linifanib + erlotinib

**Linifanib + erlotinib** is an investigational oral combination therapy composed of linifanib (a small molecule inhibitor of vascular endothelial growth factor receptor [VEGFR] and platelet-derived growth factor receptor [PDGFR] tyrosine kinases) and erlotinib (a small molecule epidermal growth factor receptor [EGFR] tyrosine kinase inhibitor)[2]. Linifanib inhibits angiogenesis and tumor growth by blocking VEGFR and PDGFR signaling[2], while erlotinib inhibits cancer cell proliferation by blocking EGFR signaling. Preclinical rationale for their combination is based on the potential to provide broader inhibition of parallel signaling pathways involved in tumor growth and resistance mechanisms in cancers such as non-small-cell lung cancer (NSCLC)[1][3][5]. Clinical development has focused mainly on NSCLC, but pivotal studies with a very similar combination (using linsitinib instead of linifanib) showed that the addition of IGF-1R/insulin receptor inhibition (closely related mechanistically) to EGFR inhibition did not improve efficacy and increased toxicity[1][5]. For linifanib + erlotinib specifically, there is no evidence of successful late-phase clinical activity or approval; any trials were likely terminated before marketing.

Brand names

Tarceva

Other names

linifanib + erlotinib