Last December, Adagrasib (KRAZATI) received approval by the FDA as an oral second-line drug for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) in adults.
It is a specific, irreversible inhibitor of KRAS harboring G12C mutation. KRAS is the most commonly mutated isoform of RAS in cancer, including 85% of oncogenic RAS mutations. In the case of NSCLC, KRAS has mutated in around one-third of patients.
Adagrasib has a warhead that permanently binds to the target.
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