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Ayvakit Generic Name & Formulations
Legal Class
Rx
General Description
Avapritinib 25mg, 50mg, 100mg, 200mg, 300mg; tabs.
Pharmacological Class
Tyrosine kinase inhibitor.
How Supplied
Tabs—30
Manufacturer
Generic Availability
NO
Ayvakit Indications
Indications
In adults with unresectable or metastatic gastrointestinal stromal tumor (GIST) harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations.
Ayvakit Dosage and Administration
Adult
Give on an empty stomach (at least 1hr before and 2hrs after a meal). 300mg once daily; continue until disease progression or unacceptable toxicity. Avoid concomitant use with strong or moderate CYP3A inhibitors; if use with moderate CYP3A inhibitor is unavoidable, initiate dosing at 100mg once daily. Dose modifications: see full labeling.
Children
Not established.
Ayvakit Contraindications
Not Applicable
Ayvakit Boxed Warnings
Not Applicable
Ayvakit Warnings/Precautions
Warnings/Precautions
Risk of intracranial hemorrhage; monitor closely including those with thrombocytopenia, vascular aneurysm, or history of intracranial hemorrhage or cerebrovascular accident within the prior year. Permanently discontinue if intracranial hemorrhage of any grade occurs. In AdvSM: interrupt or reduce dose if platelet counts <50×109/L; platelet support may be needed. Risk of CNS effects (eg, cognitive impairment, dizziness, sleep disorders, others); if occurs, withhold dose and then resume at reduced (or at same) dose upon resolution, or permanently discontinue based on severity. Severe renal impairment (CrCl 15–29mL/min) or ESRD (CrCl <15mL/min). Severe hepatic impairment. Embryo-fetal toxicity. Advise females and males of reproductive potential to use effective contraception during and for 6 weeks after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after the last dose).
Ayvakit Pharmacokinetics
See Literature
Ayvakit Interactions
Interactions
See Adults. Potentiated by strong or moderate CYP3A inhibitors (eg, itraconazole, fluconazole). Antagonized by strong or moderate CYP3A inducers (eg, rifampin, efavirenz); avoid.
Ayvakit Adverse Reactions
Adverse Reactions
Edema, nausea, fatigue/asthenia, cognitive impairment, vomiting, decreased appetite, diarrhea, increased lacrimation, abdominal pain, rash, constipation, dizziness, hair color changes; anemia, subdural hematoma, pleural effusion, ascites, pneumonia, sepsis.
Ayvakit Clinical Trials
See Literature
Ayvakit Note
Not Applicable
Ayvakit Patient Counseling
See Literature
Ayvakit Generic Name & Formulations
Legal Class
Rx
General Description
Avapritinib 25mg, 50mg, 100mg, 200mg, 300mg; tabs.
Pharmacological Class
Tyrosine kinase inhibitor.
How Supplied
Tabs—30
Manufacturer
Generic Availability
NO
Ayvakit Indications
Indications
In adults with advanced systemic mastocytosis (AdvSM), including those with aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematological neoplasm (SMAHN), and mast cell leukemia (MCL).
Limitations of Use
Not for use in patients with AdvSM with platelet counts <50x109/L.
Ayvakit Dosage and Administration
Adult
Give on an empty stomach (at least 1hr before and 2hrs after a meal). 200mg once daily; continue until disease progression or unacceptable toxicity. Avoid concomitant use with strong or moderate CYP3A inhibitors; if use with moderate CYP3A inhibitor is unavoidable, initiate dosing at 50mg once daily. Dose modifications: see full labeling.
Children
Not established.
Ayvakit Contraindications
Not Applicable
Ayvakit Boxed Warnings
Not Applicable
Ayvakit Warnings/Precautions
Warnings/Precautions
Risk of intracranial hemorrhage; monitor closely including those with thrombocytopenia, vascular aneurysm, or history of intracranial hemorrhage or cerebrovascular accident within the prior year. Permanently discontinue if intracranial hemorrhage of any grade occurs. In AdvSM: interrupt or reduce dose if platelet counts <50×109/L; platelet support may be needed. Risk of CNS effects (eg, cognitive impairment, dizziness, sleep disorders, others); if occurs, withhold dose and then resume at reduced (or at same) dose upon resolution, or permanently discontinue based on severity. Severe renal impairment (CrCl 15–29mL/min) or ESRD (CrCl <15mL/min). Severe hepatic impairment. Embryo-fetal toxicity. Advise females and males of reproductive potential to use effective contraception during and for 6 weeks after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after the last dose).
Ayvakit Pharmacokinetics
See Literature
Ayvakit Interactions
Interactions
See Adults. Potentiated by strong or moderate CYP3A inhibitors (eg, itraconazole, fluconazole). Antagonized by strong or moderate CYP3A inducers (eg, rifampin, efavirenz); avoid.
Ayvakit Adverse Reactions
Adverse Reactions
Edema, nausea, fatigue/asthenia, cognitive impairment, vomiting, decreased appetite, diarrhea, increased lacrimation, abdominal pain, rash, constipation, dizziness, hair color changes; anemia, subdural hematoma, pleural effusion, ascites, pneumonia, sepsis.
Ayvakit Clinical Trials
See Literature
Ayvakit Note
Not Applicable
Ayvakit Patient Counseling
See Literature
