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普拉替尼:治疗晚期 RET 融合阳性 NSCLC 的研究进展。

Pralsetinib: A Review in Advanced RET Fusion-Positive NSCLC.

机构信息

Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2022 May;82(7):811-816. doi: 10.1007/s40265-022-01720-4. Epub 2022 May 19.

Abstract

Activating mutations in the proto-oncogene RET have been identified as an oncogenic driver of non-small cell lung cancer (NSCLC) in a small subset of patients. Pralsetinib (Gavreto) is an orally-administered, next-generation, small-molecule selective RET inhibitor that is approved for the treatment of RET fusion-positive metastatic NSCLC. In the pivotal phase I/II ARROW trial, pralsetinib demonstrated rapid and durable anti-tumour activity in patients with advanced RET fusion-positive NSCLC who were previously treated with platinum-based chemotherapy or were treatment-naïve. Pralsetinib also showed clinical activity against intracranial metastases arising from NSCLC. Pralsetinib had a manageable tolerability profile, with the most common grade 3 treatment-related adverse events being neutropenia, hypertension, anaemia and decreased white blood cell count. Currently available data indicate that pralsetinib is a promising new targeted treatment option for patients with advanced RET fusion-positive NSCLC.

摘要

原癌基因 RET 的激活突变已被确定为一小部分非小细胞肺癌 (NSCLC) 患者的致癌驱动因素。普拉替尼 (Gavreto) 是一种口服、新一代、小分子选择性 RET 抑制剂,被批准用于治疗 RET 融合阳性转移性 NSCLC。在关键的 I/II 期 ARROW 试验中,普拉替尼在先前接受过铂类化疗或未经治疗的晚期 RET 融合阳性 NSCLC 患者中表现出快速和持久的抗肿瘤活性。普拉替尼对源自 NSCLC 的颅内转移也具有临床活性。普拉替尼具有可管理的耐受性,最常见的 3 级治疗相关不良事件是中性粒细胞减少症、高血压、贫血和白细胞计数减少。目前的数据表明,普拉替尼是一种有前途的新型针对晚期 RET 融合阳性 NSCLC 患者的靶向治疗选择。

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