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inavolisib (Itovebi)
Indications:
- in combination with palbociclib & fulvestrant treatment of endocrine-resistant, PIK3CA-mutated, hormone receptor-positive, HER2-negative, locally advanced or metastatic breast cancer
Contraindications:
- pregnancy, embryo-fetal toxicity
- lactation
Dosage:
- 9 mg PO QD with or without food
- Tablets: 3 mg, 9 mg
Dosage adjustment in renal failure:
- 6 mg orally once daily if eGFR 30-60 mL/min (based on CKD-EPI)
Adverse effects:
- stomatitis*, diarrhea, nausea, headache
- hyperglycemia, hypocalcemia. hypokalemia, hyponatremia, hypomagnesemia
- increased serum creatinine, increased serum ALT
- leukopenia, anemia, thrombocytopenia, lymphopenia
* treat stomatitis with glucocorticoid-containing mouthwash
Mechanism of action:
- inhibits phosphatidylinositol 3-kinase (PI3K), predominantly PI3K-alpha
- degrades mutated PI3K-alpha, inhibits phosphorylation of downstream AKT
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM cid=124173720
References
- HIGHLIGHTS OF PRESCRIBING INFORMATION
ITOVEBI (inavolisib) tablets, for oral use
https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/219249s001lbl.pdf