Peringatan Keamanan

The LD50 of fingolimod in rats ranges from 300-600 mg/kg.A192906

Prescribing information for fingolimod does not mention symptoms or management of an overdose L12651, however, a case report of an intentional overdose with 14mg of fingolimod and 2g phenoxymethylpenicillin resulted in hypotension in bradycardia, resolved by administering atropine.A192909 Since fingolimod has been associated with cardiotoxicity, it would be reasonable to expect cardiac effects such as bradycardia and heart block in the case of an overdose.A192912,L12651

Fingolimod

DB08868

small molecule approved investigational

Deskripsi

Multiple sclerosis, or MS, is a devastating inflammatory disease that often progresses and causes severe neurological, physical, and cognitive effects.A176474 Fingolimod is a sphingosine 1-phosphate receptor modulator for the treatment of relapsing-remitting multiple sclerosis. It was developed by Novartis and initially approved by the FDA in 2010.L12651 Fingolimod was also studied for the treatment of COVID-19, the disease caused by infection with the SARS-CoV-2 virus.L12654,L12657

Struktur Molekul 2D

Berat 307.4708
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 fingolimod and its active metabolite ranges from 6-9 days.[A38022,L12651]
Volume Distribusi The volume of distribution of fingolimod is about 1200±260 L. It is approximately 86% distributed in the red blood cells (RBC).[A38022,L12651]
Klirens (Clearance) Fingolimod blood clearance is 6.3±2.3 L/h,[L12651] according to prescribing information. Another resource mentions it ranges from 6-8 L/h.[A38022]

Absorpsi

Fingolimod is slowly but efficiently absorbed in the gastrointestinal tract. AUC varies greatly, depending on the patient, and pharmacokinetic studies demonstrate a range of AUC values for fingolimod.A38022 The Tmax of fingolimod ranges between 12-16 hours and its bioavailability is 90-93%. Steady-state concentrations of fingolimod are achieved within 1-2 months after initiation when it is administered in a single daily dose.A38022,L12651

Metabolisme

Sphingosine kinase metabolizes fingolimod to an active metabolite, fingolimod phosphate. Fingolimod metabolism occurs via 3 major metabolic pathways: firstly, phosphorylation of the (S)-enantiomer of fingolimod-phosphate (pharmacologically active), secondly, oxidation by cytochrome P450 4F2 (CYP4F2), and thirdly, fatty acid-like metabolism to various inactive metabolites. The formation of inactive non-polar ceramide analogs of fingolimod also occurs during its metabolism.A38022,L12651

Rute Eliminasi

About 81% of an oral dose of fingolimod is excreted in the urine in the form of inactive metabolites. Intact fingolimod and its active metabolite account for less than 2.5% of the dose, and can be found excreted in the feces.L12651

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

573 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Fingolimod.
Natalizumab The risk or severity of immunosuppression can be increased when Fingolimod is combined with Natalizumab.
Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Fingolimod.
Roflumilast Roflumilast may increase the immunosuppressive activities of Fingolimod.
Sipuleucel-T The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Fingolimod.
Ceritinib Fingolimod may increase the bradycardic activities of Ceritinib.
Ivabradine Fingolimod may increase the bradycardic activities of Ivabradine.
Esmolol Esmolol may increase the bradycardic activities of Fingolimod.
Betaxolol Betaxolol may increase the bradycardic activities of Fingolimod.
Metoprolol Metoprolol may increase the bradycardic activities of Fingolimod.
Atenolol Atenolol may increase the bradycardic activities of Fingolimod.
Timolol Timolol may increase the bradycardic activities of Fingolimod.
Sotalol Sotalol may increase the bradycardic activities of Fingolimod.
Propranolol Propranolol may increase the bradycardic activities of Fingolimod.
Labetalol Labetalol may increase the bradycardic activities of Fingolimod.
Bisoprolol Bisoprolol may increase the bradycardic activities of Fingolimod.
Alprenolol Alprenolol may increase the bradycardic activities of Fingolimod.
Pindolol Pindolol may increase the bradycardic activities of Fingolimod.
Carvedilol Carvedilol may increase the bradycardic activities of Fingolimod.
Propafenone Propafenone may increase the bradycardic activities of Fingolimod.
Acebutolol Acebutolol may increase the bradycardic activities of Fingolimod.
Nadolol Nadolol may increase the bradycardic activities of Fingolimod.
Bevantolol Bevantolol may increase the bradycardic activities of Fingolimod.
Practolol Practolol may increase the bradycardic activities of Fingolimod.
Penbutolol Penbutolol may increase the bradycardic activities of Fingolimod.
Oxprenolol Oxprenolol may increase the bradycardic activities of Fingolimod.
Dexpropranolol Dexpropranolol may increase the bradycardic activities of Fingolimod.
Celiprolol Celiprolol may increase the bradycardic activities of Fingolimod.
Nebivolol Nebivolol may increase the bradycardic activities of Fingolimod.
Bufuralol Bufuralol may increase the bradycardic activities of Fingolimod.
Bopindolol Bopindolol may increase the bradycardic activities of Fingolimod.
Bupranolol Bupranolol may increase the bradycardic activities of Fingolimod.
Indenolol Indenolol may increase the bradycardic activities of Fingolimod.
Arotinolol Arotinolol may increase the bradycardic activities of Fingolimod.
Levobetaxolol Levobetaxolol may increase the bradycardic activities of Fingolimod.
Talinolol Talinolol may increase the bradycardic activities of Fingolimod.
Anisodamine Anisodamine may increase the bradycardic activities of Fingolimod.
Bucindolol Bucindolol may increase the bradycardic activities of Fingolimod.
Esatenolol Esatenolol may increase the bradycardic activities of Fingolimod.
Cloranolol Cloranolol may increase the bradycardic activities of Fingolimod.
Mepindolol Mepindolol may increase the bradycardic activities of Fingolimod.
Epanolol Epanolol may increase the bradycardic activities of Fingolimod.
Tertatolol Tertatolol may increase the bradycardic activities of Fingolimod.
Landiolol Landiolol may increase the bradycardic activities of Fingolimod.
Dofetilide Fingolimod may increase the arrhythmogenic activities of Dofetilide.
Ibutilide Fingolimod may increase the arrhythmogenic activities of Ibutilide.
Amiodarone Fingolimod may increase the arrhythmogenic activities of Amiodarone.
Bretylium Fingolimod may increase the arrhythmogenic activities of Bretylium.
Dronedarone Fingolimod may increase the arrhythmogenic activities of Dronedarone.
Azimilide Fingolimod may increase the arrhythmogenic activities of Azimilide.
Tedisamil Fingolimod may increase the arrhythmogenic activities of Tedisamil.
Vernakalant Fingolimod may increase the arrhythmogenic activities of Vernakalant.
Bunaftine Fingolimod may increase the arrhythmogenic activities of Bunaftine.
Disopyramide Fingolimod may increase the arrhythmogenic activities of Disopyramide.
Quinidine Fingolimod may increase the arrhythmogenic activities of Quinidine.
Procainamide Fingolimod may increase the arrhythmogenic activities of Procainamide.
Ajmaline Fingolimod may increase the arrhythmogenic activities of Ajmaline.
Sparteine Fingolimod may increase the arrhythmogenic activities of Sparteine.
Cibenzoline Fingolimod may increase the arrhythmogenic activities of Cibenzoline.
Prajmaline Fingolimod may increase the arrhythmogenic activities of Prajmaline.
Lorajmine Fingolimod may increase the arrhythmogenic activities of Lorajmine.
Hydroquinidine Fingolimod may increase the arrhythmogenic activities of Hydroquinidine.
Carbamazepine The serum concentration of Fingolimod can be decreased when it is combined with Carbamazepine.
Diltiazem The risk or severity of bradycardia can be increased when Diltiazem is combined with Fingolimod.
Verapamil The risk or severity of bradycardia can be increased when Verapamil is combined with Fingolimod.
Ketoconazole The serum concentration of Fingolimod can be increased when it is combined with Ketoconazole.
Sulfamethoxazole The risk or severity of myelosuppression can be increased when Sulfamethoxazole is combined with Fingolimod.
Tofacitinib Fingolimod may increase the immunosuppressive activities of Tofacitinib.
Ruxolitinib Ruxolitinib may increase the immunosuppressive activities of Fingolimod.
Etanercept Etanercept may increase the immunosuppressive activities of Fingolimod.
Peginterferon alfa-2a Peginterferon alfa-2a may increase the immunosuppressive activities of Fingolimod.
Interferon alfa-n1 Interferon alfa-n1 may increase the immunosuppressive activities of Fingolimod.
Interferon alfa-n3 Interferon alfa-n3 may increase the immunosuppressive activities of Fingolimod.
Peginterferon alfa-2b Peginterferon alfa-2b may increase the immunosuppressive activities of Fingolimod.
Anakinra Anakinra may increase the immunosuppressive activities of Fingolimod.
Interferon gamma-1b Interferon gamma-1b may increase the immunosuppressive activities of Fingolimod.
Interferon alfa-2a Interferon alfa-2a may increase the immunosuppressive activities of Fingolimod.
Aldesleukin Aldesleukin may increase the immunosuppressive activities of Fingolimod.
Adalimumab Adalimumab may increase the immunosuppressive activities of Fingolimod.
Gemtuzumab ozogamicin Gemtuzumab ozogamicin may increase the immunosuppressive activities of Fingolimod.
Pegaspargase Pegaspargase may increase the immunosuppressive activities of Fingolimod.
Infliximab Infliximab may increase the immunosuppressive activities of Fingolimod.
Interferon beta-1b Interferon beta-1b may increase the immunosuppressive activities of Fingolimod.
Interferon alfacon-1 Interferon alfacon-1 may increase the immunosuppressive activities of Fingolimod.
Trastuzumab The risk or severity of neutropenia can be increased when Trastuzumab is combined with Fingolimod.
Rituximab Rituximab may increase the immunosuppressive activities of Fingolimod.
Basiliximab Basiliximab may increase the immunosuppressive activities of Fingolimod.
Muromonab Muromonab may increase the immunosuppressive activities of Fingolimod.
Ibritumomab tiuxetan Ibritumomab tiuxetan may increase the immunosuppressive activities of Fingolimod.
Tositumomab Tositumomab may increase the immunosuppressive activities of Fingolimod.
Alemtuzumab Alemtuzumab may increase the immunosuppressive activities of Fingolimod.
Alefacept Alefacept may increase the immunosuppressive activities of Fingolimod.
Efalizumab Efalizumab may increase the immunosuppressive activities of Fingolimod.
Antithymocyte immunoglobulin (rabbit) Antithymocyte immunoglobulin (rabbit) may increase the immunosuppressive activities of Fingolimod.
Interferon alfa-2b Interferon alfa-2b may increase the immunosuppressive activities of Fingolimod.
Daclizumab Daclizumab may increase the immunosuppressive activities of Fingolimod.
Phenylalanine Phenylalanine may increase the immunosuppressive activities of Fingolimod.
Flunisolide Flunisolide may increase the immunosuppressive activities of Fingolimod.
Bortezomib Bortezomib may increase the immunosuppressive activities of Fingolimod.
Cladribine Cladribine may increase the immunosuppressive activities of Fingolimod.

Target Protein

D(3) dopamine receptor DRD3
Sphingosine kinase 1 SPHK1
Sphingosine 1-phosphate receptor 5 S1PR5
Sphingosine 1-phosphate receptor 1 S1PR1
Sphingosine 1-phosphate receptor 3 S1PR3
Histone deacetylase 1 HDAC1
Sphingosine 1-phosphate receptor 4 S1PR4

Referensi & Sumber

Synthesis reference: Ramesh Matioram Gidwani, Channaveerayya Hiremath, "PROCESS FOR PRODUCING FINGOLIMOD SALTS." U.S. Patent US20120184617, issued July 19, 2012.
Artikel (PubMed)
  • PMID: 23609767
    An X, Kezuka T, Usui Y, Matsunaga Y, Matsuda R, Yamakawa N, Goto H: Suppression of experimental autoimmune optic neuritis by the novel agent fingolimod. J Neuroophthalmol. 2013 Jun;33(2):143-8. doi: 10.1097/WNO.0b013e31828ea2fc.
  • PMID: 23609782
    Ali R, Nicholas RS, Muraro PA: Drugs in development for relapsing multiple sclerosis. Drugs. 2013 May;73(7):625-50. doi: 10.1007/s40265-013-0030-6.
  • 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: 22149256
    David OJ, Kovarik JM, Schmouder RL: Clinical pharmacokinetics of fingolimod. Clin Pharmacokinet. 2012 Jan 1;51(1):15-28. doi: 10.2165/11596550-000000000-00000.
  • 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: 15772896
    Dumont FJ: Fingolimod. Mitsubishi Pharma/Novartis. IDrugs. 2005 Mar;8(3):236-53.
  • PMID: 24178903
    Stephenson M, Wong A, Rotella JA, Crump N, Kerr F, Greene SL: Deliberate fingolimod overdose presenting with delayed hypotension and bradycardia responsive to atropine. J Med Toxicol. 2014 Jun;10(2):215-8. doi: 10.1007/s13181-013-0354-3.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 76 • International brands: 1
Produk
  • Ach-fingolimod
    Capsule • 0.5 mg • Oral • Canada • Generic • Approved
  • Apo-fingolimod
    Capsule • 0.5 mg • Oral • Canada • Generic • Approved
  • Asn-fingolimod
    Capsule • 0.5 mg • Oral • Canada • Approved
  • Fingolimod
    Capsule • 0.5 mg/1 • Oral • US • Generic • Approved
  • Fingolimod
    Capsule • 0.5 mg/1 • Oral • US • Generic • Approved
  • Fingolimod
    Capsule • 0.5 mg/1 • Oral • US • Generic • Approved
  • Fingolimod
    Capsule • 0.5 mg/1 • Oral • US • Generic • Approved
  • Fingolimod
    Capsule • 0.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 76 produk.
International Brands
  • Gilenia

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