ITOVEBI® is the global commercial brand name, and Yihelai is its Chinese brand name developed by Roche. It is an oral third-generation highly selective PI3Kα inhibitor with dual inhibition and degradation mechanism. It specifically targets mutant PI3Kα protein to block PI3K/AKT tumor proliferation signaling pathway for PIK3CA-mutant breast cancer.
Main Indications
Combined use with palbociclib and fulvestrant for the treatment of HR-positive, HER2-negative, PIK3CA-mutant advanced or metastatic breast cancer in adult patients with endocrine therapy resistance (including recurrence during or after adjuvant endocrine therapy).
Clinical Research
Global multicenter phase III pivotal trials fully validated its significant progression-free survival benefit for PIK3CA-mutant endocrine-resistant advanced breast cancer;
Head-to-head comparative registration trials confirmed superior tumor control rate versus traditional PI3K inhibitor regimens with lower severe hyperglycemia risk;
Long-term follow-up cohort studies demonstrated durable tumor suppression and predictable metabolic safety during continuous daily oral administration;
Dose-finding research verified balanced anti-tumor efficacy and glycemic tolerability of the 9mg once-daily oral regimen;
Chinese domestic registration trials confirmed consistent therapeutic activity and manageable adverse reaction spectrum for local HR+/HER2- PIK3CA-mutant breast cancer populations.
Common Side Effects
Common mild adverse reactions: Hyperglycemia, diarrhea, nausea, fatigue, stomatitis and rash;
Laboratory abnormalities: Elevated blood glucose, elevated triglycerides, transient mild liver transaminase elevation and hypokalemia;
Severe but uncommon risks: Severe uncontrolled hyperglycemia, severe cutaneous adverse reactions, severe diarrhea leading to electrolyte disturbance and interstitial lung disease.
Approval Status in China
Original drug ITOVEBI® (Chinese brand: Yihelai) was officially approved for marketing in China in March 2025, with the specification of 9mg per tablet, 28 tablets per box (7 tablets per plate, 4 plates). It is currently a prescription targeted anti-tumor drug included in China’s Category B medical insurance catalogue starting from 2026.
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