lapatinib + bortezomib

Lapatinib + bortezomib is a combination of two small molecule anticancer agents used in investigational settings for the treatment of advanced malignancies, particularly HER2-overexpressing breast cancer. Lapatinib is an oral dual tyrosine kinase inhibitor that targets the intracellular domains of both epidermal growth factor receptor (HER1/EGFR/ERBB1) and human epidermal growth factor receptor 2 (HER2/ERBB2), thereby inhibiting ERBB-driven tumor cell proliferation[1][3][5]. Bortezomib is a reversible proteasome inhibitor that disrupts the ubiquitin-proteasome pathway by binding to the 26S proteasome, leading to accumulation of proteins involved in cell cycle regulation and apoptosis[4][6]. The combination has shown synergistic inhibition of tumor cell growth and enhanced apoptosis in preclinical models, with evidence suggesting more effective blockade of HER2 signaling pathways compared to monotherapy[2][3]. Clinical studies have demonstrated tolerability but limited efficacy at tested doses.

Other names

none