Tofacitinib citrate
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Category：Active Pharmaceutical Ingredients Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
English Synonyms 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile 2-hydroxypropane-1,2,3-tricarboxylate
Catalog ID99824
CAS NO.540737-29-9
Purity 98%
MDL NumberMFCD11616529
EINEC Molecular FormulaC16H20N6O.C6H8O7
Molecular Weight 504.497
| Category | Content |
|---|---|
| Generic Name | Tofacitinib Citrate |
| Brand Name | Xeljanz, Xeljanz XR |
| Drug Class | Janus Kinase (JAK) Inhibitor |
| Mechanism of Action | Tofacitinib is a selective JAK inhibitor that blocks the JAK-STAT signaling pathway, which is involved in the production of pro-inflammatory cytokines. By inhibiting JAKs, it reduces the inflammatory response in conditions like rheumatoid arthritis. |
| Indications | – Treatment of moderate to severe active rheumatoid arthritis (RA) in adults who have not responded to methotrexate.<br>- Also approved for psoriatic arthritis, ankylosing spondylitis, and ulcerative colitis. |
| Dosage Forms | Tablets (5 mg, 10 mg, 11 mg, 22 mg) and oral solution. |
| Pharmacokinetics | – Oral absorption: 74% bioavailability.<br>- Peak plasma concentration: 0.5-1 hour.<br>- Elimination: 70% hepatic metabolism (mainly by CYP3A4), 30% renal excretion.<br>- Half-life: Approximately 3 hours. |
| Side Effects | Common: Headaches, diarrhea, nausea, nasopharyngitis, upper respiratory tract infections.<br> Serious: Increased risk of infections, lymphopenia, neutropenia, anemia, and malignancies. |
| Precautions | – Screen for latent tuberculosis before starting treatment.<br>- Monitor for signs of infection and blood abnormalities.<br>- Avoid in patients with active infections. |
| Storage | Store at room temperature, protect from moisture. |
| Developer | Pfizer |
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