Rociletinib—An Investigational Therapy in Patients with Previously Treated EGFR Mutant-positive Non-small Cell Lung Cancer

Treatment for patients with non-small cell lung cancer (NSCLC) is being guided increasingly by driver mutations and, routinely, tumors from patients with adenocarcinoma are screened for mutations in the kinase domain of the epidermal growth factor receptor (EGFR) as well as for other genomic abnormalities (i.e. anaplastic lymphoma kinase [ALK] and ROS1 translocations). Effective, well-tolerated treatment options that specifically target the EGFR T790M mutation (the “gatekeeper” residue) in patients with NSCLC remains an unmet need. Rociletinib is an oral, irreversible, potent, covalent inhibitor of the activating EGFR mutations (del19 and L858R) and the T790M resistance mutation; it also spares wild-type EGFR. TIGER-X is the first of the TIGER trial series, which is a clinical development program for rociletinib in patients with mutant EGFR NSCLC. This phase I–II study is evaluating rociletinib in patients who have progressed following their first and only EGFR-directed tyrosine kinase inhibitor (TKI) therapy who have developed the T790M mutat