Peringatan Keamanan

Toxicity information regarding filgotinib is not readily available; however, it has been administered in clinical trials at doses of up to 450 mg daily.L16616 Associated adverse effects were similar to those observed at lower doses.L16616 In the event of overdose, the patient should be closely monitored and supportive measures should be initiated as required.L16616

Filgotinib

DB14845

small molecule approved investigational

Deskripsi

Rheumatoid arthritis (RA) is a chronic, autoimmune, systemic, and inflammatory disease that causes synovial joint symptoms and can limit range of motion in severe cases.A221451,A221456 The disease is associated with extra-articular manifestations, progressive disability, and comorbidities including cardiovascular disease and mental disorders.A189165 50-70% of patients with RA are unable to achieve sustained clinical remission despite the availability of several treatments including disease-modifying anti-rheumatic drugs (DMARDS) like methotrexate, interleukin-6 (IL-6) blockers, and tumor necrosis factor (TNF) inhibitors.A189165 New therapeutic developments target other inflammatory pathways implicated in RA including the Janus kinase (JAK) signaling pathway as seen with filgotinib.A221456

There are four JAK subtypes which include JAK1, JAK2, JAK3, and tyrosine kinase 2.A189165 Non-selective JAK inhibitors like tofacitinib target JAK1 and JAK3 subtypes with minimal activity at JAK2. In contrast, the newly approved filgotinib is a highly selective JAK1 inhibitor.A189165 JAK2 and JAK3 play important roles in both immune and hematologic functions; therefore, selectivity for JAK1 aims to improve the safety profile of filgotinib while maintaining clinical efficacy.A189165 Filgotinib is currently reserved for patients who cannot tolerate DMARDs, or who have been unable to achieve remission in response to one or more DMARDs.L16616

Struktur Molekul 2D

Berat 425.51
Wujud -

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 filgotinib is estimated to be 7 hours, while the half-life of its active metabolite GS-829845 is estimated to be 19 hours.[L16616]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Filgotinib is rapidly absorbed after oral administration.L16616 Median peak plasma concentrations occurred 2-3 hours post-dose for filgotinib and 5 hours post-dose for GS-829845.L16616 Steady-state concentrations can be observed in 2-3 days for filgotinib and in 4 days for GS-829845.L16616 Food does not appear to have a significant effect on the absorption of filgotinib; therefore, the medication can be administered without regard to food.L16616 After repeated oral dosing of filgotinib 200 mg, the reported Cmax and AUC? values of filgotinib were 2.15 ug/mL and 6.77 ugxh/mL, respectively.L16616 For GS-829845 (the major metabolite) the reported Cmax was 4.43 ug/mL and the reported AUC? was 83.2 ugxh/mL.L16616

Metabolisme

Carboxylesterase enzymes are involved in the metabolism of filgotinib.A221331 The carboxylesterase 2 (CES2) isoform is chiefly responsible for metabolizing filgotinib to its major metabolite, GS-829845.A221331,A221336 Although carboxylesterase 1 (CES1) plays a less prominent role in the biotransformation of filgotinib, in vitro studies have demonstrated that CES1 will partially compensate in the event of CES2 saturation.A221331 GS-829845 is thus far the only major circulating metabolite to have been identified.L16616

Rute Eliminasi

Of the total administered dose of filgotinib, approximately 87% undergoes renal elimination while 15% undergoes faecal elimination.L16616

Interaksi Obat

445 Data
Theophylline The serum concentration of Theophylline can be increased when it is combined with Filgotinib.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Filgotinib.
Erlotinib The serum concentration of Erlotinib can be increased when it is combined with Filgotinib.
Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Filgotinib.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Filgotinib.
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Filgotinib.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Filgotinib.
Dacarbazine The serum concentration of Dacarbazine can be increased when it is combined with Filgotinib.
Pimozide The serum concentration of Pimozide can be increased when it is combined with Filgotinib.
Aminophylline The serum concentration of Aminophylline can be increased when it is combined with Filgotinib.
Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Filgotinib.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Filgotinib.
Pomalidomide The serum concentration of Pomalidomide can be increased when it is combined with Filgotinib.
Tegafur The serum concentration of Tegafur can be increased when it is combined with Filgotinib.
Enasidenib The serum concentration of Enasidenib can be increased when it is combined with Filgotinib.
Imipramine The serum concentration of Imipramine can be increased when it is combined with Filgotinib.
Clonidine The serum concentration of Clonidine can be increased when it is combined with Filgotinib.
Anagrelide The serum concentration of Anagrelide can be increased when it is combined with Filgotinib.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Filgotinib.
Clomipramine The serum concentration of Clomipramine can be increased when it is combined with Filgotinib.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Filgotinib.
Valsartan The serum concentration of Valsartan can be increased when it is combined with Filgotinib.
Erythromycin The serum concentration of Erythromycin can be increased when it is combined with Filgotinib.
Torasemide The serum concentration of Torasemide can be increased when it is combined with Filgotinib.
Liothyronine The serum concentration of Liothyronine can be increased when it is combined with Filgotinib.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Filgotinib.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Filgotinib.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Filgotinib.
Raloxifene The serum concentration of Raloxifene can be increased when it is combined with Filgotinib.
Caspofungin The serum concentration of Caspofungin can be increased when it is combined with Filgotinib.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Filgotinib.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Filgotinib.
Enalapril The serum concentration of Enalapril can be increased when it is combined with Filgotinib.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Filgotinib.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Filgotinib.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Filgotinib.
Penicillamine The serum concentration of Penicillamine can be increased when it is combined with Filgotinib.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Filgotinib.
Dinoprostone The serum concentration of Dinoprostone can be increased when it is combined with Filgotinib.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Filgotinib.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Filgotinib.
Benzylpenicillin The serum concentration of Benzylpenicillin can be increased when it is combined with Filgotinib.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Filgotinib.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Filgotinib.
Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Filgotinib.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Filgotinib.
Liotrix The serum concentration of Liotrix can be increased when it is combined with Filgotinib.
Cholic Acid The serum concentration of Cholic Acid can be increased when it is combined with Filgotinib.
Taurocholic acid The serum concentration of Taurocholic acid can be increased when it is combined with Filgotinib.
Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Filgotinib.
Atrasentan The serum concentration of Atrasentan can be increased when it is combined with Filgotinib.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Filgotinib.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Filgotinib.
Axitinib The serum concentration of Axitinib can be increased when it is combined with Filgotinib.
Gimatecan The serum concentration of Gimatecan can be increased when it is combined with Filgotinib.
Temocapril The serum concentration of Temocapril can be increased when it is combined with Filgotinib.
Cholecystokinin The serum concentration of Cholecystokinin can be increased when it is combined with Filgotinib.
Gadoxetic acid The serum concentration of Gadoxetic acid can be increased when it is combined with Filgotinib.
Technetium Tc-99m mebrofenin The serum concentration of Technetium Tc-99m mebrofenin can be increased when it is combined with Filgotinib.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Filgotinib.
Fimasartan The serum concentration of Fimasartan can be increased when it is combined with Filgotinib.
Paritaprevir The serum concentration of Paritaprevir can be increased when it is combined with Filgotinib.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Filgotinib.
Selexipag The serum concentration of Selexipag can be increased when it is combined with Filgotinib.
Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Filgotinib.
Asunaprevir The serum concentration of Asunaprevir can be increased when it is combined with Filgotinib.
Revefenacin The serum concentration of Revefenacin can be increased when it is combined with Filgotinib.
Elagolix The serum concentration of Elagolix can be increased when it is combined with Filgotinib.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Filgotinib.
Letermovir The serum concentration of Letermovir can be increased when it is combined with Filgotinib.
Levosalbutamol The serum concentration of Levosalbutamol can be increased when it is combined with Filgotinib.
Levomenol The serum concentration of Levomenol can be increased when it is combined with Filgotinib.
Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Filgotinib.
Remdesivir The serum concentration of Remdesivir can be increased when it is combined with Filgotinib.
Prasterone The serum concentration of Prasterone can be increased when it is combined with Filgotinib.
Belantamab mafodotin The serum concentration of Belantamab mafodotin can be increased when it is combined with Filgotinib.
Brincidofovir The serum concentration of Brincidofovir can be increased when it is combined with Filgotinib.
Cyclosporine Filgotinib may increase the immunosuppressive activities of Cyclosporine.
Bortezomib The serum concentration of Bortezomib can be increased when it is combined with Filgotinib.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Filgotinib.
Vinblastine The serum concentration of Vinblastine can be increased when it is combined with Filgotinib.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Filgotinib.
Quinidine The serum concentration of Quinidine can be increased when it is combined with Filgotinib.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Filgotinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Filgotinib.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Filgotinib.
Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Filgotinib.
Temsirolimus The serum concentration of Temsirolimus can be increased when it is combined with Filgotinib.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Filgotinib.
Bendamustine The serum concentration of Bendamustine can be increased when it is combined with Filgotinib.
Cabazitaxel The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Filgotinib.
Crizotinib The serum concentration of Crizotinib can be increased when it is combined with Filgotinib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Filgotinib.
Vemurafenib The serum concentration of Vemurafenib can be increased when it is combined with Filgotinib.
Carfilzomib The serum concentration of Carfilzomib can be increased when it is combined with Filgotinib.
Dabrafenib The serum concentration of Dabrafenib can be increased when it is combined with Filgotinib.
Ceritinib The serum concentration of Ceritinib can be increased when it is combined with Filgotinib.
Venetoclax The serum concentration of Venetoclax can be increased when it is combined with Filgotinib.
Vinflunine The serum concentration of Vinflunine can be increased when it is combined with Filgotinib.
Talazoparib The serum concentration of Talazoparib can be increased when it is combined with Filgotinib.

Target Protein

Tyrosine-protein kinase JAK1 JAK1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29461286
    Mahajan TD, Mikuls TR: Recent advances in the treatment of rheumatoid arthritis. Curr Opin Rheumatol. 2018 May;30(3):231-237. doi: 10.1097/BOR.0000000000000496.
  • PMID: 31912462
    Tarrant JM, Galien R, Li W, Goyal L, Pan Y, Hawtin R, Zhang W, Van der Aa A, Taylor PC: Filgotinib, a JAK1 Inhibitor, Modulates Disease-Related Biomarkers in Rheumatoid Arthritis: Results from Two Randomized, Controlled Phase 2b Trials. Rheumatol Ther. 2020 Mar;7(1):173-190. doi: 10.1007/s40744-019-00192-5. Epub 2020 Jan 7.
  • PMID: 31692920
    Biggioggero M, Becciolini A, Crotti C, Agape E, Favalli EG: Upadacitinib and filgotinib: the role of JAK1 selective inhibition in the treatment of rheumatoid arthritis. Drugs Context. 2019 Oct 24;8:212595. doi: 10.7573/dic.212595. eCollection 2019.
  • PMID: 22150658
    Wasserman AM: Diagnosis and management of rheumatoid arthritis. Am Fam Physician. 2011 Dec 1;84(11):1245-52.
  • PMID: 29736302
    Guo Q, Wang Y, Xu D, Nossent J, Pavlos NJ, Xu J: Rheumatoid arthritis: pathological mechanisms and modern pharmacologic therapies. Bone Res. 2018 Apr 27;6:15. doi: 10.1038/s41413-018-0016-9. eCollection 2018.
  • PMID: 29942363
    Malemud CJ: The role of the JAK/STAT signal pathway in rheumatoid arthritis. Ther Adv Musculoskelet Dis. 2018 Jun;10(5-6):117-127. doi: 10.1177/1759720X18776224. Epub 2018 May 19.
  • PMID: 28441353
    Araki Y, Mimura T: Matrix Metalloproteinase Gene Activation Resulting from Disordred Epigenetic Mechanisms in Rheumatoid Arthritis. Int J Mol Sci. 2017 Apr 25;18(5). pii: ijms18050905. doi: 10.3390/ijms18050905.
  • PMID: 26482170
    Namour F: Author's Reply to Srinivas: "Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection". Clin Pharmacokinet. 2015 Dec;54(12):1297-8. doi: 10.1007/s40262-015-0336-5.
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