First Approval of Adagrasib for the Treatment of Non-Small Cell Lung Cancer Harboring a KRASG12C Mutation

被引:7
|
作者
De, Surya K. [1 ,2 ]
机构
[1] Conju Probe, Dept Chem, San Diego, CA 92121 USA
[2] Bharath Univ, Chennai 600126, Tamil Nadu, India
关键词
Non-small cell lung cancer; KRAS mutation; guanosine triphosphate; guanosine diphosphate; adagrasib; sotorasib; RESISTANCE; RAS;
D O I
10.2174/0929867330666230330122000
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Adagrasib is an orally bioavailable, highly selective, small-molecule, irreversible covalent inhibitor of KRAS(G12C). It was approved by the US FDA on December 12, 2022, for patients with tumors harboring the KRAS(G12C )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.
引用
收藏
页码:266 / 272
页数:7
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