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# Kinase inhibitors (targeted oncology)

Oral cancer drugs that block a kinase the tumour depends on, such as BCR-ABL in CML or mutant EGFR in lung cancer.

Updated Nov 1, 2026

## What they are

Small molecules, taken by mouth, that inhibit protein kinases driving a tumour: BCR-ABL (imatinib, dasatinib, nilotinib), EGFR (erlotinib, gefitinib, afatinib, osimertinib), BTK (ibrutinib), mutant BRAF (vemurafenib) and several angiogenic kinases (sorafenib). They work best when a test shows the tumour carries the target.

## Mechanism of action

Most compete with ATP in the kinase's catalytic pocket, so the enzyme cannot phosphorylate its substrates and the growth and survival signal stops. Some bind covalently to a cysteine near the pocket (afatinib, osimertinib, ibrutinib) and inhibit irreversibly. Tumours escape through new mutations in the kinase (for example T315I in BCR-ABL or T790M in EGFR) or by switching to other pathways.

Target: Protein kinases (BCR-ABL, EGFR, BTK, BRAF, VEGFR)

## Key points

- Imatinib: BCR-ABL in Philadelphia-positive CML, and KIT in gastrointestinal stromal tumour (GIST); fluid retention and oedema are typical.
- Dasatinib: pleural effusion and pulmonary hypertension; its absorption falls with antacids, H2 blockers and proton pump inhibitors.
- Nilotinib: QT prolongation and sudden death (boxed warning); taken on an empty stomach because food raises its absorption.
- EGFR inhibitors (erlotinib, gefitinib, afatinib, osimertinib): acne-like rash and diarrhoea; osimertinib also covers the T790M resistance mutation.
- Most are metabolised by CYP3A4: strong inducers and inhibitors change their levels.

## Drugs in this class

- [**Imatinib** The first targeted kinase inhibitor: it shuts down BCR-ABL in Philadelphia-positive CML and KIT in GIST. Typical… BCR-ABL tyrosine kinase (ABL1 kinase domain)](https://durgical.com/en/pharmacology/imatinib/)
- [**Dasatinib** A second-generation BCR-ABL and SRC inhibitor for CML and Ph-positive ALL, including after imatinib failure; known for… BCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases](https://durgical.com/en/pharmacology/dasatinib/)
- [**Erlotinib** A reversible EGFR kinase inhibitor for lung cancer with EGFR exon 19 or L858R mutations, and for pancreatic cancer… EGFR tyrosine kinase domain](https://durgical.com/en/pharmacology/erlotinib/)
- [**Afatinib** A second-generation, irreversible inhibitor of EGFR, HER2 and HER4 for EGFR-mutant lung cancer; diarrhoea and rash are… EGFR tyrosine kinase domain](https://durgical.com/en/pharmacology/afatinib/)
- [**Gefitinib** A first-generation, reversible EGFR kinase inhibitor for lung cancer with EGFR exon 19 deletion or L858R mutation… EGFR tyrosine kinase domain](https://durgical.com/en/pharmacology/gefitinib/)
- [**Ibrutinib** Oral covalent BTK inhibitor that switches off B-cell receptor signalling in CLL and Waldenström macroglobulinaemia… Bruton tyrosine kinase (BTK)](https://durgical.com/en/pharmacology/ibrutinib/)
- [**Nilotinib** A second-generation BCR-ABL inhibitor for CML. It prolongs the QT interval (boxed warning) and must be taken on an… BCR-ABL tyrosine kinase (ABL1 kinase domain)](https://durgical.com/en/pharmacology/nilotinib/)
- [**Osimertinib** A third-generation, irreversible EGFR inhibitor active against the T790M resistance mutation; now a standard… EGFR tyrosine kinase domain](https://durgical.com/en/pharmacology/osimertinib/)
- [**Sorafenib** An oral multikinase inhibitor (RAF, VEGFR, PDGFR) for liver, kidney and iodine-refractory thyroid cancer; hand-foot… VEGFR2 and other kinases (CRAF, BRAF, VEGFR1–3, PDGFR-β, KIT, FLT3, RET)](https://durgical.com/en/pharmacology/sorafenib/)
- [**Vemurafenib** An oral inhibitor of mutant BRAF V600E for melanoma that carries this mutation; it causes photosensitivity and new… BRAF kinase with the V600E mutation](https://durgical.com/en/pharmacology/vemurafenib/)
- [**Asciminib** A BCR-ABL inhibitor that binds outside the ATP site (the myristoyl pocket); works in chronic myeloid leukaemia… BCR-ABL1 tyrosine kinase (myristoyl pocket of ABL1)](https://durgical.com/en/pharmacology/asciminib/)
- [**Bosutinib** Second-generation BCR-ABL and SRC kinase inhibitor taken by mouth for Ph-positive CML. Diarrhoea is its hallmark; it… BCR-ABL tyrosine kinase (ABL1 kinase domain); also SRC-family kinases](https://durgical.com/en/pharmacology/bosutinib/)
- [**Ponatinib** Third-generation BCR-ABL inhibitor that also blocks the T315I mutant. Reserved for resistant CML and Ph-positive ALL… BCR-ABL tyrosine kinase (ABL1 kinase domain), including the T315I gatekeeper mutant](https://durgical.com/en/pharmacology/ponatinib/)
- [**Acalabrutinib** Second-generation covalent BTK inhibitor, more selective than ibrutinib, taken twice a day for CLL, small lymphocytic… Bruton's tyrosine kinase (BTK)](https://durgical.com/en/pharmacology/acalabrutinib/)

## Others in the class

- bosutinib
- ponatinib
- lapatinib
- dabrafenib
- trametinib
- sunitinib
- acalabrutinib

## Test yourself

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

## Which mutation makes BCR-ABL resistant to imatinib, dasatinib and nilotinib?

T315I, the «gatekeeper» mutation in the ABL kinase domain; ponatinib is active against it.

## Why is an EGFR kinase inhibitor chosen only after testing the lung tumour?

Because the benefit is in tumours with activating EGFR mutations (exon 19 deletion or L858R).

## Which enzyme metabolises most of these drugs, making them prone to interactions?

CYP3A4.

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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 - IMATINIB MESYLATE- imatinib tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a1787fad-3612-43e1-98fa-ce62361e0b3c) (DailyMed (U.S. National Library of Medicine), 2026); [DailyMed - ERLOTINIB tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3ecafc1e-979a-4aff-a276-18fc0b110491) (DailyMed (U.S. National Library of Medicine), 2022); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01E) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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