Peringatan Keamanan

Patients experiencing an overdose may present with bradycardia, AV conduction block, and changes in blood pressure.L32709 Patients should be monitored for pulse rate and blood pressure, as well as ECGs.L32709 Treat patients with symptomatic and supportive measures, which may include atropine for bradycardia.L32709 dialysis is not expected to remove a significant amount of drug from blood.L32709

Ponesimod

DB12016

small molecule approved investigational

Deskripsi

Ponesimod is a selective sphingosine 1-phosphate receptor 1 modulator indicated in the treatment of relapsing forms of multiple sclerosis in adults.A232079,L32709 Ponesimod was developed out of a need for a more selective modulator of sphingosine 1-phosphate receptor 1 than fingolimod.A232079 Fingolimod's activity at sphingosine 1-phosphate receptor 3 was suspected to be responsible for a portion of it's adverse effects, and so more selective modulators were developed.A232079

Ponesimod was granted FDA approval on 18 March 2021.L32709

Struktur Molekul 2D

Berat 460.97
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ponesimod has an elimination half life of 33 hours.[L32709]
Volume Distribusi The volume of distribution of ponesimod at steady state is 160 L.[L32709]
Klirens (Clearance) The clearance of ponesimod is 3.8 L/h.[L32709]

Absorpsi

A 10mg oral dose of ponesimod is 84% bioavailable.L32709 Ponesimod reaches a Cmax of 109 ng/mL, with a Tmax of 4.0 hours, and an AUC of 3872 h\*ng/mL.A232079

Metabolisme

Ponesimod can be sulfated to the M5 metabolite, oxidized to an undefined M27 metabolite, reduced to the M6 metabolite, dealkylated to the M32 metabolite, or oxidized and hydrolyzed to the M13 metabolite.A232079,L32709 Ponesimod can also be oxidized by CYP2J2, CYP3A4, CYP3A5, CYP4F3A, and CYP4F12 to the M12 metabolite.A232079,L32709 The undefined M27 metabolite can be glucuronidated by UGT1A1 and UGT 2B7 to the M38, M39, and M40 metabolites.A232079,L32709 The M12 metabolite is either dealkylated to the M32 metabolite or oxidized and hydrolyzed to M13.A232079 M13 is dealkylated to M32, which is reduced and oxidized to M48.A232079

Rute Eliminasi

57.3-79.6% of a radiolabelled oral dose is recovered in the feces, with 16-26% as the unmetabolized parent compound and 22% as the M12 metabolite.A232079,L32709 10.3-18.4% of an oral dose is eliminated in the urine.A232079,L32709 0.6-1.9% of a radiolabelled dose was recovered as expired CO2.A232079

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption of ponesimod is not significantly affected by food.

Interaksi Obat

984 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Ponesimod.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Ponesimod.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Ponesimod.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Ponesimod.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Ponesimod.
Fluticasone furoate The risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Ponesimod.
Fluticasone The risk or severity of adverse effects can be increased when Ponesimod is combined with Fluticasone.
Budesonide The risk or severity of adverse effects can be increased when Budesonide is combined with Ponesimod.
Dexamethasone The risk or severity of adverse effects can be increased when Dexamethasone is combined with Ponesimod.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Ponesimod.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Ponesimod.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Ponesimod.
Mometasone The risk or severity of adverse effects can be increased when Mometasone is combined with Ponesimod.
Clobetasol propionate The risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Ponesimod.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Ponesimod.
Fluocinonide The risk or severity of adverse effects can be increased when Fluocinonide is combined with Ponesimod.
Cortisone acetate The risk or severity of adverse effects can be increased when Cortisone acetate is combined with Ponesimod.
Paramethasone The risk or severity of adverse effects can be increased when Paramethasone is combined with Ponesimod.
Fluprednidene The risk or severity of adverse effects can be increased when Fluprednidene is combined with Ponesimod.
Fluocortolone The risk or severity of adverse effects can be increased when Fluocortolone is combined with Ponesimod.
Difluocortolone The risk or severity of adverse effects can be increased when Difluocortolone is combined with Ponesimod.
Meprednisone The risk or severity of adverse effects can be increased when Meprednisone is combined with Ponesimod.
Dexamethasone isonicotinate The risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Ponesimod.
Cortivazol The risk or severity of adverse effects can be increased when Ponesimod is combined with Cortivazol.
Prednylidene The risk or severity of adverse effects can be increased when Ponesimod is combined with Prednylidene.
Cloprednol The risk or severity of adverse effects can be increased when Ponesimod is combined with Cloprednol.
Mometasone furoate The risk or severity of adverse effects can be increased when Ponesimod is combined with Mometasone furoate.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Ponesimod.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Ponesimod.
Tretinoin The metabolism of Ponesimod can be decreased when combined with Tretinoin.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Ponesimod.
Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Ponesimod.
Hydrocortisone acetate The risk or severity of adverse effects can be increased when Ponesimod is combined with Hydrocortisone acetate.
Hydrocortisone butyrate The risk or severity of adverse effects can be increased when Ponesimod is combined with Hydrocortisone butyrate.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ponesimod.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Ponesimod.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Ponesimod.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Ponesimod.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Ponesimod.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Ponesimod.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Ponesimod.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Ponesimod.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Ponesimod.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Ponesimod.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Ponesimod.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Ponesimod.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Ponesimod.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Ponesimod.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Ponesimod.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Ponesimod.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ponesimod.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Ponesimod.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Ponesimod.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Ponesimod.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Ponesimod.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Ponesimod.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Ponesimod.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Ponesimod.
Cladribine Ponesimod may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Ponesimod.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Ponesimod.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Ponesimod.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Ponesimod.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Ponesimod.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Ponesimod.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Ponesimod.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Ponesimod.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Ponesimod.
Fluorometholone The risk or severity of adverse effects can be increased when Fluorometholone is combined with Ponesimod.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Ponesimod.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Ponesimod.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Ponesimod.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Ponesimod.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Ponesimod.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Ponesimod.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Ponesimod.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Ponesimod.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Ponesimod.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Ponesimod.
Desoximetasone The risk or severity of adverse effects can be increased when Desoximetasone is combined with Ponesimod.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Ponesimod.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Ponesimod.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Ponesimod.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Ponesimod.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Ponesimod.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Ponesimod.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Ponesimod.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Ponesimod.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Ponesimod.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Ponesimod.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Ponesimod.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Ponesimod.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Ponesimod.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Ponesimod.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Ponesimod.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Ponesimod.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Ponesimod.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Ponesimod.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Ponesimod.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Ponesimod.

Target Protein

Sphingosine 1-phosphate receptor 1 S1PR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25188442
    Reyes M, Hoch M, Brossard P, Wagner-Redeker W, Miraval T, Dingemanse J: Mass balance, pharmacokinetics and metabolism of the selective S1P1 receptor modulator ponesimod in humans. Xenobiotica. 2015 Feb;45(2):139-49. doi: 10.3109/00498254.2014.955832. Epub 2014 Sep 4.
  • PMID: 26770667
    D'Ambrosio D, Freedman MS, Prinz J: Ponesimod, a selective S1P1 receptor modulator: a potential treatment for multiple sclerosis and other immune-mediated diseases. Ther Adv Chronic Dis. 2016 Jan;7(1):18-33. doi: 10.1177/2040622315617354.

Contoh Produk & Brand

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International Brands
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