Resistance to Targeted Therapies As a Result of Mutation(s) in the Target

摘要: Tyrosine kinase inhibitors (TKIs) are effective clinical therapies in a subset of malignancies defined by oncogenic alterations. Compelling examples include EGFR mutant non-small cell lung cancer and chronic myeloid leukemia. Unfortunately, the effectiveness these treatments is ultimately limited due to development drug resistance most commonly mediated secondary mutations. These mutations often occur at gatekeeper residue, like T315I mutation BCR-ABL or T790M EGFR, but it can also outside residue. In this chapter, we will address different types mechanisms which they confer TKI. We discuss therapeutic strategies developed overcome