Takeda Masayuki, Okamoto Isamu
Dept. of Medical Oncology, Kinki University Faculty of Medicine.
Gan To Kagaku Ryoho. 2011 Jun;38(6):896-900.
Erlotinib and gefitinib are quinazoline derivatives that selectively and reversibly inhibit the tyrosine kinase activity of the EGFR. Activating mutations in the EGFR confer hypersensitivity to the tyrosine kinase inhibitors gefitinib and erlotinib in patients with advanced non-small-cell lung cancer. Erlotinib has been developed in EGFR mutation-positive patients as a firstline treatment, and results from recently completed phase III studies have shown superior progression-free survival and response rates for erlotinib, compared to chemotherapy.
厄洛替尼和吉非替尼是喹唑啉衍生物，可选择性且可逆地抑制表皮生长因子受体（EGFR）的酪氨酸激酶活性。在晚期非小细胞肺癌患者中，EGFR的激活突变使患者对酪氨酸激酶抑制剂吉非替尼和厄洛替尼敏感。厄洛替尼已被开发用于EGFR突变阳性患者的一线治疗，最近完成的III期研究结果表明，与化疗相比，厄洛替尼具有更长的无进展生存期和更高的缓解率。
