Filgotinib

Le filgotinib est une molécule inhibitrice spécifique de la janus kinase 1 et en cours de test comme médicament.

Il a une affinité trente fois supérieure pour la janus kinase 1 par rapport à celle pour la janus kinase 2^[1]

Après absorption orale, il se transforme en un métabolite actif dont la demi-vie est d'un peu moins de 24 h^[2].

Dans la polyarthrite rhumatoïde et en association avec le méthotrexate, il permet une amélioration des symptômes de la maladie^[3]. Dans les formes résistantes de la maladie, il conserve une activité^[4].

Il a des résultats prometteurs dans la maladie de Crohn^[5] et dans la rectocolite hémorragique^[6].

Le tofacitinib et le baricitinib sont deux autres inhibiteurs des janus kinases

[1]
Van Rompaey L, Galien R, van der Aar EM et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases, J Immunol, 2013;191:3568–3577
[2]
Namour F, Diderichsen PM, Cox E et al. Pharmacokinetics and pharmacokinetic/pharmacodynamic modeling of filgotinib (GLPG0634), a selective JAK1 inhibitor, in support of phase IIB dose selection, Clin Pharmacokinet, 2015;54:859–874
[3]
Genovese M, Westhovens R, Kavanaugh AF et al. The effect of filgotinib (GLPG0634, GS-6034), an oral JAK1 selective inhibitor on patient-reported outcomes: results from two 24-week phase 2B dose ranging studies, Ann Rheum Dis, 2016;75:244
[4]
Genovese MC, Kalunian K, Gottenberg J-E et al. Effect of filgotinib vs placebo on clinical response in patients with moderate to severe rheumatoid arthritis refractory to disease-modifying antirheumatic drug therapy: the FINCH 2 randomized clinical trial, JAMA, 2019;322:315-325
[5]
Vermeire, S, Schreiber, S, Petryka, R et al. Clinical remission in patients with moderate-to-severe Crohn's disease treated with filgotinib (the FITZROY study): results from a phase 2, double-blind, randomised, placebo-controlled trial, Lancet, 2017;389:266–275
[6]
Gilead and Galapagos Announce Positive Topline Results of Phase 2b/3 Trial of Filgotinib in Moderately to Severely Active Ulcerative Colitis May 20, 2020 at 4:03 PM EDT http://investors.gilead.com/news-releases/news-release-details/gilead-and-galapagos-announce-positive-topline-results-phase-2b3

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[Van_Rompaey_2013-1] [1]
Van Rompaey L, Galien R, van der Aar EM et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases, J Immunol, 2013;191:3568–3577

[Namour_2015-2] [2]
Namour F, Diderichsen PM, Cox E et al. Pharmacokinetics and pharmacokinetic/pharmacodynamic modeling of filgotinib (GLPG0634), a selective JAK1 inhibitor, in support of phase IIB dose selection, Clin Pharmacokinet, 2015;54:859–874

[Genovese_2016-3] [3]
Genovese M, Westhovens R, Kavanaugh AF et al. The effect of filgotinib (GLPG0634, GS-6034), an oral JAK1 selective inhibitor on patient-reported outcomes: results from two 24-week phase 2B dose ranging studies, Ann Rheum Dis, 2016;75:244

[Genovese_2019-4] [4]
Genovese MC, Kalunian K, Gottenberg J-E et al. Effect of filgotinib vs placebo on clinical response in patients with moderate to severe rheumatoid arthritis refractory to disease-modifying antirheumatic drug therapy: the FINCH 2 randomized clinical trial, JAMA, 2019;322:315-325

[Vermeire_2017-5] [5]
Vermeire, S, Schreiber, S, Petryka, R et al. Clinical remission in patients with moderate-to-severe Crohn's disease treated with filgotinib (the FITZROY study): results from a phase 2, double-blind, randomised, placebo-controlled trial, Lancet, 2017;389:266–275

[6] [6]
Gilead and Galapagos Announce Positive Topline Results of Phase 2b/3 Trial of Filgotinib in Moderately to Severely Active Ulcerative Colitis May 20, 2020 at 4:03 PM EDT http://investors.gilead.com/news-releases/news-release-details/gilead-and-galapagos-announce-positive-topline-results-phase-2b3

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Filgotinib

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Filgotinib

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Mode d'action

Pharmacocinétique

Efficacité

Voir aussi

Notes et références