Filgotinib maleate
[CAS# 1802998-75-9]

Identification

• Classification: Pharmaceutical intermediate >> API intermediate
• Name: Filgotinib maleate
• Synonyms: (Z)-but-2-enedioic acid;N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
• Molecular Formula: C₂₅H₂₇N₅O₇S
• Molecular Weight: 541.58
• CAS Registry Number: 1802998-75-9
• EC Number: 848-707-0
• SMILES: C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5.C(=C\C(=O)O)\C(=O)O

Safety Data

• Hazard Symbols: GHS08 Danger
• Hazard Statements: H360-H373
• Precautionary Statements: P203-P260-P280-P318-P319-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Specific target organ toxicity - repeated exposure	STOT RE	2	H373
Reproductive toxicity	Repr.	1B	H360

Discovory and Applicatios

Filgotinib maleate is a pharmaceutical compound classified as a selective Janus kinase 1 (JAK1) inhibitor. It is widely recognized for its application in treating inflammatory diseases such as rheumatoid arthritis, ulcerative colitis, and Crohn's disease. The development of JAK inhibitors like filgotinib has revolutionized treatment approaches for autoimmune disorders by targeting the underlying immune responses, reducing inflammation, and alleviating symptoms more effectively than conventional therapies.

The discovery of filgotinib maleate stemmed from extensive research into the role of JAK enzymes in immune signaling pathways. JAK enzymes, specifically JAK1, JAK2, JAK3, and TYK2, are critical mediators of cytokine signaling, which regulates immune responses. Abnormal activation of JAK pathways is implicated in autoimmune diseases, where the immune system attacks healthy tissues, causing chronic inflammation and damage. Filgotinib, designed to selectively inhibit JAK1, limits the activity of cytokines responsible for promoting inflammation while minimizing the risk of inhibiting other JAK enzymes that may lead to adverse effects.

Filgotinib maleate is the salt form of filgotinib, enhancing its solubility and stability for clinical use. The drug development process included extensive clinical trials to evaluate its efficacy and safety in treating autoimmune conditions. Studies demonstrated that filgotinib effectively reduced disease activity in patients with moderate to severe rheumatoid arthritis and other inflammatory conditions. The ability of the drug to selectively target JAK1 while sparing JAK2 and JAK3 has been associated with a favorable safety profile compared to other JAK inhibitors.

In clinical practice, filgotinib maleate is administered orally, offering a convenient alternative to injectable biologics that are commonly used in autoimmune disease management. Its mechanism of action involves blocking the phosphorylation of STAT proteins, which are activated by cytokine signaling via JAK1. This disruption in the signaling cascade reduces inflammation and immune cell activity, ultimately providing relief to patients with autoimmune diseases. Filgotinib's selective action also reduces the likelihood of side effects related to the inhibition of JAK2 and JAK3, such as anemia or immune suppression, which are seen with less selective JAK inhibitors.

The pharmaceutical industry has embraced filgotinib maleate as a critical component of combination therapies for autoimmune diseases. It is often used alongside disease-modifying antirheumatic drugs (DMARDs) such as methotrexate, which further enhances its therapeutic efficacy. The success of filgotinib and other JAK inhibitors highlights the potential of targeted therapies in transforming the treatment landscape for chronic inflammatory conditions, offering patients more personalized and effective treatment options.

Filgotinib maleate has opened new avenues in the field of immunology and pharmacology. Ongoing research continues to explore its use in other inflammatory disorders and potential long-term benefits for patients with autoimmune diseases. The introduction of JAK inhibitors like filgotinib reflects the growing trend towards targeted therapies that address the root causes of diseases, providing new hope for individuals affected by chronic inflammatory conditions.