[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/) › Bosutinib

# Bosutinib

## 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.

Second-generation BCR-ABL and SRC kinase inhibitor taken by mouth for Ph-positive CML. Diarrhoea is its hallmark; it does not work against T315I.

Updated Nov 1, 2026

## 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**
Diarrhoea · Rash · Tiredness

**Monitor**
Liver enzymes monthly at first · Blood count · Weight

**ATC**
L01EA04

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**Bosutinib

ⓘ The crystal shows bosutinib in the ATP pocket of the human ABL1 kinase domain.

**Target in 3D:** BCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases. PDB structure 3UE4 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/3UE4) · Drag to rotate · pinch to zoom

Bosutinib competes with ATP in the kinase domain of BCR-ABL, the fusion protein made by the Philadelphia chromosome that drives chronic myeloid leukaemia. Blocking it stops the signals that make the leukaemic cells multiply and survive. It also inhibits SRC-family kinases (SRC, LYN, HCK). It inhibits most imatinib-resistant forms of BCR-ABL, but not the T315I and V299L mutants.

- Bosutinib takes ATP's place in the BCR-ABL kinase
- Growth and survival signals of the leukaemic clone stop
- Works on most imatinib-resistant mutants, not on T315I

## Indications

- Chronic-phase Philadelphia chromosome-positive chronic myeloid leukaemia, newly diagnosed or resistant or intolerant to earlier therapy. [Chronic myeloid leukaemia →](https://durgical.com/en/conditions/chronic-myeloid-leukaemia/)
- Accelerated or blast phase Ph-positive chronic myeloid leukaemia after resistance or intolerance to earlier therapy. [Chronic myeloid leukaemia →](https://durgical.com/en/conditions/chronic-myeloid-leukaemia/)

## Adverse effects

### Common

- Diarrhoea (very common, usually early), nausea, vomiting, abdominal pain
- Rash
- Tiredness, headache, fever
- Respiratory infections
- Raised liver enzymes and creatinine

### Serious (rare, important)

- Myelosuppression: thrombocytopenia, anaemia, neutropenia
- Liver toxicity
- Fluid retention: pleural and pericardial effusion, oedema
- Cardiovascular events
- Decline in kidney function

## Contraindications

- Allergy to bosutinib

## Key interactions

**Strong and moderate CYP3A inhibitors (e.g., ketoconazole, grapefruit)**
Raise bosutinib levels and toxicity; avoided.

**Strong CYP3A inducers (e.g., rifampicin, St John's wort)**
Lower bosutinib levels; avoided.

**Proton pump inhibitors**
Reduce absorption; short-acting antacids or H2 blockers are used instead.

## What is monitored

- Liver enzymes monthly at first and then as needed
- Blood count
- Kidney function at baseline and during treatment
- Weight, oedema and breathlessness (fluid retention)

## Administration and safety

- Oral tablet taken once a day with food.
- Swallowed whole: not cut, crushed, broken or chewed.
- Hazardous drug: tablets are handled with care.

## Pregnancy and breastfeeding

Can cause fetal harm; effective contraception is used and breastfeeding is not advised.

## Nursing care

- Plan for diarrhoea from the start: fluids and antidiarrhoeal medicine as ordered; report severe diarrhoea.
- Review all medicines for CYP3A inhibitors, inducers and proton pump inhibitors; avoid grapefruit.
- Weigh the patient and ask about swelling or breathlessness.
- Teach to report yellow skin, bruising, bleeding or fever.

## Pharmacokinetics

**Absorption**
Oral tablet taken with food; acid suppression with proton pump inhibitors lowers absorption.

**Metabolism**
Liver, by CYP3A4.

**Half-life**
About 22 hours.

## Memory aid

BOSUtinib: BOwel trouble first (diarrhoea), SRC as a bonus target, and blind to T315I.

## Test yourself

Think of the answer, then tap the question to see it.

## Which BCR-ABL mutation is not inhibited by bosutinib?

T315I (and also V299L).

## What is the most common adverse effect of bosutinib?

Diarrhoea, usually early in treatment.

## Which acid-reducing drugs should be avoided with bosutinib, and what can be used instead?

Proton pump inhibitors; short-acting antacids or H2 blockers are used instead.

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

[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 4

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

## Related conditions 1

- [Chronic myeloid leukaemia](https://durgical.com/en/conditions/chronic-myeloid-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 - BOSUTINIB tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cb7a8d1d-07c0-462d-960f-214d44705e76) (DailyMed (U.S. National Library of Medicine), 2026); [Bosutinib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a613005.html) (MedlinePlus (U.S. National Library of Medicine), 2021); [Structural and spectroscopic analysis of the kinase inhibitor bosutinib binding to the Abl tyrosine kinase domain](https://www.rcsb.org/structure/3UE4) (RCSB Protein Data Bank, 2012).

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Representative model, for educational purposes only.

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