Drug intelligence / Profile preview

cediranib + gefitinib

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Cediranib + gefitinib is an investigational oral combination therapy consisting of two small molecule tyrosine kinase inhibitors. Cediranib is a potent inhibitor of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), targeting angiogenesis pathways critical for tumor blood vessel formation. Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR-mediated signaling involved in cell proliferation and survival. The rationale for combining these agents stems from preclinical and clinical evidence suggesting synergistic antitumor effects by simultaneously inhibiting both VEGF-driven angiogenesis and EGFR-driven tumor cell proliferation. This combination has been studied primarily in patients with recurrent or progressive glioblastoma and advanced solid tumors[1][2][3]. Clinical trials have shown the regimen to be generally well tolerated with manageable side effects such as diarrhea, anorexia, and fatigue; efficacy signals include partial responses and stable disease in a subset of patients[2]. Recruitment to some studies was limited due to early program suspension[1].

Other names
cediranib maleate + gefitinib
02

Targets

EGFR (Epidermal growth factor receptor)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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