erlotinib + tivantinib

Erlotinib + tivantinib is a combination of two small molecule inhibitors used in clinical trials for the treatment of non-small cell lung cancer (NSCLC). Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, while tivantinib is a selective MET receptor tyrosine kinase inhibitor. The rationale for combining these agents stems from evidence that activation of the MET pathway can confer resistance to EGFR inhibitors; thus, dual inhibition may overcome or delay resistance and improve outcomes in NSCLC patients. Multiple phase II and III studies have evaluated this combination, particularly in previously treated patients with advanced nonsquamous NSCLC. While the combination increased progression-free survival compared to erlotinib alone, it did not significantly improve overall survival in unselected populations. Some exploratory analyses suggested potential benefit in subgroups with high MET expression or KRAS mutations[1][2][6]. The development program was discontinued after phase III trials failed to meet primary endpoints.

Brand names

Tarceva

Other names

erlotinib plus tivantinibE + T