Peringatan Keamanan

Overdose and LD50 information for ozanimod is not readily available in the literature.A189321,A192747,L12582 The NOAEL dose is 0.164 mg/kg/d for monkeys, and the human equivalent dose to this is about 0.053 mg/kg/day.A189321 An overdose of this drug likely results in adverse effects such as somnolence, fatigue, headache, dizziness, bradyarrhythmia, cardiac conduction defects, hypertension, liver injury, and nausea.A189321,L12582

Ozanimod

DB12612

small molecule approved investigational

Deskripsi

Ozanimod is a once-daily sphingosine 1-phosphate receptor modulator for the treatment of relapsing Multiple Sclerosis (MS) and inflammatory bowel disease. It was developed by Celgene (now acquired by Bristol-Myers Squibb) L11025 and was approved by the FDA on March 26, 2020.L12573,L12582 The US approval was followed by the approval in Canada on October 2, 2020.L41524 In November 2021, ozanimod was also approved by the European Commission for the treatment of adults with relapsing remitting multiple sclerosis.L39377,L39382

MS is a devastating inflammatory disease that often progresses and causes severe neurological, physical, and cognitive effects.A176474 Inflammatory bowel disease also a chronic inflammatory condition and can cause persistent abdominal pain, diarrhea, bloody stools, and vomiting.A189336

In clinical trials, Ozanimod has been shown to be well-tolerated and has resulted in a higher decrease in the rate of MS relapses than with intramuscular interferon beta-1a, a current standard in MS therapy. Studies involving patients with inflammatory bowel disease have also shown promising results.A189318,A189342

Struktur Molekul 2D

Berat 404.47
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of ozanimod ranges from 17-21 hours.[A189321,A192744,L12582]
Volume Distribusi The average volume of distribution of ozanimod is 5590L.[L12582] Another reference mentions a volume of distribution ranging from 73-101 L/kg.[A189321] This drug crosses the blood-brain barrier.[A192744]
Klirens (Clearance) The mean apparent oral clearance of ozanimod, according to prescribing information, is 192 L/h.[L12582] Another reference indicates an oral clearance of 233 L/h.[A189321]

Absorpsi

Ozanimod is absorbed in the gastrointestinal tract after oral administration. The Cmax of ozanimod is 0.244 ng/mLL12582 and is achieved at 6 to 8 hours after administrationA192744, reaching steady-state at about 102 hours after administration. The AUC is 4.46 ng*h/mL.L12582 Its delayed absorption reduces effects that may occur after the first dose, such as heart rate changes. The peak plasma concentration of ozanimod is low due to a high volume of distribution.A192744

Metabolisme

Ozanimod has two major active metabolites CC112273 and CC1084037 and minor active metabolites such as RP101988, RP101075, and RP101509, which target the S1P1 and S1P5 receptors. The enzymes involved in the metabolism of ozanimod include ALDH/ADH, NAT-2, Monoamine Oxidase B, and AKR 1C1/1C2. After metabolism, ozanimod (6%), CC112273 (73%), and CC1084037 (15%) are accounted for in the circulation.L12582

Rute Eliminasi

The kidneys are not a major source of elimination for ozanimod.A189321 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.L12582

Interaksi Makanan

2 Data
  • 1. Avoid tyramine-containing foods and supplements. Avoid food containing high amounts of tyramine (>150mg) as these may increase the risk of hypertension when taken with ozanimod.
  • 2. Take with or without food.

Interaksi Obat

607 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Ozanimod.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Ozanimod.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ozanimod.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Ozanimod.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Ozanimod.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Ozanimod.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Ozanimod.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Ozanimod.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Ozanimod.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Ozanimod.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Ozanimod.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Ozanimod.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Ozanimod.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Ozanimod.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Ozanimod.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Ozanimod.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Ozanimod.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Ozanimod.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Ozanimod.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Ozanimod.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Ozanimod.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ozanimod.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Ozanimod.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Ozanimod.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Ozanimod.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Ozanimod.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Ozanimod.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Ozanimod.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Ozanimod.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Ozanimod.
Cladribine Ozanimod may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Ozanimod.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Ozanimod.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Ozanimod.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Ozanimod.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Ozanimod.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Ozanimod.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Ozanimod.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Ozanimod.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Ozanimod.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Ozanimod.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Ozanimod.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Ozanimod.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Ozanimod.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Ozanimod.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Ozanimod.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Ozanimod.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Ozanimod.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Ozanimod.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Ozanimod.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Ozanimod.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Ozanimod.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Ozanimod.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Ozanimod.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Ozanimod.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Ozanimod.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Ozanimod.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Ozanimod.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Ozanimod.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Ozanimod.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Ozanimod.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Ozanimod.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Ozanimod.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Ozanimod.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Ozanimod.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Ozanimod.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Ozanimod.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Ozanimod.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Ozanimod.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Ozanimod.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Ozanimod.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Ozanimod.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Ozanimod.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Ozanimod.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Ozanimod.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Ozanimod.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Ozanimod.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Ozanimod.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Ozanimod.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Ozanimod.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Ozanimod.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Ozanimod.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Ozanimod.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Ozanimod.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Ozanimod.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Ozanimod.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Ozanimod.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Ozanimod.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Ozanimod.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Ozanimod.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Ozanimod.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Ozanimod.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Ozanimod.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Ozanimod.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Ozanimod.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Ozanimod.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Ozanimod.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Ozanimod.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Ozanimod.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Ozanimod.

Target Protein

Sphingosine 1-phosphate receptor 1 S1PR1
Sphingosine 1-phosphate receptor 5 S1PR5

Referensi & Sumber

Synthesis reference: Florian Uthoff, Jana Löwe, Christina Harms, Kai Donsbach, Harald Gröger. Chemoenzymatic Synthesis of a Chiral Ozanimod Key Intermediate Starting from Naphthalene as Cheap Petrochemical Feedstock. April 2019. The Journal of Organic Chemistry. DOI: 10.1021/acs.joc.8b03290
Artikel (PubMed)
  • PMID: 31492652
    Cohen JA, Comi G, Selmaj KW, Bar-Or A, Arnold DL, Steinman L, Hartung HP, Montalban X, Kubala Havrdova E, Cree BAC, Sheffield JK, Minton N, Raghupathi K, Huang V, Kappos L: Safety and efficacy of ozanimod versus interferon beta-1a in relapsing multiple sclerosis (RADIANCE): a multicentre, randomised, 24-month, phase 3 trial. Lancet Neurol. 2019 Nov;18(11):1021-1033. doi: 10.1016/S1474-4422(19)30238-8. Epub 2019 Sep 3.
  • PMID: 28398597
    Tran JQ, Hartung JP, Peach RJ, Boehm MF, Rosen H, Smith H, Brooks JL, Timony GA, Olson AD, Gujrathi S, Frohna PA: 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.
  • PMID: 29125718
    Tran JQ, Hartung JP, Tompkins CA, Frohna PA: Effects of High- and Low-Fat Meals on the Pharmacokinetics of Ozanimod, a Novel Sphingosine-1-Phosphate Receptor Modulator. Clin Pharmacol Drug Dev. 2018 Aug;7(6):634-640. doi: 10.1002/cpdd.409. Epub 2017 Nov 10.
  • PMID: 28367411
    Ghasemi N, Razavi S, Nikzad E: Multiple Sclerosis: Pathogenesis, Symptoms, Diagnoses and Cell-Based Therapy. Cell J. 2017 Apr-Jun;19(1):1-10. Epub 2016 Dec 21.
  • PMID: 25075198
    Fakhoury M, Negrulj R, Mooranian A, Al-Salami H: Inflammatory bowel disease: clinical aspects and treatments. J Inflamm Res. 2014 Jun 23;7:113-20. doi: 10.2147/JIR.S65979. eCollection 2014.
  • PMID: 29051788
    Vetter M, Neurath MF: Emerging oral targeted therapies in inflammatory bowel diseases: opportunities and challenges. Therap Adv Gastroenterol. 2017 Oct;10(10):773-790. doi: 10.1177/1756283X17727388. Epub 2017 Sep 5.
  • PMID: 28812220
    Chaudhry BZ, Cohen JA, Conway DS: Sphingosine 1-Phosphate Receptor Modulators for the Treatment of Multiple Sclerosis. Neurotherapeutics. 2017 Oct;14(4):859-873. doi: 10.1007/s13311-017-0565-4.
  • PMID: 30043658
    Cohen JA, Comi G, Arnold DL, Bar-Or A, Selmaj KW, Steinman L, Havrdova EK, Cree BA, Montalban X, Hartung HP, Huang V, Frohna P, Skolnick BE, Kappos L: Efficacy and safety of ozanimod in multiple sclerosis: Dose-blinded extension of a randomized phase II study. Mult Scler. 2019 Aug;25(9):1255-1262. doi: 10.1177/1352458518789884. Epub 2018 Jul 25.

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