Dasatinib
Kinase inhibitors (targeted oncology)
Kinase inhibitors (targeted oncology)High alert
An error with this medicine can cause serious harm: double checks and protocols are used.
A second-generation BCR-ABL and SRC inhibitor for CML and Ph-positive ALL, including after imatinib failure; known for pleural effusions.
Also called: BMS-354825
Quick facts
- Group
- Kinase inhibitors (targeted oncology)
- Target
- BCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases
- Key effects
- Myelosuppression · Fluid retention · Diarrhoea
- Monitor
- Complete blood count regularly · Breathlessness
- ATC
- L01EA02
No doses: the clinician sets them by the current guideline.
Mechanism of action
The crystal shows dasatinib in the ATP pocket of the activated human ABL kinase domain.
Dasatinib inhibits BCR-ABL at very low concentrations and also the SRC-family kinases, KIT, EPHA2 and PDGFRβ. Unlike imatinib it binds both the active (open) and inactive conformations of ABL, which lets it overcome many imatinib-resistance mutations; it does not overcome T315I. Blocking BCR-ABL stops leukaemic proliferation and triggers apoptosis.
- Binds ABL in active and inactive shapes
- Inhibits BCR-ABL, SRC kinases, KIT and PDGFRβ
- Overcomes most imatinib-resistance mutations (not T315I)
- Leukaemic cells stop dividing and die
Indications
- Philadelphia-positive chronic myeloid leukaemia: newly diagnosed chronic phase, or any phase after resistance or intolerance to imatinib. Chronic myeloid leukaemia →
- Philadelphia-positive acute lymphoblastic leukaemia (adults after other treatment; children with chemotherapy). Acute leukaemia (AML and ALL) →
Adverse effects
Common
- Myelosuppression
- Fluid retention
- Diarrhoea, nausea
- Headache, fatigue
- Rash
- Breathlessness
- Musculoskeletal pain
Contraindications
- No absolute contraindications in the label; caution with QT prolongation, bleeding risk and lung disease
Key interactions
- Proton pump inhibitors and H2 blockers
- Reduce dasatinib absorption; avoided (short-acting antacids may be used, but not at the same time).
- Strong CYP3A4 inhibitors and inducers
- Inhibitors raise and inducers lower dasatinib levels.
- Antiplatelet drugs and anticoagulants
- Higher bleeding risk, especially with low platelets.
What is monitored
- Complete blood count regularly
- Breathlessness, cough or chest pain (effusion, pulmonary hypertension); chest X-ray or echo when symptoms appear
- Weight and oedema
- ECG and electrolytes if QT risk
- Liver tests
- BCR-ABL molecular response
Administration and safety
- Oral, with or without food, swallowed whole.
- Not taken together with antacids; proton pump inhibitors and H2 blockers are avoided.
- Check the name: dasatinib is not interchangeable with imatinib or nilotinib.
Pregnancy and breastfeeding
Can harm the fetus; effective contraception is used during treatment and breastfeeding is not advised.
Nursing care
- Ask about breathlessness, cough, chest pain and leg swelling at every visit; weigh the patient.
- Review platelet and neutrophil counts; look for bleeding or bruising.
- Review the medicine list for acid-reducing drugs and anticoagulants.
- Teaching: report breathlessness, bleeding or fever; use contraception and do not breastfeed.
Pharmacokinetics
- Absorption
- Oral; absorption falls at higher gastric pH (antacids, H2 blockers, proton pump inhibitors); food has little effect.
- Distribution
- Highly bound to plasma proteins.
- Metabolism
- Liver, mainly CYP3A4.
- Elimination
- Mainly in the faeces.
- Half-life
- Short: about 3 to 5 hours.
Test yourself
Think of the answer, then tap the question to see it.
What distinguishes dasatinib's binding from imatinib's?
Dasatinib binds both the active and inactive ABL conformations (and also inhibits SRC kinases).
A patient on dasatinib reports progressive breathlessness. What two complications are suspected?
Pleural effusion and pulmonary arterial hypertension.
Why should omeprazole be avoided with dasatinib?
Raising gastric pH reduces dasatinib absorption.
Connections
← Back to the class: Kinase inhibitors (targeted oncology)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - DASATINIB tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).
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Representative model, for educational purposes only.