Filgotinib maleateProduct ingredient for Filgotinib

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.^4,5 The disease is associated with extra-articular manifestations, progressive disability, and comorbidities including cardiovascular disease and mental disorders.³ 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.³ New therapeutic developments target other inflammatory pathways implicated in RA including the Janus kinase (JAK) signaling pathway as seen with filgotinib.⁵

There are four JAK subtypes which include JAK1, JAK2, JAK3, and tyrosine kinase 2.³ 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.³ 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.³ 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.¹⁰

ChemSpider

64853733

ChEMBL

CHEMBL4298167

Wikipedia

Filgotinib