filgotinib   

GtoPdb Ligand ID: 7913

Synonyms: GLPG-0634 | GLPG0634
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.
2D Structure
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Physico-chemical Properties
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
SMILES / InChI / InChIKey
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)
InChI Key RIJLVEAXPNLDTC-UHFFFAOYSA-N
No information available.
Summary of Clinical Use
Filgotinib has advanced to Phase 3 evaluation in patients with rheumatoid arthritis, Crohn's disease and ulcerative colitis. Click here to link to ClinicalTrials.gov'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.
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