Unidad de Investigación Básica y Traslacional, Oncosalud-AUNA, Lima, Peru.
Escuela de Medicina Humana, Universidad Privada San Juan Bautista, Lima, Peru.
Hematol Oncol Stem Cell Ther. 2021 Sep;14(3):192-198. doi: 10.1016/j.hemonc.2020.11.005. Epub 2020 Dec 1.
ROS proto-oncogene 1 (ROS1) encodes a type I integral membrane protein with tyrosine kinase activity and whose activating alterations are involved in the aggressiveness of several tumor types. Fusions involving ROS1 gene are present in 1-2% of lung adenocarcinomas and other solid tumors. Entrectinib, also known as RXDX-101, is a potent second-generation, multitarget oral inhibitor against NTRK1, NTRK2, NTRK3, ALK, and ROS1 with the ability to cross the blood-brain barrier. Results of Phase I and II trials have led the Food and Drug Administration to grant approval to entrectinib for the treatment of patients with metastatic, ROS1-positive non-small cell lung cancer (NSCLC). In this review, we will describe the biology of ROS1, as well as results of the efficacy and safety of different clinical trials evaluating entrectinib in ROS1-positive NSCLC.
ROS 原癌基因 1（ROS1）编码一种具有酪氨酸激酶活性的 I 型整合膜蛋白，其激活改变与多种肿瘤类型的侵袭性有关。ROS1 基因融合存在于 1-2%的肺腺癌和其他实体肿瘤中。恩曲替尼，也称为 RXDX-101，是一种强效的第二代、多靶点口服抑制剂，针对 NTRK1、NTRK2、NTRK3、ALK 和 ROS1，能够穿透血脑屏障。I 期和 II 期临床试验的结果促使美国食品和药物管理局批准恩曲替尼用于治疗转移性、ROS1 阳性非小细胞肺癌（NSCLC）患者。在这篇综述中，我们将描述 ROS1 的生物学特性，以及不同临床试验评估恩曲替尼在 ROS1 阳性 NSCLC 中的疗效和安全性的结果。
