阿达格拉西布首次获批用于治疗携带某种突变的非小细胞肺癌。
First Approval of Adagrasib for the Treatment of Non-Small Cell Lung Cancer Harboring a Mutation.
作者信息
De Surya K
机构信息
Department of Chemistry, Conju-Probe, San Diego, California, USA.
Bharath University, Chennai, Tamil Nadu, 600126, India.
出版信息
Curr Med Chem. 2024;31(3):266-272. doi: 10.2174/0929867330666230330122000.
Adagrasib is an orally bioavailable, highly selective, small-molecule, irreversible covalent inhibitor of KRASG12C. It was approved by the US FDA on December 12, 2022, for patients with tumors harboring the KRASG12C mutation in locally advanced or metastatic non-small cell lung cancer (NSCLC). Herein, synthesis, dosage and administration, mechanism of action, pharmacokinetics, pharmacodynamics, and adverse events of adagrasib are described.
阿达格拉西布是一种口服生物可利用的、高度选择性的小分子、不可逆共价KRASG12C抑制剂。2022年12月12日,它被美国食品药品监督管理局(US FDA)批准用于治疗局部晚期或转移性非小细胞肺癌(NSCLC)且携带KRASG12C突变的肿瘤患者。本文介绍了阿达格拉西布的合成、用法用量、作用机制、药代动力学、药效学和不良反应。