非小细胞肺癌靶向治疗新药——厄洛替尼

New drug for non-small cell lung cancer target therapy-erlotinib

厄洛替尼是一种口服、高选择性、可逆的表皮生长因子受体(EGFR)酪氨酸激酶(TK)抑制剂,它通过抑制EGFR-TK的自磷酸化反应,抑制信号转导,从而达到抑制肿瘤生长作用。一项Ⅲ期安慰剂对照临床研究结果表明,厄洛替尼每日口服150 mg单药治疗,可显著延长晚期复发性非小细胞肺癌(NSCLC)病人的生存期、延缓疾病进展和症状恶化,且耐受性较好,最常见的不良反应为皮疹和腹泻。本文对厄洛替尼的药动学和药效学特性、临床疗效和药物相互作用以及难治性晚期NSCLC病人的耐受性等作一综述。

Erlotinib is an orally active, highly selective, reversible inhibitor of the epidermal growth factor receptor （EGFR） tyrosine kinase （TK） . Erlotinib inhibits the autophosphorylation of EGFR-TK, signal transduction, and in term of tumor growth. In a phase Ⅲ placebo-controlled study of patients with advanced,treatment-relapsed non-small cell lung cancer （NSCLC） , erlotinib 150 mg once daily single treatment can significantly prolong the survival and delay disease progression with lessening of lung cancer-related symptoms.Erlotinib is well tolerated with commonest adverse reaction of rash and diarrhoea. This article reviews the pharmacokinetic and pharmacodynamic properties; and comprehends the clinical efficacy and the drug interactions together with tolerability of erlotinib in patients with refractory advanced NSCLC.