a Department of Pharmaceutical , Central Hospital of Linyi City , Yishui , Shandong , China.
Expert Rev Clin Pharmacol. 2019 Mar;12(3):173-178. doi: 10.1080/17512433.2019.1570846. Epub 2019 Jan 30.
Approximately 3-5% of patients with non-small cell lung cancer （NSCLC）belonged to anaplastic lymphoma kinase (ALK)-positive NSCLC. The treatment drugs of ALK-positive NSCLC mainly included crizotinib, ceritinib, alectinib, and brigatinib. Although these drugs had some effects, most of them were usually easy to develop drug resistance. Lorlatinib is a new inhibitor of ALK for treating ALK-positive NSCLC,the effect is obvious, and not easy to develop resistance. Areas covered: The main mechanism of action, pharmacokinetics, clinical efficacy and safety of lorlatinib were introduced in this paper. Expert commentary: Lorlatinib is a new, reversible, ATP-competitive small molecule inhibitor of ALK and c-ros oncogene 1 (ROS1). It can inhibit tumor cell growth in ALK- and ROS1-overexpressing tumor cells. Clinical trial indicated that lorlatinib had obvious therapeutic effect for patients with ALK-positive NSCLC. Lorlatinib could also pass through the blood-brain barrier, which had a good effect on patients with brain metastasis. Adverse events of lorlatinib were mostly mild and moderate in severity, and patients were easily tolerated. Most common adverse events were edema, peripheral neuropathy, cognitive effects, dyspnea, fatigue, weight gain, arthralgia, mood effects, and diarrhea.
大约 3-5%的非小细胞肺癌（NSCLC）患者属于间变性淋巴瘤激酶（ALK）阳性 NSCLC。ALK 阳性 NSCLC 的治疗药物主要包括克唑替尼、塞瑞替尼、阿来替尼和布加替尼。虽然这些药物有一定的疗效，但大多数药物通常容易产生耐药性。劳拉替尼是一种用于治疗 ALK 阳性 NSCLC 的新型 ALK 抑制剂，疗效显著，不易产生耐药性。
本文介绍了劳拉替尼的主要作用机制、药代动力学、临床疗效和安全性。
劳拉替尼是一种新型、可逆、ATP 竞争性的小分子 ALK 和 c-ros 原癌基因 1（ROS1）抑制剂，可抑制 ALK 和 ROS1 过表达肿瘤细胞中的肿瘤细胞生长。临床试验表明，劳拉替尼对 ALK 阳性 NSCLC 患者有明显的治疗效果。劳拉替尼还可以穿透血脑屏障，对有脑转移的患者有很好的疗效。劳拉替尼的不良反应大多为轻度和中度，患者容易耐受。最常见的不良反应是水肿、周围神经病、认知影响、呼吸困难、疲劳、体重增加、关节痛、情绪影响和腹泻。
