Names and pronunciation
(a’va-pri’ ti-nib) Ayvakit
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Drug reference
(a’va-pri’ ti-nib) Ayvakit
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Func. class.: Antineoplastic
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Chem. class.: Tyrosine kinase inhibitor
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ACTION: Blocks PDGFRA and KIT exon 11, 11/17, 17 mutations
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USES: Unresectable/metastatic GI stromal tumor (GIST) with these mutations
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CONTRAINDICATIONS: Hyper- sensitivity, pregnancy, breastfeeding Precautions: Intracranial hemorrhage
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SIDE EFFECTS CV: Edema INTEG: Alopecia, hair discoloration, rash GI: Abdominal pain, constipation, anorexia, diarrhea, dysgeusia, dyspepsia, nausea/vomiting CNS: CNS toxicity, cognitive dysfunction, dizziness, fatigue, headache, memory impairment, mood/sleep disorder, fever MS: Asthenia EENT: Tearing, periorbital edema RESP: Dyspnea, pleural effusion
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INTERACTIONS Increase avapritinib effect: Moderate/ strong CYP3A4 inhibitors, avoid using together Decrease avapritinib effect: Moderate/ strong CYP3A4 inducers, avoid using together Drug/Lab: Increase: LFTs, bilirubin, serum creatinine, INR, PTT, thrombo cytopenia Decrease: Serum albumin, serum mag- nesium, serum phosphate, serum potas- sium/sodium, neutrophils, leukocytes
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DOSAGE AND ROUTES • Adult: PO 300 mg daily on an empty stomach, continue until disease progres- sion or unacceptable toxicity Systemic mast cell disease • Adult: PO 200 mg daily on empty stomach, continue until disease progres- sion or unacceptable toxicity
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Available forms: Tablet 100 mg, 200 mg, 300 mg
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Administer: • Give on an empty stomach, at least 1 hr before or 2 hr after a meal • If a dose is missed, do not take if next dose is due within 8 hr • Give antiemetics to prevent nausea and vomiting • Store at room temperature
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Assess: • Assess for PDGFRA exon 18 mutations before use • Assess for pregnancy before use in females of reproductive potential, males with female partners of reproductive po- tential should use contraception during and for 6 wk after last dose • Monitor CNS effects (cognitive impair- ment, dizziness, sleep/mood/speech dis- orders), intracranial hemorrhage
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Evaluate: • Therapeutic response: Decrease in spread of GI stromal tumor
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To report adverse reactions immedi- ately: Severe headache, cognitive changes, shortness of breath, change in vision • About reason for treatment, expected results • That effect on male infertility is un- known • Not to stop or change dose • To avoid hazardous activities until re- sponse is known, dizziness may occur • To take on empty stomach • To avoid OTC products unless ap- proved by prescriber • To notify prescriber if pregnancy is planned or suspected; not to breastfeed; to use effective contraception during and for 6 wk after last dose, females of repro- ductive potential and males with female partners of reproductive potential
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PHARMACOKINETICS Onset unknown, peak 2-4 hr, duration unknown, half-life 32-57 hr, protein binding 98.8%
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• Adult: PO 300 mg daily on an empty stomach, continue until disease progres- sion or unacceptable toxicity Systemic mast cell disease
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• Adult: PO 200 mg daily on empty stomach, continue until disease progres- sion or unacceptable toxicity
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