Itovebi Inavolisib Tablets

1. Indications and Usage
Breast Cancer: Treatment of adult patients with hormone receptor (HR)-positive, HER2-negative, PIK3CA-mutant, locally advanced or metastatic breast cancer who have disease recurrence during or after endocrine therapy.
Combination Requirement: Must be used in combination with palbociclib and fulvestrant.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage: 9 mg once daily. Tablets must be swallowed whole; do not chew, crush, or split.
Critical Administration Instructions:
Dietary Impact: Can be taken with or without food.
Missed Dose: If a dose is missed, take it as soon as possible within 9 hours of the regular time. If more than 9 hours have passed, skip the dose and resume the regular schedule. Do not take two doses at once.
Vomiting: If vomiting occurs after taking a dose, do not take an extra dose on the same day; resume the next day at the regular time.
3. Mechanism of Action
PI3Kα Inhibition: Inavolisib is a selective inhibitor of the PI3Kα isoform.
Target Degradation: It induces the degradation of the mutant p110α catalytic subunit encoded by the PIK3CA gene, inhibiting the PI3K/AKT/mTOR signaling pathway.
Sensitization: This reduces phosphatidylinositol-3,4,5-trisphosphate (PIP3) accumulation and AKT phosphorylation, inhibiting tumor cell proliferation and sensitizing cells to endocrine therapy.
4. Safety and Warnings
Hyperglycemia: A major risk requiring regular monitoring of fasting blood glucose and HbA1c. Dose interruptions or reductions are required for significant elevation.
Hepatic Impairment: Monitor liver function tests (ALT, AST) regularly. Dose modifications may be necessary for significant elevations.
Mucocutaneous Toxicity: Stomatitis and rash are common. Dose holds or reductions are necessary based on severity.
Pregnancy and Lactation: Can cause fetal harm. Contraindicated in pregnancy.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Hyperglycemia, anemia, neutropenia, platelet count decrease, lymphopenia, diarrhea, nausea, stomatitis, and fatigue.
Clinical Research Highlights: The Phase 3 INAVO120 trial demonstrated that the addition of inavolisib to the standard of care significantly improved progression-free survival (PFS) in the target population.
6. Drug Interactions
CYP3A4 Modulators: Strong CYP3A4 inhibitors or inducers can significantly alter inavolisib exposure. Dose adjustments or avoidance may be necessary.
Antidiabetic Agents: Concomitant use may require adjustment of antidiabetic medication due to the risk of hyperglycemia.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Inavolisib.
Appearance: Tablets (available in 3 mg and 9 mg strengths).
Packaging: Blister packaging containing 28 tablets per box.
Storage: Store at 20°C to 25°C (68°F to 77°F); protect from moisture.