Towards better outcomes for epidermal growth factor receptor L858R+ lung cancer patients: mutant-selective allosteric inhibitors and the potential for double-drugging.

Abstract excerpt

Mutations in the kinase domain of the epidermal growth factor receptor (EGFR) are a frequent cause of non-small cell lung cancer (NSCLC). Osimertinib, a third-generation tyrosine kinase inhibitor (TKI) that is selective for mutant EGFR, is standard of care for patients with the classical exon 19 deletion variants and the L858R point mutation. Although osimertinib and a recently developed therapy that combines TKI...

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