gefitinib + zoledronic acid

Gefitinib + zoledronic acid is a combination therapy that shows cooperative antitumor effects, particularly in non-small cell lung cancer (NSCLC) with EGFR mutations. Gefitinib is an EGFR tyrosine kinase inhibitor that causes cell cycle arrest in the G0/G1 phase and induces apoptosis by inhibiting ERK1/2 and Akt protein phosphorylation. Zoledronic acid is a nitrogen-containing bisphosphonate that induces S phase accumulation and inhibits STAT3 activation. When combined, these drugs synergistically inhibit ERK1/2, Akt, and STAT3 signaling pathways, which are major pathways of EGFR. The combination has shown increased efficacy against NSCLC with EGFR activating mutations and TKI resistance both in vitro and in vivo, with effects including enhanced apoptosis induction, regulation of mitogenic factors, proangiogenic factors, and cell cycle controllers.

Other names

gefitinib + zoledronic acid