filgotinib   Click here for help

GtoPdb Ligand ID: 7913

Synonyms: GLPG-0634 | GLPG0634 | Jyseleca®
Approved drug PDB Ligand Immunopharmacology Ligand
filgotinib is an approved drug (EMA (2020))
Compound class: Synthetic organic
Comment: Filgotinib is a selective and orally acive JAK1 inhibitor [3]. It is being developed in a collaboration between Gilead Sciences and Galapagos for the treatment of inflammatory indications including psoriatic arthritis, ankylosing spondylitis, Crohn's disease, ulcerative colitis and rheumatoid arthritis. It is proposed as a once daily drug, that is predicted to cause fewer toxicity issues and adverse effects than existing JAK1 inhibitors.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 1
Rotatable bonds 6
Topological polar surface area 105.05
Molecular weight 425.15
XLogP 1.99
No. Lipinski's rules broken 0
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Canonical SMILES O=C(C1CC1)Nc1nc2n(n1)c(ccc2)c1ccc(cc1)CN1CCS(=O)(=O)CC1
Isomeric SMILES O=C(C1CC1)Nc1nc2n(n1)c(ccc2)c1ccc(cc1)CN1CCS(=O)(=O)CC1
InChI InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)
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Summary of Clinical Use Click here for help
Filgotinib was advanced to evaluation in patients with rheumatoid arthritis, Crohn's disease and ulcerative colitis. Click here to link to's complete listing of filgotinib studies. In October 2019 Gliead Sciences and Galapagos issued a press release which announced sustained efficacy, safety and tolerability of filgotinib from 12-52 weeks in RA patients in the Phase 3 FINCH1 (NCT02889796) & FINCH3 (NCT02886728) trials [2].

In August 2020, Gilead announed that the FDA had rejected their filing for approval of filgotinib in RA in a complete response letter, that expressed concerns about toxicity (on sperm concentrations) of the 200mg dose. The FDA want to review results from the ongoing MANTA and MANTA-RAy trials that are expected in the first half of 2021. However, late September 2020 saw EMA and Japanese PMDA approvals granted to filgotinib for the treatment of moderate to severe RA.
Publication of results from ulcerative colitis trials is pending, although positive indications (particulary in relation to response rates and safety) were presented at the United European Gastroenterology Week virtual meeting (October 11-13, 2020).
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02886728 Filgotinib Alone and in Combination With Methotrexate (MTX) in Adults With Moderately to Severely Active Rheumatoid Arthritis Who Are Naive to MTX Therapy Phase 3 Interventional Gilead Sciences
NCT02889796 Filgotinib in Combination With Methotrexate in Adults With Moderately to Severely Active Rheumatoid Arthritis Who Have an Inadequate Response to Methotrexate Phase 3 Interventional Gilead Sciences