非戈替尼(Filgotinib)100mg

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1. Composition:

 

   The main active ingredient of Filgotinib is not Goteinib. Its chemical name is N-(5-(4-((1-methylpiperidin-4-yl)oxy)phenyl)-3H-imidazo[1,2-b]pyridazin-6-yl)-1H-pyrazol-3-amine. The molecular formula is C21H23N5O2, and the molecular weight is 381.44. The drug is typically available in tablet form, with each tablet containing 100 mg of Filgotinib.

 

2. Pharmacodynamics:

   Filgotinib works by inhibiting the activity of Janus kinase 1 (JAK1), disrupting the JAK-STAT signaling pathway, regulating immune cell activity, and reducing the production of inflammatory mediators, thereby relieving symptoms associated with rheumatoid arthritis and other autoimmune diseases. Compared to non-selective JAK inhibitors, Filgotinib is more selective, which can reduce the risk of side effects.

 

3. Usage:

   The recommended dosage of Filgotinib is 100 mg or 200 mg taken orally once daily. The specific dosage is determined by the doctor based on the patient's condition, weight, and response to the medication. It can be taken with or without food. A comprehensive health assessment, particularly for infection risk and liver and kidney function, should be conducted before using Filgotinib.

 

4. Research & Development History:

 

   Filgotinib was developed in collaboration between the Belgian pharmaceutical company Galapagos and Gilead Sciences, initially for the treatment of rheumatoid arthritis. In 2020, the European Medicines Agency (EMA) approved Filgotinib for the treatment of moderate to severe active rheumatoid arthritis. It is an innovative drug targeting the JAK pathway, following Tofacitinib and Baricitinib.

 

5. Mechanism of Action:

   Filgotinib is a highly selective JAK1 inhibitor. JAK1 plays an important role in the signal transduction of various cytokines, which are often involved in the pathological processes of autoimmune diseases. Once JAK1 is activated, it initiates the STAT (Signal Transducer and Activator of Transcription) protein pathway, promoting the expression of inflammatory genes. Filgotinib blocks JAK1 signaling, reducing the production of inflammatory factors and the overactivation of immune responses, thereby controlling inflammation and relieving symptoms.

 

6. Summary:

   Filgotinib is a novel selective JAK1 inhibitor used to treat rheumatoid arthritis and other autoimmune diseases. By inhibiting the JAK1 signaling pathway, it reduces inflammatory responses, helping patients alleviate pain and joint damage. Compared to other JAK inhibitors, Filgotinib’s higher selectivity may reduce broad immunosuppression and associated side effects.