Jakavi 5 mg (Ruxolitinib Phosphate)

Adult dose

Treatment with this medicine should be initiated by a physician experienced in administering anticancer agents. This medicine is taken orally and may be taken with or without food. If a dose is missed, the patient should not take an additional dose and should take the next prescribed dose. Treatment with this medicine may be continued for myelofibrosis and polycythemia vera as long as the benefit-risk ratio remains positive. However, if the spleen size has not decreased or symptoms have not improved after 6 months of treatment, this medicine should be discontinued. In patients with graft-versus-host disease who respond to treatment, tapering the dose of this medicine may be considered after corticosteroids have been discontinued. It is recommended that the dose of this medicine be reduced by 50% every 2 months. If signs or symptoms of graft-versus-host disease recur during or after dose tapering, an increase in the dose should be considered. Myelofibrosis: The recommended initial dose of this medicine is based on the platelet count. 50,000∼100,000/mm3: 10mg twice daily 100,000∼200,000/mm3: 15mg twice daily >200,000/mm3: 20mg twice daily Polycythemia vera and graft-versus-host disease: 10mg twice daily The dose should be adjusted based on safety and efficacy. Myelofibrosis and polycythemia vera: If the response is considered inadequate and blood cell counts are adequate, the dose may be increased by up to 5mg twice daily at each increment. The maximum dose of this medicine is 25mg twice daily. The initial dose should be maintained for the first 4 weeks after starting treatment. Thereafter, the dose should not be increased more frequently than every 2 weeks. Treatment should be interrupted if the platelet count is less than 50,000/mm3 or the absolute neutrophil count is less than 500/mm3. When used to treat polycythemia vera, treatment should be interrupted if hemoglobin is less than 8 g/dL. When blood cell counts recover to at least these levels, treatment may be resumed at 5 mg twice daily, with careful monitoring of blood cell counts and gradual dose increases. In myelofibrosis, when the platelet count decreases as shown in the following table, dose reduction should be considered to prevent treatment interruption due to thrombocytopenia. Dose adjustment for decreased platelet count (25 mg twice daily): when the platelet count is at least 100,000/mm3 and less than 125,000/mm3, the new dose is 20 mg twice daily; when the platelet count is at least 75,000/mm3 and less than 100,000/mm3, the new dose is 10 mg twice daily; when the platelet count is at least 50,000/mm3 and less than 75,000/mm3, the new dose is 5 mg twice daily; when the platelet count is less than 50,000/mm3, interrupt treatment. Dose adjustment for decreased platelet count (20 mg twice daily): when the platelet count is at least 100,000/mm3 and less than 125,000/mm3, the new dose is 15 mg twice daily; when the platelet count is at least 75,000/mm3 and less than 100,000/mm3, the new dose is 10 mg twice daily; when the platelet count is at least 50,000/mm3 and less than 75,000/mm3, the new dose is 5 mg twice daily; when the platelet count is less than 50,000/mm3, interrupt treatment. Dose adjustment for decreased platelet count (15 mg twice daily): when the platelet count is at least 100,000/mm3 and less than 125,000/mm3, the new dose is 15 mg twice daily; when the platelet count is at least 75,000/mm3 and less than 100,000/mm3, the new dose is 10 mg twice daily; when the platelet count is at least 50,000/mm3 and less than 75,000/mm3, the new dose is 5 mg twice daily; when the platelet count is less than 50,000/mm3, interrupt treatment. Dose adjustment for decreased platelet count (10 mg twice daily): when the platelet count is at least 100,000/mm3 and less than 125,000/mm3, the new dose is 10 mg twice daily; when the platelet count is at least 75,000/mm3 and less than 100,000/mm3, the new dose is 10 mg twice daily; when the platelet count is at least 50,000/mm3 and less than 75,000/mm3, the new dose is 5 mg twice daily; when the platelet count is less than 50,000/mm3, interrupt treatment. Dose adjustment for decreased platelet count (5mg twice daily): when the platelet count is at least 100,000/mm3 and less than 125,000/mm3, the new dose is 5 mg twice daily; when the platelet count is at least 75,000/mm3 and less than 100,000/mm3, the new dose is 5 mg twice daily; when the platelet count is at least 50,000/mm3 and less than 75,000/mm3, the new dose is 5 mg twice daily; when the platelet count is less than 50,000/mm3, interrupt treatment. When used to treat polycythemia vera, dose reduction should be considered if hemoglobin decreases to less than 12 g/dL, and dose reduction is recommended if hemoglobin is less than 10 g/dL. Hemoglobin at least 12 g/dL and platelet count at least 100,000/mm3: No dose adjustment required Hemoglobin at least 10 g/dL and less than 12 g/dL and platelet count at least 75,000/mm3 and less than 100,000/mm3: Consider dose reduction to prevent treatment interruption due to anemia and thrombocytopenia Hemoglobin at least 8 g/dL and less than 10 g/dL or platelet count at least 50,000/mm3 and less than 75,000/mm3: Reduce the dose to 5mg twice daily; for patients already receiving 5mg twice daily, reduce the dose to 5mg once daily Hemoglobin less than 8 g/dL or platelet count less than 50,000/mm3: Interrupt treatment In patients with graft-versus-host disease, dose reduction and temporary interruption may be required if thrombocytopenia, neutropenia, or increased total bilirubin occurs despite standard supportive care, including growth factors, anti-infective therapy, and transfusions. A one-level dose reduction is recommended (reduce from 10 mg twice daily to 5mg twice daily or from 5mg twice daily to 5mg once daily). Treatment should be discontinued in patients who do not tolerate this medicine at a dose of 5mg once daily. Platelet count less than 20,000/mm3: Reduce the dose level of this medicine by one step. If the platelet count is at least 20,000/mm3 within 7 days, the dose may be increased to the original dose level; otherwise, maintain the reduced dose. Platelet count less than 15,000/mm3: Interrupt treatment with this medicine until the platelet count is at least 20,000/mm3, then resume treatment at a dose level one step lower. Absolute neutrophil count (ANC) at least 500/mm3 and less than 750/mm3: Reduce the dose level of this medicine by one step. Resume treatment at the original dose if the ANC exceeds 1,000/mm3. Absolute neutrophil count (ANC) less than 500/mm3: Interrupt treatment with this medicine until the ANC exceeds 500/mm3, then resume treatment at a dose level one step lower. Treatment may be resumed at the original dose if the ANC exceeds 1,000/mm3. Increased total bilirubin in patients without hepatic graft-versus-host disease Greater than 3.0 x ULN and up to 5.0 x ULN: Continue this medicine at a dose level one step lower until total bilirubin is at or below 3.0 x ULN. Greater than 5.0 x ULN and up to 10.0 x ULN: Interrupt treatment with this medicine for up to 14 days until total bilirubin is at or below 3.0 x ULN. If total bilirubin is at or below 3.0 x ULN, treatment may be resumed at the current dose. If it does not reach 3.0 x ULN or below after 14 days, resume treatment at a dose level one step lower. Greater than 10.0 x ULN: Interrupt treatment with this medicine until total bilirubin is at or below 3.0 x ULN, then resume treatment at a dose level one step lower. Increased total bilirubin in patients with hepatic graft-versus-host disease Greater than 3.0 x ULN: Continue this medicine at a dose level one step lower until total bilirubin is at or below 3.0 x ULN. When this medicine is coadministered with a strong CYP3A4 inhibitor in patients with myelofibrosis or polycythemia vera, or with a dual moderate inhibitor of CYP2C9 and CYP3A4 enzymes, such as fluconazole, in patients with myelofibrosis, polycythemia vera, or graft-versus-host disease, the total daily dose of this medicine should be reduced by approximately 50%. Adjust the dose by reducing the twice-daily dose or, if twice-daily dosing is not possible, by reducing the dosing frequency to an equivalent once-daily dose. When this medicine is coadministered with fluconazole, the dose of fluconazole should not exceed 200mg per day. In patients with moderate (creatinine clearance at least 30 mL/min and less than 50 mL/min) or severe renal impairment (creatinine clearance less than 30 mL/min), the recommended initial dose for myelofibrosis is 10mg twice daily. The recommended initial dose for polycythemia vera and graft-versus-host disease in patients with moderate or severe renal impairment is 5mg twice daily. There are limited data to determine the optimal dose for myelofibrosis in patients with end-stage renal disease (ESRD) requiring hemodialysis. Based on available findings in these patients, the recommended initial dose is a single dose of 15mg for patients with a platelet count of 100,000∼200,000/mm3 and a single dose of 20mg for patients with a platelet count exceeding 200,000/mm3. It should be administered only on the day of dialysis, after dialysis, and should not be administered more than once daily. The recommended initial dose for polycythemia vera and graft-versus-host disease in patients with ESRD requiring hemodialysis is a single dose of 10mg, administered only on the day of dialysis after dialysis. Safety and efficacy should be monitored carefully. In patients with hepatic impairment, the recommended initial dose for myelofibrosis should be reduced to 10mg twice daily, and the recommended initial dose for polycythemia vera should be reduced to 5mg twice daily. Subsequent doses should be adjusted with careful monitoring of safety and efficacy. No change to the initial dose is recommended for patients with graft-versus-host disease who have hepatic impairment, including hepatic graft-versus-host disease. In patients with hepatic involvement of graft-versus-host disease and total bilirubin levels exceeding 3 x ULN, toxicity and blood counts should be monitored more frequently, and a one-level dose reduction may be considered. No dose adjustment is required in elderly patients.

Child dose

In pediatric patients aged 12 years and older with graft-versus-host disease, the dose of this drug is the same as that for adults. The safety and efficacy of this drug have not been established in patients under 12 years. The safety and efficacy of this drug have not been established in pediatric patients with myelofibrosis and polycythemia vera.

This drug may reduce blood cell counts. Therefore, blood cell counts must be checked before using this medication, and treatment should be discontinued if platelet or neutrophil counts are too low. This drug should not be administered to patients with specific genetic disorders, such as lactose intolerance or glucose-galactose malabsorption. During the use of this drug, blood-related adverse reactions such as anemia, thrombocytopenia, and neutropenia may occur frequently. If these symptoms arise, it may be necessary to consult a physician for dose adjustment or discontinuation of therapy. As there may be an increased risk of infection, immediate treatment should be received if any infection symptoms occur, and infection status must be checked prior to treatment. This drug can cause liver dysfunction, so regular liver function tests should be performed, and caution is needed for patients who carry hepatitis viruses. It is recommended not to use this drug during pregnancy, and women of childbearing potential should use effective contraceptive methods while on medication. Women who are breastfeeding should consider interrupting breastfeeding or discontinuing the drug, as it may transfer into breast milk. This drug may interact with other medications; therefore, dose adjustment and caution are needed, especially when co-administered with drugs that inhibit or induce the CYP3A4 enzyme. In case of overdose, as there is no antidote, immediate medical assistance and appropriate supportive treatment are necessary. Store out of reach of children in a safe place, and avoid transferring to other containers.

• Anemia
• thrombocytopenia
• neutropenia
• bruising
• dizziness
• urinary tract infection
• ALT elevation
• AST elevation
• hypertriglyceridemia
• weight gain

This drug must be stored in a tightly closed container to protect it from air and moisture. It is important to maintain the storage temperature between 1 degree and 25 degrees at room temperature to adequately preserve the drug's efficacy.

Appearance

White to off-white round tablets

Package unit

56 tablets (14 tablets/PTP packaging x 4)