Imatinib

Gleevec, Imkeldi

Antineoplastic • Tyrosine kinase inhibitor

Premium

QT RiskHepatotoxicNephrotoxic

Half-life

18 hours (40 hours for active metabolite)

Protein Binding

95%

Metabolized By

CYP3A4, CYP1A2, CYP2D6, CYP2C9, CYP2C19

External

Drugs.com

Boxed warning

Hepatotoxicity
Fluid retention (pleural effusion, ascites)

Clinical alerts

Boxed warning

2 boxed warnings

QT prolongation

Avoid combining with other QT-prolonging agents; check electrolytes

Nephrotoxic

Monitor renal function; avoid other nephrotoxins where possible

Hepatotoxic

Monitor liver function

Mechanism of action

Inhibits BCR-ABL, c-KIT, and PDGFR tyrosine kinases

Recorded indications

From the drug index — may include conditions studied rather than approved indications

·GIST
·Gastrointestinal Stromal Tumor(GIST)
·Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive
·Minimal Residual Disease
·Gastrointestinal Neoplasms

Monitoring

Therapeutic range: 1–3 mg/L; Cmin > 1.0 mg/L

Interactions

2 curated · 1 major or contraindicated · select a row for management

Interacting drug	Severity	Effect
rifampicin	major	Loss of tyrosine kinase inhibition; risk of cancer progression.
omeprazole	moderate	Reduced imatinib efficacy; potential treatment failure

Common adverse effects

Edema
Nausea
Muscle cramps
Diarrhea
Rash
Myelosuppression

Food, alcohol & herbal

Food

Take with food to reduce GI irritation

Alcohol · moderate

Additive hepatotoxicity

Herbal

St. John's Wort (major) — Significantly reduces imatinib levels

Pharmacokinetics

Published parameters · PMID:15180075

Half-life: 18 hours (40 hours for active metabolite)
Protein binding: 95%
Metabolised by: CYP3A4
Inhibits: CYP3A4, CYP2D6, CYP2C9
Clearance: 12 L/h; adult CML patients
Volume of distribution: 250 L
Bioavailability: 98%
Renally eliminated: 13%
Model: 1-compartment

Pregnancy & lactation

Not recorded for Imatinib. Absence here means this database does not hold a category — not that the drug is safe in pregnancy or breastfeeding.

Sources

Assembled from: drug index, curated drug database, curated interaction pairs, published PK literature.

Not a substitute for clinical judgement

Imatinib

Gleevec, Imkeldi

Antineoplastic • Tyrosine kinase inhibitor

Premium

QT RiskHepatotoxicNephrotoxic

Half-life

18 hours (40 hours for active metabolite)

Protein Binding

95%

Metabolized By

CYP3A4, CYP1A2, CYP2D6, CYP2C9, CYP2C19

External

Drugs.com

Boxed warning

Hepatotoxicity
Fluid retention (pleural effusion, ascites)

Clinical alerts

Boxed warning

2 boxed warnings

QT prolongation

Avoid combining with other QT-prolonging agents; check electrolytes

Nephrotoxic

Monitor renal function; avoid other nephrotoxins where possible

Hepatotoxic

Monitor liver function

Mechanism of action

Inhibits BCR-ABL, c-KIT, and PDGFR tyrosine kinases

Recorded indications

From the drug index — may include conditions studied rather than approved indications

·GIST
·Gastrointestinal Stromal Tumor(GIST)
·Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive
·Minimal Residual Disease
·Gastrointestinal Neoplasms

Monitoring

Therapeutic range: 1–3 mg/L; Cmin > 1.0 mg/L

Interactions

2 curated · 1 major or contraindicated · select a row for management

Interacting drug	Severity	Effect
rifampicin	major	Loss of tyrosine kinase inhibition; risk of cancer progression.
omeprazole	moderate	Reduced imatinib efficacy; potential treatment failure

Common adverse effects

Edema
Nausea
Muscle cramps
Diarrhea
Rash
Myelosuppression

Food, alcohol & herbal

Food

Take with food to reduce GI irritation

Alcohol · moderate

Additive hepatotoxicity

Herbal

St. John's Wort (major) — Significantly reduces imatinib levels

Pharmacokinetics

Published parameters · PMID:15180075

Half-life: 18 hours (40 hours for active metabolite)
Protein binding: 95%
Metabolised by: CYP3A4
Inhibits: CYP3A4, CYP2D6, CYP2C9
Clearance: 12 L/h; adult CML patients
Volume of distribution: 250 L
Bioavailability: 98%
Renally eliminated: 13%
Model: 1-compartment

Pregnancy & lactation

Not recorded for Imatinib. Absence here means this database does not hold a category — not that the drug is safe in pregnancy or breastfeeding.

Sources

Assembled from: drug index, curated drug database, curated interaction pairs, published PK literature.

Not a substitute for clinical judgement

Imatinib Drug Profile | PharmaGraphX