A targeted cancer medicine for ROS1 and NTRK gene changes
Entrectinib
A targeted cancer medicine for tumours driven by ROS1 or NTRK gene changes, which can also reach the brain.
What is Entrectinib?
Entrectinib is a specialist targeted cancer medicine used to treat cancers that are driven by particular gene changes called ROS1 or NTRK fusions. It blocks the faulty growth signals these gene changes produce, and it can also reach cancer that has spread to the brain. It only works for cancers with these gene changes, so the tumour is tested first. Important safety points include effects on the heart's pumping strength and rhythm (the QT interval), a higher risk of bone fractures, effects on thinking and balance, and weight gain. It can harm an unborn baby, so contraception is important.
Education and reference only. This is a plain-language guide to Entrectinib — it deliberately contains no doses. Doses depend on the person, the brand and the reason for treatment, and belong with your prescriber. Always check the BNF, the product labelling (SmPC) and follow medical advice.
What it is
Entrectinib is a targeted cancer medicine, a type of tyrosine kinase inhibitor. It is used to treat cancers that are driven by specific gene changes known as ROS1 or NTRK fusions, which can occur in several different cancer types. A feature of entrectinib is that it can cross into the brain, so it can be useful when cancer has spread there. It only works for cancers that carry these gene changes, which are checked by a test first. It is taken by mouth as capsules under the care of a cancer specialist.
How it works
Certain gene changes, called ROS1 or NTRK fusions, create faulty proteins that act like a stuck 'on' switch, driving the cancer to keep growing. Entrectinib blocks these faulty proteins, switching off that growth signal so the cancer slows or shrinks. Unlike some similar medicines, it is designed to pass into the brain, which is why it can act on cancer that has spread there. Because the proteins it blocks also play roles in the nervous system, heart and bones, it can cause effects in those areas, which is why monitoring is part of treatment.
Company & origin
Originated / developed by: Specialist manufacturer.
A specialist targeted cancer medicine used in the UK for cancers driven by ROS1 or NTRK gene changes, including some that have spread to the brain.
Practical use
How to take Entrectinib
General, dose-free guidance — always follow your prescriber's and the leaflet's specific instructions.
- Take the capsules by mouth as prescribed, at evenly spaced times, and swallow them whole.
- Report any breathlessness, swelling of the ankles, palpitations or fainting, which may relate to the heart.
- Report new bone pain or injuries, and any changes in balance, memory, mood or thinking.
- Take care with driving or operating machinery if you feel dizzy or your thinking is affected.
- Use reliable contraception throughout treatment and for the advised time afterwards, and tell your team at once if you might be pregnant.
Weighing it up
Advantages & disadvantages of Entrectinib
Advantages
- Targets cancers driven by ROS1 or NTRK gene changes, slowing or shrinking them.
- Can pass into the brain, so it may help when cancer has spread there.
- Taken by mouth as capsules rather than by infusion.
Disadvantages
- Only works for cancers with ROS1 or NTRK gene changes, so the tumour must be tested first.
- Can affect the heart's pumping strength and rhythm, increase fracture risk and affect thinking and balance.
- Commonly causes weight gain and can harm an unborn baby, so contraception is required.
Practical use
Good to know
Entrectinib only works for cancers driven by ROS1 or NTRK gene changes, so the tumour is tested before it is used. Several effects need watching for: it can reduce the heart's pumping strength and can affect the heart's electrical rhythm (the QT interval), so heart scans and tracings are used; it can increase the risk of bone fractures, so any new bone pain should be reported; and it can affect the brain and nervous system, causing dizziness, problems with balance, changes in mood, memory or thinking, and disturbed sleep, so these should be reported and care taken with driving. Weight gain is also common. It can harm an unborn baby, so reliable contraception is needed during treatment and for a time afterwards.
Who should not take it / use with caution
- People who have had a serious allergic reaction to entrectinib should not take it.
- It should not be used for cancers that do not carry the ROS1 or NTRK gene changes, as it will not work.
- It must not be used in pregnancy because it can harm an unborn baby, and it is used with caution in people with heart problems.
Monitoring
- Confirming the ROS1 or NTRK gene change before starting treatment.
- Heart scans for pumping strength and tracings (ECGs) for the QT interval.
- Watching for fractures, weight gain and effects on thinking, balance and mood.
Side effects
- Tiredness, weight gain, constipation and changes in taste.
- Dizziness, problems with balance, and changes in mood, memory, thinking or sleep.
- A fall in the heart's pumping strength or changes in the heart's rhythm (the QT interval).
- Less commonly but importantly, bone fractures, which is why new bone pain should be reported.
Key interactions
- Some medicines and grapefruit can raise entrectinib levels and side effects, so tell your team about everything you take.
- Medicines that affect the heart's QT interval should be reviewed alongside it.
- Other medicines that affect the brain, mood or sleep may add to its effects.
Available as: Capsules taken by mouth.
Answers
Entrectinib: frequently asked questions
What is entrectinib used for?
It is used to treat cancers driven by particular gene changes called ROS1 or NTRK fusions, and it can also reach cancer that has spread to the brain.
Why does the tumour need testing first?
Entrectinib only works for cancers that carry the ROS1 or NTRK gene changes, so a test is done first to check the tumour has one of them.
Why do I need heart checks?
It can reduce the heart's pumping strength and affect the heart's electrical rhythm (the QT interval), so heart scans and tracings are used to keep an eye on this.
Can it affect my thinking or balance?
Yes. It can cause dizziness, problems with balance and changes in memory, mood or thinking, so report these and take care with driving.
Why might I gain weight on it?
Weight gain is a common effect of entrectinib; your team can advise on managing it, and you should report any rapid or large change.
Authoritative sources
- BNF
- NICE CKS
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