Asciminib
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.Pregnancy: avoid
Avoid in pregnancy. Asciminib may harm the fetus: contraception is used during treatment and for a week after, and breastfeeding is stopped.
A BCR-ABL inhibitor that binds outside the ATP site (the myristoyl pocket); works in chronic myeloid leukaemia, including T315I.
Quick facts
- Group
- Kinase inhibitors (targeted oncology)
- Target
- BCR-ABL1 tyrosine kinase (myristoyl pocket of ABL1)
- Key effects
- Muscle · Fatigue · Nausea
- Monitor
- Complete blood count · Lipase and amylase
- ATC
- L01EA06
No doses: the clinician sets them by the current guideline.
Mechanism of action
The crystal shows asciminib in the myristoyl pocket of the human ABL1 kinase domain, with nilotinib in the ATP site at the same time; the protein carries two mutations.
Normal ABL1 is kept switched off when a myristoyl group folds into a pocket of its kinase domain. BCR-ABL loses that brake. Asciminib fills the empty myristoyl pocket and locks the kinase in its inactive shape. Because it does not use the ATP site, it works when ATP-site mutations, such as T315I, cause resistance to other inhibitors.
- Asciminib fills the myristoyl pocket of BCR-ABL
- The kinase is locked in its inactive shape
- CML cells lose their growth signal, even with T315I
Indications
- Philadelphia chromosome-positive chronic myeloid leukaemia in chronic phase: newly diagnosed, after two or more kinase inhibitors, or with the T315I mutation. Chronic myeloid leukaemia →
Adverse effects
Common
- Muscle, bone and joint pain
- Fatigue, headache
- Nausea, diarrhoea
- Rash
Contraindications
- Hypersensitivity to asciminib
Key interactions
- St John's wort
- Can lower asciminib levels; avoided.
- Other medicines and supplements
- Many interact; the full list is reviewed before starting.
What is monitored
- Complete blood count, often at first
- Lipase and amylase
- Blood pressure
- BCR-ABL molecular response
Administration and safety
- Oral tablets swallowed whole on an empty stomach, not split, crushed or chewed.
- Taken at the same time each day; it is not stopped without the treating team.
Pregnancy and breastfeeding
Avoid in pregnancy. Asciminib may harm the fetus: contraception is used during treatment and for a week after, and breastfeeding is stopped.
Nursing care
- Check blood counts and teach to report bleeding, bruising or fever.
- Teach the signs of pancreatitis: abdominal pain spreading to the back, nausea, vomiting.
- Measure blood pressure at visits.
- Contraception during treatment and for a week after; breastfeeding is stopped.
Pharmacokinetics
- Absorption
- Oral tablets on an empty stomach (before or well after a meal).
Test yourself
Think of the answer, then tap the question to see it.
Where does asciminib bind BCR-ABL?
In the myristoyl pocket, an allosteric site away from the ATP site.
Why does asciminib work against T315I?
T315I changes the ATP site, which asciminib does not use.
Which pancreatic test is followed on asciminib?
Lipase and amylase (pancreatitis).
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: Asciminib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Asciminib Hydrochloride - NCI (National Cancer Institute, 2024); RCSB PDB - 5MO4: ABL1 kinase (T334I_D382N) in complex with asciminib and nilotinib (RCSB Protein Data Bank, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.