非小细胞肺癌的靶向表皮生长因子受体：回顾对于相同的目标的不同的策略

Title:Epidermal Growth Factor Receptor Targeting in Non-Small Cell Lung Cancer: Revisiting Different Strategies Against the Same Target

Volume: 15 Issue: 14

Author(s): Eduardo Castanon, Patricia Martin, Christian Rolfo, Juan P. Fusco, Lucia Ceniceros, Jairo Legaspi, Marta Santisteban and Ignacio Gil-Bazo

Affiliation:

关键词: 激活突变，表皮生长因子受体，络氨酸激酶抑制剂

摘要: Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) have changed the paradigm of treatment in non-small cell lung cancer (NSCLC). The molecular biology study of EGFR has led to clinical trials that select patients more accurately, regarding the presence of EGFR activating mutations. Nonetheless, a lack of response or a temporary condition of the response has been detected in patients on EGFR TKIs. This has urged to study potential resistance mechanisms underneath. The most important ones are the presence of secondary mutations in EGFR, such as T790M, or the overexpression of mesenchymal-epithelial transition factor (MET) that may explain why patients who initially respond to EGFR TKIs, may ultimately become refractory. Several approaches have been taken and new drugs both targeting EGFR resistance-mutation or MET are currently being developed. Here we review and update the EGFR biological pathway as well as the clinical data leading to approval of the EGFR TKIs currently in the market. New compounds under investigation targeting resistance mutations or dually targeting EGFR and other relevant receptors are also reviewed and discussed.

Cite this article as:

Castanon Eduardo, Martin Patricia, Rolfo Christian, P. Fusco Juan, Ceniceros Lucia, Legaspi Jairo, Santisteban Marta and Gil-Bazo Ignacio, Epidermal Growth Factor Receptor Targeting in Non-Small Cell Lung Cancer: Revisiting Different Strategies Against the Same Target, Current Drug Targets 2014; 15 (14) . https://dx.doi.org/10.2174/138945011514141216092935