Penn State Hershey Cancer Institute, Penn State Milton S. Hershey Medical Center, 500 University Drive, Hershey, PA 17033, USA.
Cancer Invest. 2010 May;28(4):413-23. doi: 10.3109/07357901003631072.
Reversible epidermal growth factor receptor tyrosine kinase inhibitors are often used for the treatment of non-small cell lung cancer following failure of cytotoxic chemotherapy. While these agents are active in a subset of patients, most develop resistance and progress within the course of 1 year. In nearly half of the cases, acquired resistance is caused by a secondary epidermal growth factor receptor T790M mutation. Irreversible epidermal growth factor receptor tyrosine kinase inhibitors are an emerging class of agents that may have the potential to overcome and prevent the emergence of such mutation-related resistance.
可逆表皮生长因子受体酪氨酸激酶抑制剂常用于细胞毒化疗失败后的非小细胞肺癌治疗。虽然这些药物对一部分患者有效,但大多数患者在 1 年内会产生耐药性并进展。在近一半的情况下,获得性耐药是由继发的表皮生长因子受体 T790M 突变引起的。不可逆表皮生长因子受体酪氨酸激酶抑制剂是一类新兴的药物,可能具有克服和预防这种突变相关耐药性的潜力。