Apatinib + EGFR-TKI

Apatinib + EGFR-TKI is a combination therapy being investigated for non-small cell lung cancer (NSCLC), particularly for patients who have developed resistance to EGFR-TKI monotherapy. The combination pairs apatinib, an oral tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor-2 (VEGFR-2), with epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) such as erlotinib, gefitinib, icotinib, or osimertinib. This approach aims to overcome acquired resistance to EGFR-TKI therapy by simultaneously targeting both the VEGFR and EGFR signaling pathways. The rationale is based on the observation that resistance to EGFR inhibitors is often associated with increased VEGF levels. Dual inhibition is hypothesized to provide synergistic effects in controlling tumor growth and delaying disease progression. Clinical trials have explored this combination in various NSCLC settings, including patients with slow progression after first-line EGFR-TKI treatment, those with osimertinib-refractory EGFR-positive disease, and patients with advanced NSCLC with wild-type EGFR. Clinical evidence suggests improvements in the duration of first-generation EGFR-TKI use and better objective response rates (ORR) and disease control rates (DCR) when combined with osimertinib in refractory cases. Common adverse events include hypertension, diarrhea, and proteinuria. Less common events like rash, hand-foot syndrome, hoarseness, thrombocytopenia, and liver dysfunction have also been reported. A notable severe adverse event leading to discontinuation was tachycardia and decreased left ventricular ejection fraction.

Other names

Combination of apatinib and EGFR-TKI