Gefitinib: a targeted therapy for NSCLC

Non-small cell lung cancer targeted therapy

Gefitinib, a small molecule tyrosine kinase inhibitor, is a targeted therapy for the treatment of patients with non-small cell lung cancer

• Targeted therapy acts predominantly against tumour cells
• Gefitinib acts against EGFR by inhibiting the tyrosine kinase domain of the molecule
• This blocks the signalling pathways that are initiated by EGFR

Non-small cell lung cancer personalised therapy

EGFR mutations found in the tyrosine kinase domain of EGFR are a type of mutation that is associated with tumour cells and not healthy cells – also known as somatic mutations.

For non-small cell lung cancer (NSCLC) patients who harbour these EGFR mutations, gefitinib binds to the EGFR TK domain with high specificity and affinity resulting in highly effective inhibition of the aberrant signalling pathways.

• This leads to significant tumour shrinkage in many patients

Through targeting mutations in the EGFR as a personalised medicine, gefitinib is transforming the treatment of non-small cell lung cancer.

Doroshow 2005

Gefitinib Product Information

You can view an animation of the gefitinib mode of action here 

Next: The effect of EGFR mutations