lapatinib + pegylated liposomal doxorubicin (Arbeitsgemeinschaft medikamentoese Tumortherapie)

This combination therapy consists of lapatinib, a small-molecule dual tyrosine kinase inhibitor, and Caelyx (pegylated liposomal doxorubicin), a cytotoxic anthracycline. Lapatinib targets the intracellular kinase domains of both the epidermal growth factor receptor (EGFR/ErbB1) and the human epidermal growth factor receptor 2 (HER2/ErbB2), effectively blocking downstream signaling pathways involved in cell proliferation and survival. Caelyx utilizes a pegylated liposomal delivery system to prolong the circulation time of doxorubicin and enhance its accumulation in tumor tissues via the enhanced permeability and retention (EPR) effect. Once released, doxorubicin inhibits topoisomerase II and intercalates into DNA, leading to cell death. This regimen was specifically investigated by the Arbeitsgemeinschaft medikamentoese Tumortherapie (AGMT) in a Phase II clinical trial (NCT00954304) for patients with HER2-positive metastatic breast cancer who had failed prior trastuzumab-based therapy, aiming to provide an effective treatment with a manageable cardiotoxicity profile.

Other names

lapatinib + doxorubicin hydrochloride liposomelapatinib + PLD