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Ruxolitinib is a kinase inhibitor that works by selectively inhibiting the Janus-related kinases JAK1 and JAK2. The JAK signaling pathway is involved in regulating the signal transduction of a variety of cytokines and growth factors, which are crucial for hematopoiesis and immune regulation.
1. Common name: Ruxolitinib (Ruxolitinib)
2. Trade name: Jakafi®
3. English name: Ru xolitinib Tablets
Ruxolitinib is suitable for the treatment of patients with intermediate-risk or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis¹.
This product is an oral tablet, available in 2 specifications: 5mg and 20mg.
Each ruxolitinib tablet contains ruxolitinib phosphate, which is equivalent to the specified dose of ruxolitinib free base. Excipients include: microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silica, hydroxypropyl cellulose, etc.
1. The recommended starting dose is determined according to the platelet count:
Platelet count >200×10⁹/L: 20mg, twice a day;
Platelet count 100–200×10⁹/L: 15mg, twice a day.
2. Blood routine should be monitored regularly during treatment, and the dose should be adjusted according to efficacy and tolerance. The maximum dose should not exceed 25 mg twice a day.
1. When platelets decrease, the dose needs to be adjusted or the medication is suspended, which is determined based on the platelet count and current dose;
2. If the efficacy is insufficient and the blood cell count allows, 5 mg can be increased every 2 weeks, up to a maximum of 25 mg daily. Twice;
3. When combined with strong CYP3A4 inhibitors, the starting dose should be reduced to 10 mg twice a day;
4. For patients with moderate to severe renal or liver dysfunction, if the platelet count is 100–150×10⁹/L, the starting dose should be 10 mg twice a day.
1. It can be taken with food or on an empty stomach;
2. If you miss a dose, you should not make up for it and take the next dose according to the original plan;
3. If you need to stop the medication (not due to thrombocytopenia) , it is recommended to gradually reduce the dose, for example, 5 mg twice a day per week;
4. If the tablet cannot be swallowed, it can be administered through a nasogastric tube: add one tablet to 40 mL of water and stir for 10 minutes, inject through the nasogastric tube within 6 hours, and flush the tube with 75 mL of water.
1. Renal insufficiency:For moderate to severe patients (CrCl15–59mL/min), the recommended starting dose is 10 mg twice a day; avoid use in non-dialysis patients with end-stage renal disease (CrCl<15mL/min);
2. Hepatic insufficiency:Any degree of liver damage and platelet count For those with a count of 100–150 × 10⁹/L, the starting dose is 10 mg twice daily;
3. Pregnancy: Only used when the benefits to the mother outweigh the risks to the fetus;
4. Lactation: It is recommended to discontinue the drug or stop breastfeeding;
5. Children and the elderly: The safety and effectiveness have not been clear or are similar to those in adults.
1. Common hematological adverse reactions:Including thrombocytopenia (69.7%), anemia (96.1%) and neutrophils Cytopenia (18.7%);
2. Non-hematological adverse reactions:Including bruises (23.2%), dizziness (18.1%) and headache (14.8%)⁶.¹. Serious infections and shingles have also been reported.
No clear contraindications.
1. Dosage adjustment is required when combined with strong CYP3A4 inhibitors (such as ketoconazole, clarithromycin, etc.);
2. Dosage adjustment is not required when combined with moderate and weak CYP3A4 inhibitors or inducers, but close monitoring is required.
Store at room temperature 20°C–25°C (68°F–77°F), permitted brief storage at 15°C–30°C (59°F–86°F).