dovitinib + erlotinib

Dovitinib + erlotinib is a combination of two small molecule tyrosine kinase inhibitors used experimentally in cancer treatment, specifically metastatic non-small cell lung cancer (NSCLC). Erlotinib is an FDA-approved inhibitor targeting the epidermal growth factor receptor (EGFR), while dovitinib is a novel inhibitor targeting fibroblast growth factor receptors (FGFR) and vascular endothelial growth factor receptors (VEGFR). The combination was studied to evaluate safety, tolerability, maximum tolerated dose, and pharmacokinetic interactions. Dovitinib induces CYP1A1/1A2 enzymes which significantly reduce the plasma concentration of erlotinib when co-administered. The combination showed considerable toxicity including dose-limiting toxicities such as transaminitis, syncope, pulmonary embolism, and fatigue. Due to these toxicities and significant pharmacokinetic interaction leading to decreased erlotinib exposure, further development of this drug combination has been discontinued[1][2].

Brand names

Tarceva

Other names

TKI258 + erlotinib