TAVALISSE Film-coated tablet (2020)

Βιβλιογραφική αναφορά

Συγγραφείς

Rigel Pharmaceuticals, Inc.

Λέξεις κλειδιά

71332-001 71332-002

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1. Indications and Usage

TAVALISSE is indicated for the treatment of thrombocytopenia in adult patients with chronic immune thrombocytopenia (ITP) who have had an insufficient response to a previous treatment.

2. Dosage and Administration

2.1 Recommended Dosage Initiate TAVALISSE at a dose of 100 mg taken orally twice daily. After a month, if platelet count has not increased to at least 50 × 109/L, increase TAVALISSE dose to ...

3. Dosage Forms and Strengths

TAVALISSE is available as: 100 mg tablet: orange, film-coated, round, biconvex tablets debossed with 100 on one side and R on the reverse side. 150 mg tablet: orange, film-coated, oval, biconvex tablets ...

4. Contraindications

None.

5. Warnings and Precautions

5.1 Hypertension Hypertension can occur with TAVALISSE treatment; hypertensive crisis occurred in 1% of patients. Patients with pre-existing hypertension may be more susceptible to the hypertensive effects ...

6. Adverse Reactions

The following clinically important adverse reactions, that can become serious are described elsewhere in the labeling: Hypertension [see Warnings and Precautions (5.1)] Hepatotoxicity [see ...

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

7. Drug Interactions

7.1 Effect of Other Drugs on TAVALISSE Strong CYP3A4 Inhibitors Concomitant use with strong CYP3A4 inhibitors increases exposure to R406 (the major active metabolite), which may increase the risk of adverse ...

8.1. Pregnancy

Risk Summary Based on findings from animal studies and the mechanism of action, TAVALISSE can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1)]. There are ...

8.2. Lactation

Risk Summary There are no data on the presence of fostamatinib and/or its metabolites in human milk, the effects on the breastfed child, or on milk production. In rodents, R406 (the major active metabolite) ...

8.3. Females and Males of Reproductive Potential

Pregnancy Testing Based on animal studies, TAVALISSE can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1)]. For females of reproductive potential, ...

8.4. Pediatric Use

Safety and effectiveness in pediatric patients have not been established. TAVALISSE is not recommended for use in patients less than 18 years of age because adverse effects on actively growing bones were ...

8.5. Geriatric Use

Of the 102 patients with ITP who received TAVALISSE, 28 (27%) were 65 years of age and older, while 11 (11%) were 75 years of age and older. In patients 65 years of age and older, 6 (21%) patients experienced ...

10. Overdosage

There is no specific antidote for overdose with TAVALISSE, and the amount of R406 (the pharmacologically active metabolite of fostamatinib) cleared by dialysis is negligible. In the event of an overdose, ...

11. Description

Fostamatinib is a tyrosine kinase inhibitor. TAVALISSE is formulated with the disodium hexahydrate salt of fostamatinib, a phosphate prodrug that converts to its pharmacologically active metabolite, R406, ...

12.1. Mechanism of Action

Fostamatinib is a tyrosine kinase inhibitor with demonstrated activity against spleen tyrosine kinase (SYK). The major metabolite of fostamatinib, R406, inhibits signal transduction of Fc-activating receptors ...

12.2. Pharmacodynamics

Mean treatment-related increases of 2.93 mmHg in systolic blood pressure and 3.53 mmHg in diastolic blood pressure over placebo were observed following TAVALISSE doses of 100 mg twice daily for 28 days. ...

12.3. Pharmacokinetics

TAVALISSE is a prodrug that is converted in the gut to the major active metabolite, R406. Mean (± standard deviation [SD]) exposure estimates of R406 are 550 (± 270) ng/mL for Cmax and 7080 ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Fostamatinib was not carcinogenic in a 2-year study in mice when administered daily by oral gavage at doses up to 500/250 mg/kg/day, and was not carcinogenic in rats when administered by oral gavage at ...

14. Clinical Studies

TAVALISSE was studied in two placebo-controlled efficacy and safety studies (referred to as FIT-1 [NCT02076399] and FIT-2 [NCT02076412]), and in an open-label extension study referred to as FIT-3 (NCT ...

16.1. How Supplied

TAVALISSE 100 mg tablets are round, biconvex, orange, film-coated tablets debossed with 100 on one side and R on the reverse side. TAVALISSE 150 mg tablets are oval, biconvex, orange, film-coated tablets ...

16.2. Storage and Handling

Store at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Do not remove desiccants.

17. Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling (Patient Information). Hypertension: Inform patients that periodic monitoring of their blood pressure is required, as high blood pressure ...