Overview
Baricitinib is a selective inhibitor of Janus kinase (JAK) enzymes, particularly JAK1 and JAK2, which play a critical role in inflammatory signaling pathways. Developed by Eli Lilly and Incyte, it was first approved by the FDA in 2018 for the treatment of moderate-to-severe rheumatoid arthritis. Its mechanism involves disrupting cytokine signaling, thereby reducing inflammation and immune system overactivity. Beyond rheumatoid arthritis, baricitinib has been investigated for other autoimmune conditions like alopecia areata and atopic dermatitis. During the COVID-19 pandemic, it gained emergency use authorization in some regions due to its potential to mitigate cytokine storms. The drug is typically administered orally in tablet form, with dosing adjusted based on patient response and tolerability.
Physical and Chemical Properties
Baricitinib is a small molecule with a molecular weight of 371.42 g/mol, classified as a pyrrolopyrimidine derivative. It appears as a white to off-white crystalline powder with limited water solubility but higher solubility in organic solvents like DMSO. The compound is stable under recommended storage conditions but should be protected from moisture and light to prevent degradation. Its chemical structure includes a sulfonamide group, which contributes to its binding affinity for JAK enzymes. The melting point ranges between 200-205°C, indicative of its crystalline nature. Analytical methods such as HPLC and mass spectrometry are commonly used to verify purity, which is critical for pharmaceutical applications.
Main Applications
The primary use of baricitinib is in the management of rheumatoid arthritis, especially in patients who have not responded adequately to conventional disease-modifying antirheumatic drugs (DMARDs). It is often prescribed as a monotherapy or in combination with methotrexate. Clinical trials have demonstrated its efficacy in reducing joint swelling, pain, and structural damage. In 2020, baricitinib was repurposed for COVID-19 treatment under emergency protocols due to its anti-inflammatory effects and potential antiviral properties (via disruption of viral entry). Off-label uses include treating alopecia areata and atopic dermatitis, though these applications require further validation. Research is ongoing to explore its utility in other autoimmune and inflammatory disorders.
Safety and Storage
Baricitinib carries a boxed warning for serious infections, thrombosis, and malignancies, necessitating careful patient monitoring. Common side effects include upper respiratory infections, nausea, and elevated cholesterol levels. It is contraindicated in patients with active tuberculosis or severe hepatic impairment. For storage, the drug should be kept in its original packaging at 2-8°C, avoiding exposure to humidity and direct sunlight. Bulk pharmaceutical ingredients require controlled environments with documented temperature logs. Handling precautions include the use of gloves and masks to minimize occupational exposure, particularly in powder form.
B2B Procurement Guide
Procuring baricitinib for pharmaceutical manufacturing demands strict adherence to regulatory standards. Buyers should prioritize suppliers with Good Manufacturing Practice (GMP) certification and auditable quality control systems. Key documentation includes certificates of analysis (CoA), stability studies, and compliance with pharmacopeial monographs (e.g., USP, EP). Pricing varies by order volume and purity grade, with bulk purchases (kilogram-scale) often yielding cost advantages. Lead times can extend to several weeks due to stringent testing requirements. Import/export regulations, such as FDA Form 483 or EMA inspections, must be verified for cross-border transactions. Alternative suppliers in India and China may offer competitive pricing but require rigorous due diligence.
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