A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib

Danielle Brazel; Zhaohui Arter; Misako Nagasaka

doi:10.2147/LCTT.S383662

A Long Overdue Targeted Treatment for KRAS Mutations in NSCLC: Spotlight on Adagrasib

Lung Cancer (Auckl). 2022 Nov 10:13:75-80. doi: 10.2147/LCTT.S383662. eCollection 2022.

Authors

Danielle Brazel¹, Zhaohui Arter¹, Misako Nagasaka^{1

2

3}

Affiliations

¹ Department of Medicine, University of California Irvine School of Medicine, Orange, CA, USA.
² Chao Family Comprehensive Cancer Center, Orange, CA, USA.
³ St. Marianna University School of Medicine, Kawasaki, Japan.

Abstract

KRAS^G12C is one of the most common oncogenes in non-small cell lung cancer (NSCLC) and is associated with a poor prognosis. Historically, KRAS mutations have been difficult to target due to lack of binding sites and exceptionally high affinity for guanosine triphosphate/guanosine diphosphate (GTP/GDP). Recently, KRAS^G12C selective inhibitors have shown promising results in Phase I/II studies. Here we discuss the mechanism of action, pharmacokinetic and pharmacodynamic properties, efficacy, and tolerability of adagrasib (MRTX849).

Keywords: KRAS; MRTX849; non-small cell lung cancer; targeted therapy.

Publication types

Review

Grants and funding

No funding was secured for this report.