Drug intelligence / Profile preview

gefitinib + icotinib

Development stage
Preclinical
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

Gefitinib + icotinib is a combination of two first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), both used primarily in the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations. Gefitinib and icotinib selectively inhibit the EGFR tyrosine kinase domain, blocking downstream signaling pathways involved in tumor cell proliferation and survival. Both drugs are small molecules that act by competitively binding to the ATP-binding site of EGFR, thereby inhibiting its autophosphorylation and subsequent activation of signal transduction cascades. This combination has been proposed as a potential synergistic regimen for targeting cancer-associated proteins/genes in NSCLC, particularly lung adenocarcinoma[1][2][3][4][5]. Each drug individually has demonstrated efficacy as monotherapy; their combined use is under investigation for enhanced therapeutic benefit.

Brand names
Iressa (for gefitinib)Conmana (for icotinib)
Other names
gefitinib + icotinib
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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