Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York, USA.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York, USA and Department of Otolaryngology-Head and Neck Surgery, Zhongnan Hospital of Wuhan University, Wuhan, China.
Drugs Today (Barc). 2021 Apr;57(4):265-275. doi: 10.1358/dot.2021.57.4.3238323.
Non-small cell lung cancer (NSCLC) is one of the most devastating cancers with high mortality worldwide. By inhibiting the activity of specific molecular targets in the cancer cells, tyrosine kinase inhibitors (TKIs) have become a standard treatment in combating NSCLC. Tepotinib hydrochloride is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations. Tepotinib demonstrated durable clinical response in phase II clinical trials, which led to its approval for use in Japan and breakthrough therapy designation and accelerated approval in the U.S. These progresses highlighted tepotinib as a promising candidate for NSCLC patients. This review summarizes the pharmacological profile of tepotinib, preclinical studies and landmark clinical trials of tepotinib. In addition, we share our perspectives on the future direction of tepotinib as a novel anticancer drug.
非小细胞肺癌（NSCLC）是全球死亡率较高的最具破坏性的癌症之一。通过抑制癌细胞中特定分子靶标的活性，酪氨酸激酶抑制剂（TKI）已成为治疗 NSCLC 的标准方法。盐酸特泊替尼是一种口服生物利用度的间质-上皮转化（MET）TKI，主要针对具有 METex14 跳跃突变的选定 NSCLC 患者开发。盐酸特泊替尼在 II 期临床试验中表现出持久的临床反应，这促使其在日本获得批准，并在美国获得突破性治疗指定和加速批准。这些进展凸显了盐酸特泊替尼作为 NSCLC 患者有前途的候选药物。本综述总结了盐酸特泊替尼的药理学特征、盐酸特泊替尼的临床前研究和里程碑式临床试验。此外，我们还分享了我们对盐酸特泊替尼作为一种新型抗癌药物的未来发展方向的看法。
