What is entrectinib (Rozlytrek®)?

Entrectinib (Rozlytrek®) is used to treat different types of cancer.

It can be used to treat cancers that have a change in genes called NTRK, if:

  • the cancer is locally advanced or has spread to other parts of the body
  • the cancer cannot be removed with surgery because it is likely to cause complications
  • other treatment has not worked or is not suitable for you.

Entrectinib is also used to treat non-small cell lung cancer (NSCLC) that has changes to a gene called ROS1, if the cancer has spread to other parts of the body.

These genetic changes encourage the cancer cells to grow and divide. Entrectinib blocks the effect of the gene change and slows or stops the cancer cell growth.

Tests are done on the cancer cells to check for gene changes. This tells your doctor whether entrectinib is likely to work for you.

It is best to read this information with our general information about the type of cancer you have.

Entrectinib belongs to a group of targeted therapy drugs called tyrosine kinase inhibitors (TKIs). TKIs are also known as cancer growth inhibitors.

Your doctor will talk to you about this treatment and its possible side effects before you agree (consent) to have treatment.

How entrectinib is given

Entrectinib comes as capsules so you can take it at home. During treatment you will usually see a cancer doctor, a cancer nurse or specialist nurse, and a specialist pharmacist. This is who we mean when we mention doctor, nurse, or pharmacist in this information.

Before and during treatment, you will have:

  • blood tests to check the level of your blood cells and how well your liver and kidneys are working
  • heart tests such as an ECG to check your heart rhythm.

If there are any changes in your test results, your doctor may temporarily delay your treatment or reduce the dose.

Your doctor, nurse or pharmacist will discuss your treatment plan with you. They will give you the capsules to take home with you. Take all your medicines exactly as you have been told to.

You will usually take entrectinib for as long as it is working for you and side effects can be managed. Do not stop taking entrectinib without talking to your doctor first.

Taking entrectinib capsules

Entrectinib is taken once a day. Try to take the capsules at the same time each day. You can take them with or without food. Swallow the capsules whole with water. Do not chew, break, or crush them. They must not be opened or dissolved.

If you are sick (vomit) just after taking the capsules, do not take another dose. Take your next dose at the usual time the following day.

If you forget to take your capsules and there is more than 12 hours until your next dose, take your capsules as soon as you remember.

If there is less than 12 hours until your next dose, do not take the missed dose. Take your next dose at the usual time and let your doctor or nurse know. Do not take a double dose.

Other things to remember about your capsules:

  • Keep them safe and out of sight and reach of children.
  • Other people should avoid direct contact with the entrectinib capsules.
  • Keep them in the original package and at room temperature, away from heat and direct sunlight.
  • If your treatment is stopped, return any unused capsules to the pharmacist.

Entrectinib and food

Grapefruit and oranges: Do not eat grapefruit or Seville oranges, or drink grapefruit or Seville orange juice while taking this medicine. This is because it may increase the amount of entrectinib in your body.

Lactose: Entrectinib capsules contain lactose. Lactose is a type of sugar found in milk and dairy products. If you have a lactose intolerance, talk to your doctor.

Food Colouring: Entrectinib contains sunset yellow FCF (E110) in the 200mg hard capsules. This is a food colouring which may cause an allergic reaction.

Entrectinib and driving

Entrectinib may affect your ability to drive or use machines. It may cause you to:

  • have blurred vision
  • feel dizzy or faint
  • feel tired
  • feel confused or see things that are not there (hallucinate).

If this happens, you should not drive, use a bicycle, or operate machinery. Talk to your doctor, nurse, or pharmacist about whether it is okay for you to drive or use machines.

About side effects

We explain the most common side effects of this treatment here. We also include some less common side effects.

You may get some of the side effects we mention, but you are unlikely to get all of them. If you are also having treatment with other cancer drugs, you may have some side effects that we have not listed here. Always tell your doctor, nurse or pharmacist about any side effects you have.

Your doctor can give you drugs to help control some side effects. It is important to take them exactly as your nurse or pharmacist explains. This means they will be more likely to work for you. Your nurse will give you advice about managing your side effects. After your treatment is over, most side effects start to improve.

Serious and life-threatening side effects

Some cancer treatments can cause severe side effects. Rarely, these may be life-threatening. Your cancer doctor or nurse can explain the risk of these side effects to you.

Contact the hospital

Your nurse will give you telephone numbers for the hospital. If you feel unwell or need advice, you can call them at any time of the day or night. Save these numbers in your phone or keep them somewhere safe.

More information

We cannot list every side effect for this treatment. There are some rare side effects that are not listed. You can visit the electronic Medicines Compendium (eMC) for more detailed information.

Common side effects

Feeling tired

Feeling tired is a common side effect of this treatment. Try to pace yourself and plan your day so you have time to rest. Gentle exercise, like short walks, can give you more energy.

Entrectinib can affect your sleep. If you feel sleepy, do not drive, ride a bicycle or use machinery.

Effects on the nervous system

Entrectinib may affect the nervous system. You may have:

  • problems with balance and co-ordination
  • tingling, numbness or a burning feeling in your hands and feet
  • blurred vision
  • problems with swallowing.

Tell your doctor if you notice any of these side effects.

Less commonly, entrectinib may cause:

  • changes in your mood
  • confusion
  • memory problems
  • seeing things that are not there (hallucinations).

Contact the hospital straight away on the number you have been given if you have any of these side effects.

Risk of infection

This treatment can reduce the number of white blood cells in your blood. These cells fight infection. If the number of white blood cells is low, you are more likely to get an infection. A low white blood cell count is sometimes called neutropenia.

An infection can be very serious when the number of white blood cells is low. It is important to get any infection treated as soon as possible. Contact the hospital straight away on the 24-hour contact number you have been given if:

  • your temperature goes over 37.5°C (99.5°F)
  • you suddenly feel unwell, even with a normal temperature
  • you have symptoms of an infection
  • your temperature goes below 36°C (96.8°F).

Symptoms of an infection include:

  • feeling shivery and shaking
  • a sore throat
  • a cough
  • breathlessness
  • diarrhoea
  • needing to pass urine (pee) a lot, or discomfort when you pass urine.

It is important to follow any specific advice your cancer treatment team gives you.

You will have regular blood tests during treatment. If needed, your doctor may reduce or delay your treatment for a short time, until your cell count increases.

Anaemia (low number of red blood cells)

This treatment can reduce the number of red blood cells in your blood. Red blood cells carry oxygen around the body. If the number of red blood cells is low, this is called anaemia. You may have symptoms such as:

  • pale skin
  • lack of energy
  • feeling breathless
  • feeling dizzy and light-headed.

Tell your doctor or nurse if you have these symptoms.

If you are very anaemic, you may need a drip to give you extra red blood cells. This is called a blood transfusion.

Constipation

This treatment can cause constipation. Constipation means that you are not able to pass stools (poo) as often as you normally do. It can become difficult or painful. Here are some tips that may help:

  • Drink at least 2 litres (3½ pints) of fluids each day.
  • Eat high-fibre foods, such as fruit, vegetables and wholemeal bread.
  • Do regular gentle exercise, like going for short walks.

If you have constipation, contact the hospital for advice. Your doctor can give you drugs called laxatives to help.

Diarrhoea

This treatment may cause diarrhoea. Diarrhoea means passing more stools (poo) than is usual for you, or having watery or loose stools. If you have a stoma, it will be more active than usual.

If you have diarrhoea:

  • try to drink at least 2 litres (3½ pints) of fluids each day
  • avoid alcohol, caffeine, milk products, high-fat foods and high-fibre foods
  • contact the hospital for advice.

Tummy pain

This treatment can cause pain in the tummy (abdomen). Your doctor or nurse can suggest treatments to help.

Feeling sick

Your doctor will give you anti-sickness drugs to help prevent or control sickness during your treatment. Take the drugs exactly as your nurse or pharmacist tells you. It is easier to prevent sickness than to treat it after it has started.

If you feel sick, take small sips of fluids often and eat small amounts regularly. It is important to drink enough fluids. If you continue to feel sick, or are sick (vomit) more than once in 24 hours, contact the hospital as soon as possible. They will give you advice. Your doctor or nurse may change the anti-sickness drug to one that works better for you.

Loss of appetite

This treatment can affect your appetite. Don't worry if you do not eat much for a day or two. But if your appetite does not come back after a few days, or if you are losing weight, tell your nurse or dietitian. They can give you advice. They may give you food or drink supplements. Or they may suggest changes to your diet or eating habits to help.

Dehydration

Entrectinib can cause fluid loss (dehydration) so it is important to drink at least 2 litres (3½ pints) of fluids each day.

Changes to your taste

You may get a bitter or metal taste in your mouth. Sucking sugar-free sweets may help with this. Some foods may taste different or have no taste. Try different foods to find out what tastes best to you. Your nurse can give you more advice.

Fluid build-up

This treatment may cause a build-up of fluid. You may gain weight, or your face, ankles and legs may swell. This improves slowly after your treatment has finished. Your doctor may give you drugs to help reduce the swelling.

Effects on the lungs

This treatment can cause changes to the lungs. It can cause a build-up of fluid around the lungs (pleural effusion).

Contact the hospital straight away on the number you have been given if you develop:

  • a cough
  • wheezing
  • breathlessness.

You should also tell them if any existing breathing problems get worse. You may have tests to check your lungs.

Weight gain

You may gain weight when you are having this treatment. Your nurse or doctor may check your weight at appointments. They can give you advice and refer you to a dietitian if needed. Eating healthily and being active can help you keep to a healthy weight.

Bone or joint pain

You may get pain in your bones or joints with this treatment. If this happens, contact the hospital straight away on the 24-hour number you have been given.

Headaches

This treatment may cause headaches. If you have headaches, tell your doctor. They may give you painkillers to help.

Low blood pressure

This treatment may cause low blood pressure. This can cause you to feel dizzy.

Effects on the kidneys

This treatment can affect how your kidneys work. This is usually mild and goes back to normal after treatment finishes. You will have blood tests to check how well your kidneys are working.

It is important to drink at least 2 litres (3½ pints) of non-alcoholic fluid each day to help protect your kidneys.

Bladder problems

Tell your doctor or nurse if you have difficulty peeing (passing urine).

Effects on the liver

This treatment may affect how your liver works. You will have blood tests to check how well your liver is working.

Effects on the skin

Entrectinib can cause a skin rash. Tell your doctor or nurse if you develop a rash.

This treatment can cause your skin to be more sensitive to sunlight. If you are out in the sun, use a sun cream with a high sun protection factor (at least SPF 30) to protect your skin.

Less common side effects

Effects on the heart

This treatment can affect how the heart works. You may have tests to see how well your heart is working. These may be done before, during and after treatment.

If the treatment is causing heart problems, your doctor may need to reduce the dose of your treatment, or stop it for a while, or stop it completely.

Contact the hospital straight away on the 24-hour number the hospital has given you if you have any of these symptoms during or after treatment:

  • a cough
  • pain or tightness in your chest
  • breathlessness
  • swelling in the arms or legs (fluid retention)
  • dizziness or feel lightheaded
  • changes to your heartbeat.
Other conditions can cause these symptoms, but it is important to get them checked by a doctor. If you cannot get through to your doctor, call the NHS urgent advice number on 111.

Fractures

Entrectinib may cause bones to break more easily than usual. If you have pain, you cannot walk or move properly, or a bone is out of place, you need to be seen by a doctor straight away. Let your doctor know if you have a condition that might increase your risk of broken bones such as osteoporosis or osteopenia.

Tumour lysis syndrome (TLS)

This treatment may cause cancer cells to die and break down very quickly. When cancer cells break down, it can lead to a sudden release of chemicals into the blood. This is called tumour lysis syndrome (TLS).

Your kidneys can usually keep these chemicals in balance, but they might not be able to cope with very large amounts. The chemical imbalance can affect how well your kidneys work and cause problems with your heart rhythm.

You will have regular blood tests to check the levels of these chemicals.

If you are at risk of TLS, your doctor can give treatment to help prevent it. You may have:

  • extra fluids through a drip
  • medicines such as rasburicase or allopurinol.

Drinking at least 2 litres (3½ pints) of fluid a day will also help.

Contact the hospital straight away on the 24 hour number they have given you, if you have:

  • any kidney problems such as passing less urine than usual
  • pain and swelling in your joints.

Other information

Blood clot risk

Cancer and some cancer treatments can increase the risk of a blood clot. Symptoms of a blood clot include:

  • throbbing pain, redness or swelling in a leg or arm
  • suddenly feeling breathless or coughing
  • sharp chest pain, which may be worse when you cough or take a deep breath.

If you have any of these symptoms, contact the hospital straight away on the 24-hour contact number you have been given. If you cannot get through to your doctor, call the NHS urgent advice number on 111.

A blood clot is serious, but it can be treated with drugs that thin the blood (anticoagulants). Your doctor or nurse can give you more information.

You can help reduce the risk of developing a blood clot by:

  • staying active during treatment
  • drinking plenty of fluids, especially water.

You may be given anticoagulants to help prevent a clot.

Other medicines

Some medicines can affect how this treatment works or be harmful when you are having it. Always tell your cancer doctor about any drugs you are taking or planning to take, such as:

  • medicines you have been prescribed
  • medicines you buy in a shop or chemist
  • vitamins, herbal drugs and complementary therapies.

Tell other doctors, pharmacists or dentists who prescribe or give you medicines that you are having this cancer treatment.

You can visit the electronic Medicines Compendium (eMC) for more detailed information about your treatment.

Vaccinations

Vaccinations can reduce your risk of getting certain infections. Your doctor or nurse may talk to you about having vaccinations.

Doctors usually recommend that people with cancer have a flu vaccination and a coronavirus (covid) vaccination. These are both inactivated vaccinations that can help reduce the risk of infection. People with weak immune systems can have these, as they are not live vaccinations. 

If your immune system is weak, you need to avoid live vaccinations. This is because they can make you unwell. Live vaccines contain a very weak version of the illness they are vaccinating you against. Your cancer doctor or GP can tell you more about live and inactivated vaccinations.

Contraception

Your doctor will advise you not to get pregnant or make someone pregnant while having this treatment. The drugs may harm a developing baby. You may need a pregnancy test before starting treatment. If you use a hormonal contraception, you are advised to also use barrier contraception, such as a condom. You should do this during your treatment and for a while after treatment finishes. Your doctor, nurse or pharmacist can tell you more about this.

Breastfeeding

You are advised not to breastfeed while having this treatment, or for some time after treatment finishes. This is because the drugs could be passed to the baby through breast milk.

Your doctor or nurse can give you more information.

Medical and dental treatment

If you need medical treatment for any reason other than cancer, always tell the doctors and nurses you are having cancer treatment. Give them the contact details for your cancer doctor so they can ask for advice.

If you think you need dental treatment, talk to your cancer doctor or nurse. Always tell your dentist you are having cancer treatment.

About our information

References


Reviewers

  • Reviewers

    This information has been written, revised and edited by Macmillan Cancer Support’s Cancer Information Development team. It has been reviewed by expert health professionals and people living with cancer.

    Our cancer information has been awarded the PIF TICK. Created by the Patient Information Forum, this quality mark shows we meet PIF’s 10 criteria for trustworthy health information.