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Gefitinib (Iressa)

Raw research findings for this medication. Mostly single studies, not curated or confirmed robust.

About Gefitinib

What it is

Gefitinib is a targeted cancer medicine, an EGFR tyrosine kinase inhibitor: it blocks the growth signal sent by the EGFR protein on cancer cells. It is used for non-small cell lung cancer whose tumour carries particular EGFR mutations. It is sold as Iressa.

How genes come into it

Whether gefitinib works depends above all on EGFR mutations in the tumour itself, such as L858R (rs121434568) and exon 19 deletions; T790M (rs121434569) is linked to resistance. These arise in the cancer and are found by testing tumour tissue, not in the DNA a person was born with. For inherited genes, the US FDA notes that CYP2D6 poor metabolizers have higher gefitinib levels. Studies have also looked at the transporters ABCB1 and ABCG2 and at CYP3A enzymes, with weaker evidence.

Published guidelines

Clinical guidelines that name a gene for Gefitinib. They sort people into groups by the gene copies they carry.

US FDA: CYP2D6. CYP2D6 activity score 0.

US FDA: CYP2D6. CYP2D6 activity score 0. Data that Support Therapeutic Management Recommendations.

What research found

Every published finding on gene variants and Gefitinib. Upload your DNA file to see which of these rows apply to you.

Rated evidence (22 rated variants)

PharmGKB weighs all studies of a variant and rates how strong the evidence is, from 1A (strongest) to 4.

EGFR rs121434568: Level 1A · replicated. Efficacy: Non-Small Cell Lung Carcinoma. 24.

EGFR rs121434569: Level 2B · replicated. Efficacy: Drug Resistance, Non-Small Cell Lung Carcinoma. 16.

CYP2D6 CYP2D6*1, CYP2D6*2, CYP2D6*5, CYP2D6*10: Level 3. Toxicity: Adenocarcinoma, Drug Toxicity, Exanthema, Non-Small Cell Lung Carcinoma, Toxic liver disease. 5.

EGFR rs11568315: Level 3. Efficacy: Non-Small Cell Lung Carcinoma. 4.

Metabolism (20 findings)

Studies of how quickly the body processes this medication.

CYP2C9 rs1057910: Genotype AC is associated with increased concentrations of gefitinib in healthy individuals as compared to genotype AA.

CYP2D6 CYP2D6*1, CYP2D6*2, CYP2D6*3, CYP2D6*4, CYP2D6*4xN, CYP2D6*5, CYP2D6*6, CYP2D6*41: CYP2D6 *4/*4 + *4/*5 + *3/*4 + *4/*6 + *3/*5 + *4/*4xN (assigned as poor metabolizer phenotype) is associated with increased concentrations of gefitinib in healthy individuals as compared to CYP2D6 *1/*4 + *1/*2 + *2/*4 + *1/*3 + *2/*5 + *2/*41 (assigned as normal metabolizer phenotype) .

CYP3A5 rs776746: Genotype CC is associated with increased concentrations of gefitinib in healthy individuals as compared to genotypes CT + TT.

ABCB1 rs1045642: Genotype GG are not associated with concentrations of gefitinib in people with Carcinoma, Non-Small-Cell Lung as compared to genotypes AA + AG.

Response (6 findings)

Studies of how well it worked in people carrying a variant.

EGFR rs121434568: Allele G is associated with decreased response to erlotinib or gefitinib in people with Carcinoma, Non-Small-Cell Lung as compared to allele T.

EGFR rs121434568: Allele G is associated with response to gefitinib in people with Carcinoma, Non-Small-Cell Lung.

EGFR rs121434568: Genotype GT is associated with increased response to gefitinib in people with Carcinoma, Non-Small-Cell Lung as compared to genotype TT.

ABCG2 rs2231142: Allele T is not associated with decreased response to gefitinib in people with Non-Small Cell Lung Carcinoma as compared to allele G.

Study findings and evidence levels: PharmGKB (CC BY-SA 4.0). Guidelines: CPIC and DPWG, as bundled in PharmCAT. Most studies were done mainly in people of European ancestry.

Related Drugs

More drugs from the same category

Erbitux (EGFR Inhibitors)

Tagrisso (EGFR Inhibitors)

Tarceva (EGFR Inhibitors)

Not a prescribing recommendation. This page is educational information about pharmacogenomic research and clinical guidelines - it is not medical or dosing advice, and not a prediction of how any medication will work for you. Never start, stop, or change a medication or dose based on it; talk to your doctor or pharmacist, who can order clinical-grade testing if appropriate.

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Content updated September 2026.

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