Merck

Last updated January 31, 2026

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Macrocyclic and small molecule kras-g12-specific inhibitors: MerckRecent Research Landscape

The G12C mutation renders the KRAS protein constitutively active, driving uncontrolled oncogenic signaling and therapeutic resistance. These innovations utilize electrophilic small molecules to irreversibly bind the mutant cysteine residue, locking the protein in its inactive state.

What technical problems is Merck addressing in Macrocyclic and small molecule kras-g12-specific inhibitors?

Oncogenic kras mutant hyperactivation

(8)evidences

Constitutive activation of mutant KRAS isoforms drives uncontrolled cellular proliferation. Neutralizing this specific biochemical signaling failure prevents tumor progression.

Oncogenic kras g12c hyperactivation

(6)evidences

Ineffective inhibition of mutated signaling proteins due to structural instability or weak binding affinity. Overcoming these limitations prevents uncontrolled cellular proliferation in resistant cancer phenotypes.