inavolisib

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Diabetes mellitus;
Moderate renal impairment (↓ dose);
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may be more sensitive to drug effects.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia, dry skin, rash

Endo: hyperglycemia

F and E: hypocalcemia, hypokalemia, hypomagnesemia, hyponatremia

GI: ↑lipase, ↑liver enzymes, diarrhea, nausea, stomatitis, vomiting

GU: ↑serum creatinine, ↓fertility

Hemat: anemia, lymphopenia, neutropenia, thrombocytopenia

Metab: ↓appetite, weight loss

Neuro: fatigue, headache

Misc: infection

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Tablets: 3 mg; 9 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 9 mg once daily; continue until disease progression or unacceptable toxicity.

Renal Impairment

PO (Adults ): 6 mg once daily; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as an inhibitor of phosphatidylinositol 3-kinase (PI3K). Mutations in the gene encoding the catalytic α-subunit of PI3K (PI3KCA) lead to activation of PI3Kα and Akt-signaling, cellular transformation, and tumor generation. Inavolisib inhibits phosphorylation of PI3K downstream targets (including Akt) and demonstrated activity in cell lines harboring a PIK3CA mutation. Activating mutations in PIK3CA may induce overgrowths and malformations in PIK3CA-related overgrowth spectrum.

Therapeutic effects:

Decreased progression of breast cancer.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 76% absorbed following oral administration.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Primarily metabolized via hydrolysis; minimally metabolized by the CYP3A4 isoenzyme. 49% excreted in urine (40% as unchanged drug); 48% excreted in feces (11% as unchanged drug).

Half-Life: 15 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of inavolisib. Advise patient to take as directed. Swallow tablets whole, with or without food, at the same time each day; do not chew, crush, or split tablets prior to swallowing. If ≤9 hr from when dose is missed, take the missed dose as soon as possible; if >9 hr since missed dose, skip the dose and take the next dose at the scheduled time. If a dose is vomited, do not take an additional dose on that day and resume the usual dosing schedule the next day. Advise patient to read Patient Information before starting therapy.
Teach patient to report symptoms of hyperglycemia (↑ thirst, frequent urination, headache, blurred vision, fatigue).
Advise patient to report symptoms of stomatitis (painful mouth ulcers, sores, or blisters; bad breath; discomfort with eating and drinking). Sugar-free hard candies or mints can be used to prevent dry mouth. Teach patient about maintaining good oral hygiene and hydration.
Instruct patient to report severe diarrhea; advise patient to drink plenty of fluid to prevent dehydration.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Advise women of reproductive potential to use effective nonhormonal contraception during treatment and for 1 wk after last dose. Advise men with female partners of reproductive potential to use effective contraception during treatment and for 1 wk after last dose.

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Indications ⬇

Contraind./Precautions ⬆ ⬇