In a preclinical study presented at the EORTC-NCI-AACR meeting, a compound known as XL184 (Exelixis), showed
encouraging results in boosting sensitivity to erlotinib (Tarceva) and gefitinib
(Iressa) in drug-resistant lung cancer.
Gefitinib and erlotinib belong to a
class of targeted drugs that target the epidermal growth factor
receptor (EGFR) gene, which is mutated in many non-small cell lung
MET kinase, which is inhibited by XL184, is implicated in the
resistance to EGFR kinase inhibitors. This approach potentially has the opportunity to turn the resistance mechanisms off, thereby allowing Tarceva to work more effectively in NSCLC when taken in combination with a MET kinase inhibitor such as XL184.