Dual-State KRAS G12C Inhibitors as Emerging Therapeutics for Brain and Lung Metastases.
New-generation KRAS G12C inhibitors demonstrate enhanced activity in both peripheral and central nervous system malignancies.
APA
Renner AC, Kargbo RB (2025). Dual-State KRAS G12C Inhibitors as Emerging Therapeutics for Brain and Lung Metastases.. ACS medicinal chemistry letters, 16(12), 2389-2391. https://doi.org/10.1021/acsmedchemlett.5c00662
MLA
Renner AC, et al.. "Dual-State KRAS G12C Inhibitors as Emerging Therapeutics for Brain and Lung Metastases.." ACS medicinal chemistry letters, vol. 16, no. 12, 2025, pp. 2389-2391.
PMID
41403995
Abstract
New-generation KRAS G12C inhibitors demonstrate enhanced activity in both peripheral and central nervous system malignancies. Frontier Medicines' pyridopyrimidines and Novartis's spiro-indazole inhibitor (opnurasib) overcome resistance mechanisms by targeting both GDP- and GTP-bound KRAS states. Their blood-brain barrier permeability and synergy with immune checkpoint inhibitors represent a transformative advance for KRAS-driven cancers, especially metastatic nonsmall cell lung cancer (NSCLC).