pictilisib + trastuzumab

**Pictilisib + trastuzumab** is an investigational combination regimen consisting of pictilisib (GDC-0941), an oral small molecule pan-phosphatidylinositol 3-kinase (PI3K) inhibitor, and trastuzumab, a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2). Pictilisib inhibits all class I PI3K isoforms, interfering with downstream PI3K/AKT signaling, critical for cell proliferation and survival. Trastuzumab binds to the extracellular domain of HER2, blocking receptor activation and mediating antibody-dependent cell-mediated cytotoxicity (ADCC). The combination was tested in phase I trials for locally recurrent or metastatic breast cancer, especially HER2-positive disease, aiming to block two oncogenic pathways: PI3K signaling and HER2-driven proliferation. The regimen was evaluated for safety, tolerability, pharmacokinetics, and preliminary anti-tumor activity, with the potential for improved outcomes in breast cancer by dual pathway blockade[1][2][3][7].

Brand names

pictilisib + trastuzumab

Other names

pictilisib + trastuzumabGDC-0941 + trastuzumab