Alectinib
ALK and ROS1 inhibitors
ALK and ROS1 inhibitorsHigh alert
An error with this medicine can cause serious harm: double checks and protocols are used.Pregnancy: avoid
Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men…
A selective second-generation ALK inhibitor for ALK-positive lung cancer, also after surgery. Watch muscles, liver, pulse and sun exposure.
Also called: CH5424802
Quick facts
- Group
- ALK and ROS1 inhibitors
- Target
- ALK receptor tyrosine kinase
- Key effects
- Fatigue · Constipation or diarrhoea · Muscle aches
- Monitor
- Heart rate and blood pressure regularly · Liver tests
- ATC
- L01ED03
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows alectinib (CH5424802) in the ATP pocket of the human ALK kinase domain.
Alectinib blocks the ATP site of the ALK kinase more selectively than crizotinib and stays active against several ALK mutations that make tumours resistant to crizotinib. Without ALK signalling, ALK-driven lung cancer cells stop growing and die.
- EML4-ALK fusion keeps the ALK kinase switched on
- Alectinib blocks the ATP site, selective for ALK
- Also covers several crizotinib-resistant ALK mutants
Indications
- ALK-positive non-small cell lung cancer that has spread. Lung cancer →
- ALK-positive non-small cell lung cancer after surgical removal, to lower the risk of recurrence. Lung cancer →
Adverse effects
Common
- Fatigue
- Constipation or diarrhoea
- Swelling of the hands, face or eyelids; weight gain
- Muscle aches
- Rash and sensitivity to sunlight
Contraindications
- No absolute contraindications in the label apart from hypersensitivity; see the warnings
Key interactions
- Strong CYP3A inhibitors or inducers
- Change alectinib levels.
- Other drugs that slow the heart
- Additive bradycardia.
What is monitored
- Heart rate and blood pressure regularly
- Liver tests
- Muscle symptoms and urine output
- New cough, breathlessness or fever
Administration and safety
- Oral capsules taken with food and swallowed whole.
- Strict sun protection (clothing, sunglasses, high-protection sunscreen) during treatment and for about a week after it.
- If the patient vomits after a dose, the dose is not repeated; the next one is taken at the usual time.
Pregnancy and breastfeeding
Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men with partners who could conceive), and breastfeeding is avoided.
Nursing care
- Check pulse and blood pressure; report dizziness, fainting or a slow pulse.
- Teach to report sudden muscle pain or weakness, dark urine, jaundice or new swelling of the legs.
- Teach sun protection and avoidance of tanning beds.
- Confirm a negative pregnancy test before the first dose and teach contraception during treatment and afterwards.
Pharmacokinetics
- Absorption
- Oral capsules, taken with food.
- Metabolism
- Liver, CYP3A4.
- Half-life
- About 33 hours.
Test yourself
Think of the answer, then tap the question to see it.
What advantage does alectinib have over crizotinib in ALK-positive lung cancer?
It is more selective for ALK and stays active against several mutations that cause crizotinib resistance.
Which skin precaution is taught to patients on alectinib?
Strict sun protection, because it causes photosensitivity.
A patient on alectinib reports sudden muscle pain and weakness. Why does it matter?
It can signal drug-induced muscle injury and must be reported promptly.
Connections
← Back to the class: ALK and ROS1 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: Alectinib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Alectinib - NCI (National Cancer Institute, 2024); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.