug (ID: DMT6AM2)

Drug Name
Ozanimod
Synonyms
1306760-87-1; Ozanimod (RPC1063); UNII-Z80293URPV; Z80293URPV; (S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile; Ozanimod [USAN:INN]; Ozanimod (USAN/INN); SCHEMBL2195490; GTPL8709; CHEMBL3707247; 5-[3-[(1S)-1-(2-hydroxyethylamino)-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile; EX-A1316; s7952; ZINC116109867; AKOS026674086; DB12612; CS-5070; HY-12288; AC-29883; Benzonitrile, 5-(3-((1
Indication
Disease Entry ICD 11 Status REF
Multiple sclerosis 8A40 Approved [1]
Non-small-cell lung cancer 2C25.Y Phase 3 [2]
Ulcerative colitis DD71 Phase 3 [3]
Crohn disease DD70 Phase 2 [3]
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 404.5
Logarithm of the Partition Coefficient (xlogp) 3.1
Rotatable Bond Count (rotbonds) 7
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 4.46 mcgh/L [4]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 0.244 mcg/L [4]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 6-8 h [4]
Clearance
The apparent oral clearance of drug is 192 L/h [4]
Elimination
After a 0.92 mg dose of radiolabeled ozanimod was administered, about 26% of the labeled drug was accounted for in the urine and 37 % in the feces, mainly in the form of inactive metabolites [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 17 - 21 hours [5]
Metabolism
The drug is metabolized via the ALDH/ADH, NAT-2, Monoamine Oxidase B, and AKR 1C1/1C2 [4]
Vd
The volume of distribution (Vd) of drug is 5590 L [4]
Chemical Identifiers
Formula
C23H24N4O3
IUPAC Name
5-[3-[(1S)-1-(2-hydroxyethylamino)-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile
Canonical SMILES
CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CC[C@@H](C4=CC=C3)NCCO)C#N
InChI
InChI=1S/C23H24N4O3/c1-14(2)29-21-9-6-15(12-16(21)13-24)23-26-22(27-30-23)19-5-3-4-18-17(19)7-8-20(18)25-10-11-28/h3-6,9,12,14,20,25,28H,7-8,10-11H2,1-2H3/t20-/m0/s1
InChIKey
XRVDGNKRPOAQTN-FQEVSTJZSA-N
Cross-matching ID
PubChem CID
52938427
CAS Number
1306760-87-1
DrugBank ID
DB12612
TTD ID
D07EDB
ACDINA ID
D01311
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Sphingosine-1-phosphate receptor 1 (S1PR1) TT9JZCK S1PR1_HUMAN Agonist [1]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Ozanimod (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of ventricular arrhythmias by the combination of Ozanimod and Ivosidenib. Acute myeloid leukaemia [2A60] [6]
Oliceridine DM6MDCF Major Increased risk of ventricular arrhythmias by the combination of Ozanimod and Oliceridine. Acute pain [MG31] [6]
Levalbuterol DM5YBO1 Major Increased risk of ventricular arrhythmias by the combination of Ozanimod and Levalbuterol. Asthma [CA23] [6]
Ag-221 DMS0ZBI Moderate Decreased clearance of Ozanimod due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [7]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Ozanimod and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [8]
Lisocabtagene maraleucel DMP45ME Major Additive immunosuppressive effects by the combination of Ozanimod and Lisocabtagene maraleucel. Diffuse large B-cell lymphoma [2A81] [9]
Axicabtagene ciloleucel DMYHN59 Major Additive immunosuppressive effects by the combination of Ozanimod and Axicabtagene ciloleucel. Diffuse large B-cell lymphoma [2A81] [9]
Ripretinib DM958QB Moderate Decreased metabolism of Ozanimod caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [7]
Avapritinib DMK2GZX Major Additive immunosuppressive effects by the combination of Ozanimod and Avapritinib. Gastrointestinal stromal tumour [2B5B] [9]
177Lu-DOTATATE DMT8GVU Major Additive immunosuppressive effects by the combination of Ozanimod and 177Lu-DOTATATE. Hepatitis virus infection [1E50-1E51] [9]
Lurbinectedin DMEFRTZ Major Additive immunosuppressive effects by the combination of Ozanimod and Lurbinectedin. Lung cancer [2C25] [9]
Selpercatinib DMZR15V Major Increased risk of ventricular arrhythmias by the combination of Ozanimod and Selpercatinib. Lung cancer [2C25] [6]
Tisagenlecleucel DMM9BJD Major Additive immunosuppressive effects by the combination of Ozanimod and Tisagenlecleucel. Mature B-cell lymphoma [2A85] [9]
Belantamab mafodotin DMBT3AI Major Additive immunosuppressive effects by the combination of Ozanimod and Belantamab mafodotin. Multiple myeloma [2A83] [9]
Macimorelin DMQYJIR Major Increased risk of ventricular arrhythmias by the combination of Ozanimod and Macimorelin. Pituitary gland disorder [5A60-5A61] [6]
Lefamulin DME6G97 Major Increased risk of ventricular arrhythmias by the combination of Ozanimod and Lefamulin. Pneumonia [CA40] [6]
Darolutamide DMV7YFT Moderate Decreased clearance of Ozanimod due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [10]
Tildrakizumab DMLW9HG Major Additive immunosuppressive effects by the combination of Ozanimod and Tildrakizumab. Psoriasis [EA90] [9]
Risankizumab DMM32GT Major Additive immunosuppressive effects by the combination of Ozanimod and Risankizumab. Psoriasis [EA90] [9]
Upadacitinib DM32B5U Major Additive immunosuppressive effects by the combination of Ozanimod and Upadacitinib. Rheumatoid arthritis [FA20] [9]
⏷ Show the Full List of 20 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Carmellose sodium E00625 Not Available Disintegrant
Ferric oxide black E00522 16211978 Colorant
Gelatin E00630 Not Available Other agent
Magnesium stearate E00208 11177 lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Colcothar yellow E00436 518696 Colorant
Haematite red E00236 14833 Colorant
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 9 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Ozanimod 0.23 mg capsule 0.23 mg Capsule Oral
Ozanimod 0.46 mg capsule 0.46 mg Capsule Oral
Ozanimod 0.92 mg capsule 0.92 mg Capsule Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
2 ClinicalTrials.gov (NCT02294058) Phase 3 Study of RPC1063 in Relapsing MS. U.S. National Institutes of Health.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 FDA Approved Products: Zeposia (Ozanimod) oral capsules
5 Results From the First-in-Human Study With Ozanimod, a Novel, Selective Sphingosine-1-Phosphate Receptor Modulator. J Clin Pharmacol. 2017 Aug;57(8):988-996. doi: 10.1002/jcph.887. Epub 2017 Apr 11.
6 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
7 Cerner Multum, Inc. "Australian Product Information.".
8 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
9 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
10 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.