Peringatan Keamanan

Teriflunomide is contraindicated in pregnant women or women of childbearing age due to the risk of teratogenicity. Teriflunomide is also contraindicated in severe hepatic impairment due to reports of hepatotoxicity, hepatic failure, and death.

Teriflunomide

DB08880

small molecule approved

Deskripsi

Teriflunomide is the active metabolite of leflunomide, and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis. It is marketed under the name Aubagio® and is indicated for the treatment of multiple sclerosis, specifically relapsing forms. The FDA label states an important warning about the risk of hepatoxicity and teratogenicity for patients using teriflunomide.

Struktur Molekul 2D

Berat 270.2073
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median half-life is 18 to 19 days.
Volume Distribusi After a single intravenous dose, the volume of distribution is 11 L.
Klirens (Clearance) After a single IV dose, teriflunomide has a total body clearance of 30.5 mL/h.

Absorpsi

After oral administration of teriflunomide, maximum plasma concentrations are reached, on average, in 1-4 hours.

Metabolisme

Teriflunomide mainly undergoes hydrolyis to minor metabolites. Other minor metabolic pathways include oxidation, N-acetylation and sulfate conjugation. Teriflunomide is not metabolized by CYP450 or flavin monoamine oxidase.

Rute Eliminasi

Teriflunomide is eliminated unchanged and mainly through bile. Specifically 37.5% is eliminated in the feces and 22.6% in urine.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

824 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Teriflunomide.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Teriflunomide.
Peginterferon alfa-2a The risk or severity of liver damage can be increased when Peginterferon alfa-2a is combined with Teriflunomide.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Teriflunomide.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Teriflunomide.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Teriflunomide.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Teriflunomide.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Teriflunomide.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Teriflunomide.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Teriflunomide.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Teriflunomide.
Gemtuzumab ozogamicin The risk or severity of liver damage can be increased when Gemtuzumab ozogamicin is combined with Teriflunomide.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Teriflunomide.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Teriflunomide.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Teriflunomide.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Teriflunomide.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Teriflunomide.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Teriflunomide.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Teriflunomide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Teriflunomide.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Teriflunomide.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Teriflunomide.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Teriflunomide.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Teriflunomide.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Teriflunomide.
Interferon alfa-2b The risk or severity of liver damage can be increased when Interferon alfa-2b is combined with Teriflunomide.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Teriflunomide.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Teriflunomide.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Teriflunomide.
Cladribine The excretion of Cladribine can be decreased when combined with Teriflunomide.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Teriflunomide.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Teriflunomide.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Teriflunomide.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Teriflunomide.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Teriflunomide.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Teriflunomide.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Teriflunomide.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Teriflunomide.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Teriflunomide.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Teriflunomide.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Teriflunomide.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Teriflunomide.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Teriflunomide.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Teriflunomide.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Teriflunomide.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Teriflunomide.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Teriflunomide.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Teriflunomide.
Epirubicin The risk or severity of liver damage can be increased when Epirubicin is combined with Teriflunomide.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Teriflunomide.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Teriflunomide.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Teriflunomide.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Teriflunomide.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Teriflunomide.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Teriflunomide.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Teriflunomide.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Teriflunomide.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Teriflunomide.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Teriflunomide.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Teriflunomide.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Teriflunomide.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Teriflunomide.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Teriflunomide.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Teriflunomide.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Teriflunomide.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Teriflunomide.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Teriflunomide.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Teriflunomide.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Teriflunomide.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Teriflunomide.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Teriflunomide.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Teriflunomide.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Teriflunomide.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Teriflunomide.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Teriflunomide.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Teriflunomide.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Teriflunomide.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Teriflunomide.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Teriflunomide.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Teriflunomide.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Teriflunomide.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Teriflunomide.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Teriflunomide.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Teriflunomide.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Teriflunomide.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Teriflunomide.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Teriflunomide.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Teriflunomide.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Teriflunomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Teriflunomide.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Teriflunomide.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Teriflunomide.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Teriflunomide.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Teriflunomide.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Teriflunomide.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Teriflunomide.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Teriflunomide.
Ifosfamide The risk or severity of adverse effects can be increased when Ifosfamide is combined with Teriflunomide.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Teriflunomide.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Teriflunomide.

Target Protein

Dihydroorotate dehydrogenase (quinone), mitochondrial
3-hydroxy-3-methylglutaryl-coenzyme A reductase HMGCR
Dihydroorotate dehydrogenase (quinone), mitochondrial DHODH

Referensi & Sumber

Synthesis reference: Keshav Deo, Samir Patel, Snehal Dhol, Sunil Sanghani, Vishal Ray, " PROCESS FOR PREPARING TERIFLUNOMIDE." U.S. Patent US20110092727, issued April 21, 2011.
Artikel (PubMed)
  • PMID: 16567708
    O'Connor PW, Li D, Freedman MS, Bar-Or A, Rice GP, Confavreux C, Paty DW, Stewart JA, Scheyer R: A Phase II study of the safety and efficacy of teriflunomide in multiple sclerosis with relapses. Neurology. 2006 Mar 28;66(6):894-900.
  • PMID: 18782502
    Tallantyre E, Evangelou N, Constantinescu CS: Spotlight on teriflunomide. Int MS J. 2008 Jun;15(2):62-8.

Contoh Produk & Brand

Produk: 91 • International brands: 0
Produk
  • Ach-teriflunomide
    Tablet • 14 mg • Oral • Canada • Generic • Approved
  • Apo-teriflunomide
    Tablet • 14 mg • Oral • Canada • Generic • Approved
  • Aubagio
    Tablet, film coated • 7 mg/1 • Oral • US • Approved
  • Aubagio
    Tablet, film coated • 14 mg/1 • Oral • US • Approved
  • Aubagio
    Tablet • 14 mg • Oral • Canada • Approved
  • Aubagio
    Tablet, film coated • 14 mg • Oral • EU • Approved
  • Aubagio
    Tablet, film coated • 14 mg • Oral • EU • Approved
  • Aubagio
    Tablet, film coated • 14 mg • Oral • EU • Approved
Menampilkan 8 dari 91 produk.

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