erlotinib + metformin

Erlotinib + metformin is an investigational combination therapy consisting of erlotinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and metformin, a biguanide antidiabetic agent. Erlotinib inhibits EGFR signaling by blocking its tyrosine kinase activity, thereby suppressing downstream pathways involved in cell proliferation and survival. Metformin primarily acts by inhibiting mitochondrial complex I, leading to activation of AMP-activated protein kinase (AMPK), which in turn inhibits the mTOR pathway and reduces cellular proliferation. Preclinical studies have shown that this combination can synergistically induce apoptosis and inhibit tumor growth in basal-like breast cancer models with EGFR overexpression or PTEN loss. Clinical studies have evaluated the safety and tolerability of this combination in metastatic triple-negative breast cancer (mTNBC), but efficacy has not been demonstrated in this population[1][2]. The rationale for combining these agents is to overcome resistance to EGFR inhibition by targeting both upstream receptor signaling (EGFR) and downstream metabolic/proliferative pathways (MAPK/PI3K/mTOR).

Other names

Metformin and Erlotinib combination therapyErlotinib and Metformin in Triple Negative Breast Cancer