Tavalisse Tablets 100mg (Fostamatinib Disodium Hydrate)

Adult dose

This medicine should be initiated and supervised by a physician with sufficient experience in the treatment of blood disorders. The recommended starting dose is 100mg twice daily as fostamatinib. This medicine is administered orally, regardless of meals. If the platelet count does not increase to 50x109/L(50,000/μL) or more after administration of the recommended starting dose for at least 4 weeks, increase the dose to 150mg twice daily. To reduce the risk of bleeding, administer the lowest dose that can achieve and maintain a platelet count of at least 50x109/L(50,000/μL). The maximum dose of this medicine is 150mg twice daily. If a dose of this medicine is missed, instruct the patient to take the prescribed dose at the next scheduled dosing time. Daily dose 300mg/day: 150mg in the morning, 150mg in the afternoon 200mg/day: 100mg in the morning, 100mg in the afternoon 150mg/day: 150mga) in the morning, - in the afternoon 100mg/dayb): 100mga) in the morning, - in the afternoon a) If administered once daily, administer in the morning. b) If it is necessary to reduce the dose to less than 100mg/day, discontinue this medicine. If hypertension, hepatic impairment, neutropenia, or diarrhea occurs during treatment with this medicine, adjust treatment with reference to the criteria below. Systolic blood pressure 130 – 139mmHg or diastolic blood pressure 80– 89mmHg: In patients at high cardiovascular risk, initiate antihypertensive treatment or increase the dose, and adjust as needed until blood pressure is controlled. Measure blood pressure periodically. If blood pressure is not controlled after 8 weeks despite appropriate treatment, reduce the daily dose of this medicine by 1 dose level, with reference to Table 1. Systolic blood pressure 140mmHg or higher or diastolic blood pressure 90mmHg or higher: Initiate antihypertensive treatment or increase the dose, and adjust as needed until blood pressure is controlled. Measure blood pressure periodically. If blood pressure remains at 140/90mmHg or higher after 8 weeks despite appropriate treatment, reduce the daily dose of this medicine by 1 dose level, with reference to Table 1. If blood pressure is 160/100mmHg or higher after 1 week despite intensive antihypertensive treatment, temporarily or permanently discontinue this medicine. Hypertensive crisis: systolic blood pressure 180mmHg or higher or diastolic blood pressure 120mmHg or higher: Temporarily or permanently discontinue this medicine. Initiate antihypertensive treatment or increase the dose, and adjust as needed until blood pressure is controlled. If blood pressure decreases to below the target, resume this medicine at the same daily dose. If blood pressure is 160/100mmHg or higher after 1 week despite intensive antihypertensive treatment, discontinue this medicine. AST or ALT is at least 3 times and less than 5 times the upper limit of normal (ULN), and the patient has symptoms (e.g., nausea, vomiting, abdominal pain): Temporarily discontinue this medicine. Perform liver function tests every 72 hours until ALT and AST levels are no longer elevated (less than 1.5 x ULN) and total bilirubin is less than 2 x ULN. Resume this medicine at a daily dose reduced by 1 dose level, with reference to Table 1. AST or ALT is at least 3 times and less than 5 times the upper limit of normal (ULN), and the patient is asymptomatic: Perform liver function tests every 72 hours until ALT and AST levels are less than 1.5 x ULN and total bilirubin is less than 2 x ULN. If AST or ALT and total bilirubin levels remain in this category (AST/ALT 3 – 5 x ULN, total bilirubin less than 2 x ULN), temporarily discontinue this medicine or reduce the dose. If this medicine was temporarily discontinued, resume it at a daily dose reduced by 1 dose level, with reference to Table 1, when AST, ALT, and total bilirubin levels have recovered (less than 1.5 x ULN) and total bilirubin remains less than 2 x ULN. AST or ALT is at least 5 times the upper limit of normal and total bilirubin is less than 2 times the upper limit of normal: Temporarily discontinue this medicine. Perform liver function tests every 72 hours. Continue liver function tests until AST and ALT levels have recovered (less than 1.5 x ULN) and total bilirubin remains less than 2 x ULN; when AST and ALT decrease, resume this medicine at a daily dose reduced by 1 dose level, with reference to Table 1. Discontinue this medicine if AST or ALT remains at least 5 x ULN for more than 2 weeks. AST or ALT is at least 3 times the upper limit of normal and total bilirubin is greater than 2 times the upper limit of normal: Discontinue this medicine. Increased unconjugated (indirect) bilirubin without abnormalities in other liver function tests: An isolated increase in unconjugated (indirect) bilirubin is due to UGT1A1 inhibition; continue treatment with this medicine with frequent monitoring. If diarrhea occurs, immediately initiate symptomatic treatment (e.g., dietary changes, hydration, antidiarrheal agents) until symptoms resolve. If symptoms are severe (Grade 3a) or higher), temporarily discontinue this medicine. When symptoms improve to mild (Grade 1), resume this medicine at a daily dose reduced by 1 dose level, with reference to Table 1. If the absolute neutrophil count decreases (less than 1.0 x 109/L) and remains decreased for 72 hours, temporarily discontinue this medicine until the neutrophil count recovers (greater than 1.5 x 109/L). If the neutrophil count has recovered (greater than 1.5 x 109/L), resume this medicine at a daily dose reduced by 1 dose level, with reference to Table 1. a) Grade is based on CTCAE ver 5.0. If the platelet count does not increase enough to prevent clinically significant bleeding despite 12 weeks of treatment with this medicine, discontinue this medicine. No dose adjustment of this medicine is necessary in patients with renal impairment. In patients with severe hepatic impairment (Child-Pugh class C), the blood concentration of unbound R406, the major active metabolite of this medicine, may increase; therefore, carefully determine whether to administer this medicine. If treatment is necessary, consider reducing the initial dose and administer cautiously while closely monitoring the patient's condition. In patients with mild or moderate hepatic impairment (Child-Pugh class A and B), monitor liver function during treatment with this medicine. Dose adjustment may be necessary depending on platelet count and tolerability (see Tables 1 and 2).

This medication may cause hypertension during treatment, so blood pressure should be regularly monitored, checking every two weeks until it stabilizes. Patients with pre-existing hypertension should be particularly cautious, and medication for blood pressure control may need to be newly prescribed or adjusted. If blood pressure remains consistently high, the dosage of this medication may need to be reduced or stopped. This medication can also cause diarrhea, so treatment to alleviate symptoms, such as dietary management, adequate hydration, and the use of antidiarrheals if necessary, is required if diarrhea occurs. If diarrhea symptoms worsen, the dosage of this medication may need to be reduced or stopped. Women who are pregnant or may become pregnant should be cautious as this medication may pose risks to the fetus, so pregnancy testing should be conducted before taking this medication, and effective contraception should be maintained at least for one month while taking and after stopping this medication. If pregnancy is confirmed, this medication should be stopped immediately. This medication may affect liver function; therefore, regular liver function tests should be conducted, and if liver enzymes significantly increase, the dosage should be reduced or stopped. Since neutrophil counts may decrease during treatment, regular blood tests are necessary for infection prevention, and if neutrophil counts decrease significantly, this medication may need to be stopped or reduced. The tendency for bleeding may increase, so if bleeding symptoms occur, this medication should be stopped or the dosage reduced. This medication may interact with other drugs, so if other medications are being taken, consult with a doctor or pharmacist. This medication is not for use in children and adolescents and should be administered cautiously in elderly patients. In the case of an overdose, there are no specific antidotes, so appropriate treatment and observation based on symptoms are necessary. This medication is sensitive to moisture, so after the package is opened, it must be stored properly and kept out of reach of children. Transferring to other containers is not advised as it may compromise the quality.

• Hypertensive crisis
• diarrhea
• febrile neutropenia
• pneumonia
• difficulty breathing
• increased blood pressure
• neutropenia
• arthralgia
• chest pain
• dizziness

This medication should be stored at room temperature between 1°C and 30°C, and it is important to keep it in a tightly closed container to prevent air from entering. By storing it this way, the effectiveness of the medication can be maintained and deterioration can be prevented.

Appearance

Pale yellowish round film-coated tablet

Package unit

60 tablets/PVTP [10 tablets/PVTP x 6]