[Comment] KRASG12C inhibitor combination therapy in metastatic non-small-cell lung cancer: choosing the right path
Summary
KRAS has long been regarded as an indomitable oncogenic driver which defines a distinct and therapeutically elusive class of solid tumours. The recent advent of direct KRAS inhibitors has fundamentally altered the drug development landscape of KRAS-mutated tumours, including non-small-cell lung cancer (NSCLC). The first entrants in this class used a unique mechanism of action which inhibited KRASG12C by irreversibly…
KRAS has long been regarded as an indomitable oncogenic driver which defines a distinct and therapeutically elusive class of solid tumours. The recent advent of direct KRAS inhibitors has fundamentally altered the drug development landscape of KRAS-mutated tumours, including non-small-cell lung cancer (NSCLC). The first entrants in this class used a unique mechanism of action which inhibited KRASG12C by irreversibly binding to its inactive GDP-bound conformation at the switch-II binding pocket (KRASG12C[OFF] inhibitors).