BCR-ABL inhibitor
BCR-ABL tyrosine kinase inhibitor
- BCR-ABL is the fusion kinase created by the Philadelphia chromosome
- Turns CML from fatal to chronic
- Kinase-domain mutations drive resistance
Drugs with this mechanism (5)
- Asciminib — Allosteric BCR-ABL inhibitor targeting the myristoyl pocket; designed for resistant CML.
- Bosutinib — BCR-ABL inhibitor for CML; prominent early diarrhea.
- Imatinib — The pioneering BCR-ABL inhibitor that transformed CML.
- Nilotinib — Second-generation BCR-ABL inhibitor for CML; QT prolongation.
- Ponatinib — Broad BCR-ABL inhibitor active against T315I disease; arterial occlusion sharply limits use.
Self-check
- Which chromosome abnormality creates the BCR-ABL fusion kinase?
The Philadelphia chromosome. - What molecular changes drive BCR-ABL inhibitor resistance?
Kinase-domain mutations.
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