erlotinib + azacitidine

Erlotinib + azacitidine is an investigational combination of two small molecule drugs with antineoplastic activity, studied primarily in hematologic malignancies such as myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML). Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling, thereby inhibiting cancer cell proliferation. Azacitidine is a pyrimidine nucleoside analogue that incorporates into RNA and DNA, disrupting their function and inhibiting DNA methyltransferase, leading to hypomethylation of DNA and reactivation of tumor suppressor genes. Preclinical studies have shown that this combination exerts synergistic effects by blocking cell-cycle progression and inducing caspase-dependent apoptosis more effectively than either agent alone. The synergy involves proteasomal degradation of anti-apoptotic proteins MCL-1 and BCL2L10, upregulation of pro-apoptotic PUMA, and increased intracellular accumulation of azacitidine when combined with erlotinib[1]. This regimen remains experimental but has demonstrated promising cytotoxic responses in AML/MDS models.

Other names

5-azacytidine + erlotinibazacitidine + erlotinib5-azacytidine and erlotinib hydrochloride