描述
Tofacitinib citrate is a small-molecule Janus kinase (JAK) inhibitor that blocks signaling downstream of cytokines, lessening inflammatory responses by suppressing JAK1/JAK3 pathways. The 11?mg once-daily sustained-release form achieves exposure equivalent to twice-daily immediate-release dosing. Clinically approved for rheumatoid arthritis, ulcerative colitis, psoriatic arthritis, and ankylosing spondylitis, it is widely applied in research models to study JAK?STAT-mediated inflammation, immune modulation, and pharmacokinetics of sustained-release formulations. For laboratory research use only.
Product Specifications
Parameter | Detail |
---|---|
Product Name | Xeljanz® (Tofacitinib?Citrate SR Tablets) |
Synonyms | Tofacitinib citrate extended-release; JAK inhibitor |
Strength & Packaging | 11?mg per tablet, 30 tablets per bottle |
Dosage Form | Extended-release oral tablets |
Manufacturer | Pfizer Pharmaceuticals LLC (USA) |
Approval Number | HJ20210071 |
Drug Standard Code | 86978718001568 |
Barcode | Not yet assigned |
CAS Number | 477600?75?2 |
Molecular Formula | C??H??N?O·C?H?O? (tofacitinib citrate) |
Molecular Weight | ~504.5?Da (citrate salt) |
Mechanism of Action & Research Applications
Tofacitinib inhibits JAK1 and JAK3 enzymes, disrupting STAT-mediated cytokine signaling cascades crucial in autoimmune inflammation. The sustained-release tablet provides stable pharmacokinetics with once-daily dosing. Common research applications include modeling rheumatoid arthritis, ulcerative colitis, JAK-STAT pathway modulation, and dose-response pharmacodynamic studies.
Side Effects (For Reference Only in Research Models)
Reported side effects from clinical analogs include diarrhea, headache, hypertension, serious infections (e.g., TB, fungal, viral), increased risk of malignancies and thromboembolic events. These inform safety monitoring and dose-adjustment protocols in experimental designs.
Disclaimer
Xeljanz® (Tofacitinib?Citrate SR Tablets) is strictly intended for laboratory research use only. Not for human or veterinary therapeutic, diagnostic, or prophylactic use.
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