RO7771950

RO7771950 is an investigational, orally bioavailable, small molecule tyrosine kinase inhibitor (TKI) developed by Roche that specifically targets the Human Epidermal Growth Factor Receptor 2 (HER2). It is designed to be highly selective for HER2 over the Epidermal Growth Factor Receptor (EGFR/HER1), a feature intended to reduce off-target toxicities such as severe diarrhea and skin rash often associated with dual HER2/EGFR inhibitors. A critical attribute of RO7771950 is its ability to penetrate the blood-brain barrier (BBB), allowing it to reach therapeutic concentrations in the central nervous system (CNS). This makes it particularly relevant for treating HER2-positive metastatic breast cancer, where brain metastases are a frequent and challenging complication. It is currently being evaluated in the Phase 2/3 BREnnA study in combination with trastuzumab and capecitabine, comparing its efficacy and safety directly against tucatinib.

Other names

bizrolertinibbizrolertinib sesquifumarateperzebertinib