Lukotinib is a kinase inhibitor that works by selectively inhibiting Janus associated kinases JAK1 and JAK2. The JAK signaling pathway is involved in regulating the signal transduction of various cytokines and growth factors, which are crucial for hematopoietic function and immune regulation.

1、 Drug name

1. Common name: Ruxolitinib

2. Product Name: Jakafi ®

3. English name: Ruxolitinib Tablets

2、 Indications

Lukotinib is suitable for the treatment of patients with moderate to high-risk bone marrow fibrosis, including primary bone marrow fibrosis, post polycythemia vera bone marrow fibrosis, and post thrombocytopenia bone marrow fibrosis.

3、 Specifications and characteristics

This product is an oral tablet with two specifications: 5mg and 20mg.

4、 Main components

Each tablet of fluconazole contains fluconazole phosphate, which is equivalent to the specified dose of fluconazole free base. Accessories include microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silica, hydroxypropyl cellulose, etc.

5、 Usage and dosage

1. The recommended starting dose is determined based on platelet count:

Platelet count>200 × 10 ⁹/L: 20mg, twice daily;

Platelet count 100-200 × 10 ⁹/L: 15mg, twice daily.

2. During the treatment period, regular monitoring of blood routine should be conducted, and the dosage should be adjusted according to the efficacy and tolerability. The maximum dosage should not exceed 25mg twice a day.

6、 Dose adjustment

1. When platelet count decreases, the dosage needs to be adjusted or the medication needs to be suspended, depending on the platelet count and current dosage;

2. If the therapeutic effect is insufficient and the blood cell count allows, an increase of 5mg can be made every 2 weeks, up to a maximum of 25mg twice a day;

3. When using potent CYP3A4 inhibitors in combination, the initial dose should be reduced to 10mg twice daily;

4. For patients with moderate to severe renal or liver dysfunction, if the platelet count is between 100-150 × 10 ⁹/L, the starting dose is 10mg twice daily.

7、 Medication precautions

1. Can be taken with food or on an empty stomach;

2. If missed, the next dose should not be taken as planned;

3. If the medication needs to be discontinued (not due to thrombocytopenia), it is recommended to gradually reduce the dosage, such as reducing 5mg twice a day per week;

4. If it is not possible to swallow the tablet, it can be administered through a nasogastric tube: add one tablet to 40mL of water and stir for 10 minutes, inject through a nasogastric tube within 6 hours, and rinse the tube with 75mL of water.

8、 Medication for special populations

1. Renal insufficiency: For moderate to severe cases (CrCl15-59mL/min), it is recommended to start with a dose of 10mg twice a day; Non dialysis patients with end-stage renal disease (CrCl<15mL/min) should avoid using it;

2. Liver dysfunction: For patients with any degree of liver damage and platelet count between 100-150 × 10 ⁹/L, the initial dose is 10mg twice a day;

3. Pregnancy: Use only when the benefits to the mother outweigh the risks to the fetus;

4. Breastfeeding period: It is recommended to stop taking medication or breastfeeding;

5. Children and elderly: Safety and efficacy are not yet clear or comparable to adults.

9、 Adverse reactions

1. Common hematological adverse reactions include thrombocytopenia (69.7%), anemia (96.1%), and neutropenia (18.7%);

2. Non hematological adverse reactions: including bruising (23.2%), dizziness (18.1%), and headache (14.8%) Severe infections and shingles have also been reported.

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. Dosage adjustment is required when combined with potent CYP3A4 inhibitors such as ketoconazole and clarithromycin;

2. When used in combination with moderate to weak acting CYP3A4 inhibitors or inducers, there is no need to adjust the dosage, but close monitoring is required.

12、 Storage method

Store at room temperature of 20 ° C-25 ° C (68 ° F-77 ° F) and allow for brief storage within the range of 15 ° C-30 ° C (59 ° F-86 ° F).

Ruxolitinibinformation