lapatinib + FOLFIRI

Lapatinib + FOLFIRI is a combination regimen consisting of **lapatinib**, an oral small-molecule dual tyrosine kinase inhibitor targeting both **epidermal growth factor receptor (EGFR/ErbB1)** and **human epidermal growth factor receptor 2 (HER2/ErbB2)**, and **FOLFIRI**, a chemotherapy regimen comprising irinotecan, fluorouracil (5-FU), and leucovorin. Lapatinib blocks growth-promoting signaling cascades by inhibiting the phosphorylation of EGFR and HER2, while FOLFIRI targets rapidly dividing cells by disrupting DNA synthesis (5-FU, an antimetabolite), impeding DNA replication (irinotecan, a topoisomerase I inhibitor), and enhancing 5-FU's effectiveness (leucovorin). The combination is under clinical investigation, mainly for advanced or metastatic colorectal cancer and potentially other solid tumors, aiming to leverage cytotoxic and targeted mechanisms to overcome resistance and improve efficacy in settings where tumors express HER2 and/or EGFR.

Brand names

Tykerb + FOLFIRI

Other names

lapatinib plus FOLFIRI