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Erlotinib (Tarceva)

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

About Erlotinib

What it is

Erlotinib is a targeted cancer medicine, an EGFR tyrosine kinase inhibitor: it blocks the growth signal from the EGFR protein on cancer cells. It is used for non-small cell lung cancer whose tumour carries activating EGFR mutations, and with gemcitabine for pancreatic cancer. A skin rash is its most common side effect. It is sold as Tarceva.

How genes come into it

Whether erlotinib works depends above all on EGFR mutations in the tumour, such as exon 19 deletions and L858R, while T790M (rs121434569) is linked to resistance. These arise in the cancer and are found in tumour tissue, not in the DNA a person was born with. For inherited genes, erlotinib is broken down by CYP3A4 and CYP1A2 (sped up by smoking), and studies have looked at ABCB1 and EGFR variants for rash and diarrhoea. There is no CPIC or DPWG guideline.

What research found

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

Rated evidence (5 rated variants)

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

EGFR rs121434569: Level 2B · replicated. Efficacy: Adenocarcinoma, Drug Resistance, Lung Neoplasms, Non-Small Cell Lung Carcinoma. 11.

EGFR rs712829: Level 3. Efficacy: Neoplasms. 1.

EGFR rs712829: Level 3. Toxicity: Neoplasms. 1.

MAP3K1 rs726501: Level 3. Efficacy. 1.

Metabolism (1 finding)

Studies of how quickly the body processes this medication.

CYP1A2 rs2472304: Genotypes AA + AG is associated with increased concentrations of erlotinib in healthy individuals as compared to genotype GG.

Response (3 findings)

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

EGFR rs121434568: Genotypes GT + TT are associated with decreased response to erlotinib in people with Carcinoma, Non-Small-Cell Lung as compared to genotype GG.

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 erlotinib in people with Carcinoma, Non-Small-Cell Lung.

Side effects (3 findings)

Studies of side effects in people carrying a variant.

ABCB1 rs1045642: Genotype AA is associated with decreased clearance of erlotinib in people with Carcinoma, Non-Small-Cell Lung.

ABCB1 rs1128503: Genotype AA is associated with decreased clearance of erlotinib in people with Carcinoma, Non-Small-Cell Lung.

ABCB1 rs2032582: Genotype AA is associated with decreased clearance of erlotinib in people with Carcinoma, Non-Small-Cell Lung.

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)

Iressa (EGFR Inhibitors)

Tagrisso (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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