Inavolisib Application Scope

Inavolisib (Itovebi™) is indicated in combination with palbociclib and fulvestrant for the treatment of adults with endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy.

Inavolisib Characteristics

Ingredients:

Active Ingredient: Inavolisib
Inactive Ingredients: Microcrystalline cellulose, lactose monohydrate, sodium starch glycolate type A, magnesium stearate, polyvinyl alcohol, polyethylene glycol, ferric oxide red, ferric oxide yellow, talc, titanium dioxide.

Properties:

Mechanism of Action: Inavolisib is a kinase inhibitor that targets the phosphatidylinositol 3-kinase (PI3K) pathway, specifically inhibiting the activity of the PIK3CA variant, thereby reducing cancer cell proliferation and inducing apoptosis.

Packaging Specification:

3 mg Tablets: Red, round, convex-shaped with “INA 3” debossed on one side; packaged in bottles of 28 tablets.
9 mg Tablets: Pink, oval-shaped with “INA 9” debossed on one side; packaged in bottles of 28 tablets.

Storage:
Store at room temperature between 68°F to 77°F (20°C to 25°C). Excursions permitted between 59°F to 86°F (15°C to 30°C). Store in a cool, dry place.

Expiry Date:
Refer to the packaging for the specific expiration date.

Executive Standard:
Approved under New Drug Application (NDA) 219249.

Approval Number:
NDA 219249

Date of Revision:
October 2024

Manufacturer:
Genentech, Inc.

Guidelines for the Use of Inavolisib

Dosage and Administration:

Recommended Dose: 9 mg orally once daily, with or without food.
Administration: Swallow tablets whole; do not chew, crush, or split.
Patient Selection: Confirm the presence of PIK3CA mutation using an FDA-approved test before initiating treatment.
Monitoring: Evaluate fasting plasma glucose and hemoglobin A1C prior to starting and periodically during treatment.

Adverse Reactions:

Common (≥20%): Stomatitis, diarrhea, decreased appetite, fatigue, nausea, rash, headache, hyperglycemia, decreased neutrophils, decreased hemoglobin, decreased platelets, decreased lymphocytes, decreased calcium, decreased potassium, increased creatinine, increased ALT, decreased sodium, decreased magnesium.

Contraindications:
None.

Precautions:

Hyperglycemia: Monitor blood glucose levels; manage with antihyperglycemic medications as needed.
Stomatitis: Monitor for symptoms; consider corticosteroid-containing mouthwash for management.
Diarrhea: Advise increased oral fluids; initiate antidiarrheal treatment at first sign.
Embryo-Fetal Toxicity: Advise on potential fetal harm; recommend effective contraception during treatment and for 1 week after the last dose.

Inavolisib Interactions

Drug Interactions:

Proton Pump Inhibitors: No clinically significant differences in inavolisib pharmacokinetics observed with concomitant use.
CYP450 Enzymes: Inavolisib induces CYP3A and CYP2B6; it is a time-dependent inhibitor of CYP3A.

Indications:
Treatment of adults with endocrine-resistant, PIK3CA-mutated, HR-positive, HER2-negative, locally advanced or metastatic breast cancer, in combination with palbociclib and fulvestrant.

Note:

If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.