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Imatinib (Gleevec)

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

About Imatinib

What it is

Imatinib was the first targeted tyrosine kinase inhibitor and transformed the outlook of chronic myeloid leukaemia (CML). It blocks BCR-ABL, the abnormal fusion protein that drives CML, and also KIT, which drives gastrointestinal stromal tumours (GIST). It is used for CML, GIST and some other blood cancers. It is sold as Gleevec and Glivec, among other names.

How genes come into it

Whether imatinib works depends above all on the BCR-ABL fusion and KIT mutations in the cancer cells, which arise in the tumour and are not part of the DNA a person was born with. For inherited genes, studies have looked at the transporters that move imatinib in and out of cells (ABCB1, ABCG2, SLC22A1) and at the enzymes CYP3A4, CYP3A5 and CYP2C8, for blood levels and response, with mixed results. There is no CPIC or DPWG guideline.

What research found

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

Rated evidence (39 rated variants)

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

ABCB1 rs1045642: Level 3. Efficacy: Chronic myelogenous leukemia, BCR-ABL1 positive. 5.

SLC22A1 rs628031: Level 3. Efficacy, Toxicity, Metabolism/PK: Neoplasms. 4.

ABCB1 rs1128503: Level 3. Efficacy: Chronic myelogenous leukemia, BCR-ABL1 positive. 3.

SLC22A4 rs1050152: Level 3. Efficacy: Chronic myelogenous leukemia, BCR-ABL1 positive, Gastrointestinal Stromal Tumors. 2.

Metabolism (23 findings)

Studies of how quickly the body processes this medication.

ABCB1 rs1045642: Genotype AG is associated with decreased trough concentration of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + GG.

ABCB1 rs1045642: Genotype AA is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AG + GG.

ABCB1 rs1045642: Genotype AA is associated with increased concentrations of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AG + GG.

ABCB1 rs1045642: Genotypes AG + GG is associated with increased trough concentration of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype AA.

Response (64 findings)

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

ABCA3 rs150929: Genotypes GG + GT is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype TT.

ABCB1 rs1045642: Allele A is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele G.

ABCB1 rs1045642: Genotype AA is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AG + GG.

ABCB1 rs1045642: Genotype GG is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + AG.

Dosing (36 findings)

Studies of how much of the drug people needed or tolerated.

ABCG2 rs2231137: Genotypes CT + TT are associated with decreased dose of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype CC.

CYP1A2 rs762551: Genotype CC is associated with decreased dose of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AA + AC.

ABCB1 rs1045642: Allele G is not associated with dose of imatinib in people with Gastrointestinal Stromal Tumors as compared to allele A.

ABCB1 rs28656907: Genotype TT is associated with increased dose of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes CC + CT.

Side effects (3 findings)

Studies of side effects in people carrying a variant.

SLCO1A2 rs4148978: Genotypes CT + TT is associated with increased dose-adjusted trough concentrations of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype CC.

SLCO1B3 rs4149117: Genotype GG is associated with increased dose-adjusted trough concentrations of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes GT + TT.

ABCB1 rs1128503: Allele A is associated with increased dose-adjusted trough concentrations of imatinib in people with Gastrointestinal Stromal Tumors 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

Apatinib (Tyrosine Kinase Inhibitors)

Gilotrif (Tyrosine Kinase Inhibitors)

Inlyta (Tyrosine Kinase 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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