Lumakras (sotorasib) broke a barrier that had stood for nearly four decades, arriving as the first KRAS inhibitor ever approved for a target long considered undruggable.
Sotorasib binds irreversibly to a pocket present only in the mutant protein, locking KRAS G12C in its inactive state. The once-daily tablet treats adults with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer after at least one prior systemic therapy.
Lumakras remains under an ongoing accelerated approval, and its confirmatory CodeBreaK 200 data drew FDA scrutiny including a dose-comparison requirement. It is the reference KRAS G12C agent and the primary benchmark against which later entrants are measured.
