[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/) › Dasatinib

# 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.

Updated Nov 1, 2026

Also called: BMS-354825

## Quick facts

**Group**
[Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/)

**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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**BCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases**Dasatinib

ⓘ The crystal shows dasatinib in the ATP pocket of the activated human ABL kinase domain.

**Target in 3D:** BCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases. PDB structure 2GQG (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/2GQG) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/chronic-myeloid-leukaemia/)
- Philadelphia-positive acute lymphoblastic leukaemia (adults after other treatment; children with chemotherapy). [Acute leukaemia (AML and ALL) →](https://durgical.com/en/conditions/acute-leukaemia/)

## Adverse effects

### Common

- Myelosuppression
- Fluid retention
- Diarrhoea, nausea
- Headache, fatigue
- Rash
- Breathlessness
- Musculoskeletal pain

### Serious (rare, important)

- Pleural effusion (sometimes severe)
- Pulmonary arterial hypertension
- Bleeding, including gastrointestinal and brain bleeding, with low platelets
- QT prolongation and other cardiac events
- Severe skin reactions
- Tumour lysis syndrome
- Hepatotoxicity
- Growth and bone effects in children

## 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.

## Memory aid

«DaSatinib = Dual SRC + ABL, and Drowns the lungs» (pleural effusion, pulmonary hypertension). Keep acid blockers away.

## 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.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/dasatinib/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**High alert**
An error with this medicine can cause serious harm: double checks and protocols are used.

## Connections

## Related drugs 2

- [Imatinib](https://durgical.com/en/pharmacology/imatinib/)
- [Nilotinib](https://durgical.com/en/pharmacology/nilotinib/)

## Related conditions 2

- [Chronic myeloid leukaemia](https://durgical.com/en/conditions/chronic-myeloid-leukaemia/)
- [Acute leukaemia (AML and ALL)](https://durgical.com/en/conditions/acute-leukaemia/)

[← Back to the class: Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/)

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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bffb38c3-f556-492f-a9db-aa417ec0a856) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EA02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/) (World Health Organization, 2025).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/dasatinib/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/dasatinib/