How does it work?
Afinitor tablets contain the active ingredient everolimus, which is a type of medicine known as a protein kinase inhibitor. It works by interfering with the pathways that signal certain cancer cells to grow.
The way that cells in the body work and grow is regulated by various enzymes called protein kinases. These enzymes can be found in certain receptors on the surface of cells that are involved in the growth and spread of cancer cells.
In cancerous cells, the kinases make the cells grow and multiply abnormally. They also stimulate nearby blood vessels to grow into the tumour. The new blood vessels allow the cancer cells to grow and multiply by supplying them with oxygen and nutrients. They also allow the cancerous cells to spread into other areas of the body through the blood circulation.
Everolimus works by attaching to a certain protein inside the cancer cells and blocking the action of a protein kinase called mammalian target of rapamycin (mTOR). This stops the signals that tell the cancer cells to grow and multiply. It also stops blood vessels growing into the tumour. This reduces the tumour’s blood supply and with it, its supply of oxygen and nutrients. Both these effects stop the tumour from growing.
What is it used for?
- Advanced kidney cancer (renal cell carcinoma).
Everolimus is licensed to treat advanced kidney cancer that has not responded to treatment with other medicines called VEGF-targeted therapy, for example sunitinib or sorafenib.
- Hormone receptor-positive advanced breast cancer in postmenopausal women.
Everolimus is used in combination with a medicine called exemestane (Aromasin) for women whose breast cancer has not been controlled by treatment with a type of medicine called a non-steroidal aromatase inhibitor, for example anastrazole.
- Advanced tumours called neuroendocrine tumours that start in the pancreas.
Neuroendocrine cells are specialised nerve cells that produce hormones. Cancers originating in these cells are rare. Some produce hormones while others do not. Everolimus is used to treat tumours of this type that are not suitable for surgery or that have spread from the pancreas to other areas of the body.
How do I take it?
- Afinitor tablets should be taken once a day at the same time each day. Swallow the tablets whole with a glass of water; do not break, crush or chew them.
- Afinitor tablets can be taken either with or without food. However, you should be consistent in the way you take them - either always take your tablet with food, or always take it without food. This helps to maintain consistent effective levels of the medicine in your blood.
- You should avoid drinking grapefruit juice or eating grapefruit while taking this medicine, as it may increase the level of this medicine in your blood and hence increase the risk of side effects.
- If you forget to take a dose at your normal time, just skip that dose and take your next dose as usual. Do not take a double dose to make up for a missed dose.
- Mouth ulcers and inflammation of the lining of the mouth are common side effects experienced by people taking this medicine. It is important to speak to your doctor or pharmacist before treating any mouth ulcers or soreness in your mouth. Mouthwashes containing alcohol or peroxide should be avoided as they can make the problem worse.
- This medicine can increase your risk of getting infections, including pneumonia or other bacterial infections, invasive fungal infections, such as aspergillosis or candidiasis (thrush), and viral infections including reactivation of hepatitis B. You should tell your doctor immediately if you notice any signs of infection while you are taking this medicine, for example, a high temperature (fever), sore throat, mouth ulcers or swollen glands. If you get an infection you may need to stop taking this medicine while it is treated.
- This medicine can sometimes cause lung inflammation. You should tell your doctor if you experience any new or worsening shortness of breath, difficulty breathing or cough while taking this medicine, so this can be investigated.
- This medicine can decrease the number of blood cells in your blood. A low white blood cell count can increase your susceptibility to infections; a low red blood cell count causes anaemia and a low platelet count can cause problems with blood clotting and increase the risk of bleeding. For this reason, you will need regular blood tests to monitor your blood cells during treatment with this medicine. Tell your doctor immediately if you experience any of the following symptoms during your treatment, as they may indicate problems with your blood cells: unexplained bruising or bleeding, purple spots, sore mouth or throat, mouth ulcers, high temperature (fever) or other signs of infection, or suddenly feeling tired, breathless, or generally unwell.
- You should also have regular blood tests to monitor your liver and kidney function and your blood sugar and cholesterol levels while you are having treatment with this medicine.
- This medicine can slow wound healing. For this reason, you may need to stop taking this medicine before any major surgical procedures or operation. Follow your doctor’s instructions.
- This medicine could be harmful to a developing baby. Women who could get pregnant must use a reliable method of contraception to avoid getting pregnant while taking this medicine. Seek further medical advice from your doctor. Tell your doctor immediately if you think you could be pregnant during treatment.
- The ability of men to father a child may be affected by treatment with this medicine. It is important to discuss fertility with your doctor before starting treatment.
Use with caution in
- People with an infection (infections should normally be treated before this medicine is started).
- People with a history of hepatitis B infection.
- People with liver disease.
- People with decreased kidney function.
- People with raised levels of cholesterol in their blood.
- People who have recently had surgery.
Not to be used in
- Rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption (Afinitor tablets contain lactose).
- This medicine is not recommended for people with severely decreased liver function, as it has not been studied in people with severe liver problems.
- This medicine is not recommended for children and adolescents under 18 years of age, as its safety and effectiveness have not been studied in this age group.
This medicine should not be used if you are allergic to any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.
If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.
Pregnancy and breastfeeding
Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.
- This medicine could be harmful to a developing baby. It should not be used during pregnancy. Women who could get pregnant must use a reliable method of contraception to avoid getting pregnant while taking this medicine. Seek further medical advice from your doctor on which types of contraception are recommended. You should continue to use contraception to prevent pregnancy for at least 8 weeks after you have stopped taking this medicine. Tell your doctor straight away if you think you could be pregnant while taking this medicine.
- It is not known if this medicine passes into breast milk. Mothers who need to take this medicine should not breastfeed, because if the medicine does pass into the breast milk it could be harmful to a nursing infant. Seek medical advice from your doctor.
Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Just because a side effect is stated here, it does not mean that all people using this medicine will experience that or any side effect.
Very common (affect more than 1 in 10 people)
- Decrease in the number of red blood cells or platelets in the blood (anaemia or thrombocytopenia - see warning section above).
- Infections (see warning section above).
- Inflammation of the lining of the mouth (stomatitis) or mouth ulcers (see warning section above).
- Feeling weak or tired.
- Change in taste.
- Loss of appetite.
- Weight loss.
- Disturbances of the gut such as diarrhoea, nausea or vomiting.
- Inflammation of the lungs (pneumonitis - see warning section above).
- Shortness of breath (dyspnoea).
- Skin reactions such as dry skin, itching or rash.
- Swollen ankles due to fluid retention.
- Increased levels of fats called cholesterol and triglycerides in the blood.
- Increased blood sugar levels (hyperglycemia).
Common (affect between 1 in 10 and 1 in 100 people)
- Decreased numbers of white blood cells in the blood (see warning section above).
- Difficulty sleeping (insomnia).
- Inflammation of the eyes (conjunctivitis).
- Swelling of the eyelids.
- Dry mouth.
- Difficulty or pain when swallowing (dysphagia).
- Indigestion or stomach ache.
- Painful redness, swelling, blistering or ulceration of the palms and soles (hand-foot syndrome or palmar-plantar erythrodysesthesia).
- Skin redness, peeling or inflammation.
- Mild hair loss.
- Increased blood pressure (hypertension).
- Chest pain.
- Aching joints.
- Coughing up blood.
- Blood clot in the lungs (pulmonary embolism).
- Kidney failure.
- Decreased levels of potassium, calcium or phosphate in the blood (hypokalaemia, hypophosphataemia or hypocalcaemia).
Uncommon (affect between 1 in 100 and 1 in 1000 people)
- Slowed wound healing.
- Loss of sense of taste.
- Blood clot in a vein of the leg (deep vein thrombosis).
- Heart failure.
- Swelling of the lips, throat and tongue (angioedema).
- Acute breathing difficulties (respiratory distress syndrome).
The side effects listed above may not include all of the side effects reported by the medicine's manufacturer.
For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.
How can this medicine affect other medicines?
It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to make sure that the combination is safe.
The medicines listed below are strong inhibitors of the enzyme in the liver that breaks down everolimus. They may increase the blood level of everolimus, which could increase the risk of its side effects. These are not recommended for people taking everolimus:
- the antibiotic medicines clarithromycin and telithromycin
- the antifungal medicines ketoconazole, itraconazole, posaconazole or voriconazole
- the HIV protease inhibitors atazanavir,darunavir, nelfinavir, ritonavir, saquinavir or indinavir.
The medicines listed below are moderate inhibitors of the enzyme in the liver that breaks down everolimus. These may also increase the blood level of everolimus, which could increase the risk of its side effects. These should be used with caution in people taking everolimus. You should tell your doctor if you get any new or increased side effects if you are prescribed one of these medicines while taking Afinitor:
The following medicines may increase the breakdown of everolimus by the body and so could decrease the amount of everolimus in the blood, making it less effective. These should be avoided where possible while you are taking Afinitor, but if they can’t be avoided your doctor may need to increase your dose of Afinitor while you are on the combination:
- corticosteroids such as dexamethasone, prednisolone or prednisone
- the herbal remedy St John's wort (Hypericum perforatum).
This medicine can decrease the body's immune response. This means that vaccines may be less effective if given during treatment, because the body does not produce sufficient antibodies. Live vaccines may cause serious infections. Live vaccines include: measles, mumps, rubella, MMR, BCG, chickenpox, oral polio, oral typhoid and yellow fever. These should not be given to people whose immune system is underactive due to treatment with this medicine.
Other medicines containing the same active ingredient
- Votubia tablets also contain everolimus. These are used to treat a type of brain tumour called subependymal giant cell astrocytoma (SEGA).