Shangjie Tofacitinib Citrate Sustained-release Tablets

1. Indications and Usage
Tofacitinib citrate sustained-release tablets are indicated for the treatment of moderately to severely active rheumatoid arthritis (RA), active psoriatic arthritis (PsA), and moderately to severely active ankylosing spondylitis (AS).
2. Dosage and Administration
Recommended Dosage: The recommended dosage is 11 mg taken orally once daily.
Administration: Tablets must be swallowed whole and must not be crushed, chewed, or split. They may be taken with or without food.
Dose Adjustments: The dosage must be reduced to 5 mg once daily if co-administered with strong CYP3A4 inhibitors (e.g., ketoconazole) or with moderate CYP3A4 and strong CYP2C19 inhibitors.
3. Mechanism of Action
Tofacitinib is a small molecule Janus kinase (JAK) inhibitor. It selectively inhibits JAK1 and JAK3, which are involved in the signaling pathways of various cytokines. This inhibition suppresses the immune response and reduces inflammation associated with autoimmune diseases.
4. Safety and Warnings
Serious Infections: Patients are at increased risk for serious infections requiring hospitalization or leading to death, including tuberculosis, invasive fungal infections, and viral infections.
Malignancy and Lymphoproliferation: An increased risk of malignancy, including lymphoma and lung cancer, has been observed.
Thrombosis: Serious and sometimes fatal venous thromboembolism (VTE), including deep vein thrombosis and pulmonary embolism, may occur.
Gastrointestinal Perforation: Serious GI perforations have been reported.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: The most common adverse reactions include upper respiratory tract infections, nasopharyngitis, headache, and diarrhea.
Clinical Research: Efficacy and safety were established in multiple pivotal Phase 3 clinical trials (e.g., ORAL Scan, PEARL) demonstrating significant improvements in disease activity scores compared to placebo.
6. Drug Interactions
Strong CYP3A4 Inhibitors: Co-administration requires a dosage reduction to 5 mg once daily.
Moderate CYP3A4 and Strong CYP2C19 Inhibitors: Co-administration requires a dosage reduction to 5 mg once daily.
Immunosuppressants: Concomitant use with biologic DMARDs or potent immunosuppressants (e.g., azathioprine, cyclosporine) is not recommended due to increased risk of infection.
7. Pharmaceutical Information
Composition: The active ingredient is tofacitinib citrate.
Appearance: Pink oval-shaped film-coated sustained-release tablets.
Storage: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F). Keep in the original container to protect from moisture.