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Everolimus

(eh-vuh-role-uh-muss)

Trade/other name(s): Afinitor®, Afinitor® Disperz

Why would this drug be used?

This drug is used to treat advanced kidney cancer, advanced breast cancer, a rare type of brain tumor (subependymal giant cell astrocytoma), and a rare type of pancreatic cancer (pancreatic neuroendocrine tumor). It may also be used for other conditions, and it is being studied for use in treating a number of other cancers.

How does this drug work?

Everolimus is a type of targeted therapy that blocks mTOR, a protein in cells that normally promotes their growth and division. By blocking this protein, everolimus can help stop cancer cells from growing. Everolimus may also stop tumors from developing new blood vessels, which would help limit their growth.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have diabetes. Everolimus may raise blood sugar levels. You and your doctor will want to watch this closely during treatment.
  • If you have any type of liver disease (including hepatitis). This drug is cleared from the body mainly by the liver. Reduced liver function might result in more of the drug staying in the body than expected, which could lead to unwanted side effects. Your doctor may need to adjust your dose accordingly. This drug should not be used in people with severe liver problems.
  • If you ever had infection with the hepatitis B virus. This drug can cause this infection to become active again (see “Precautions”).
  • If you have ever had high cholesterol. Everolimus may raise blood levels of cholesterol.
  • If you have any type of kidney disease. Everolimus may affect the kidneys. Your doctor will probably want to monitor this closely during treatment.
  • If you have an active infection. This drug can suppress the immune system, making it harder for your body to fight the infection.
  • If you have any other medical conditions such as heart disease, gout, or infections. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you have recently had or are scheduled to have surgery. Everolimus may delay the time it takes for wounds to heal or cause healing wounds to re-open.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug can cause problems with the fetus if taken at the time of conception or during pregnancy. See “Precautions” section.
  • If you are breast-feeding. It is not known if this drug can pass into breast milk and affect the baby. Breast-feeding is not recommended during treatment with this drug.
  • If you think you might want to have children in the future. This drug has not been tested for its effect on fertility. Talk with your doctor about the possible risk with this drug and the options that may preserve your ability to have children.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs. In fact, keeping a written list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

This drug can interact with a number of drugs and supplements. Some cause the drug to build up in your blood, and can worsen side effects and other problems:

  • Anti-depressant drugs nefazodone (Serzone), fluvoxamine (Luvox), fluoxetine (Prozac, Serafem)
  • Antibiotics erythromycin, clarithromycin (Biaxin), telithromycin (Ketek), and similar drugs
  • Anti-fungal antibiotics such as ketoconazole (Nizoral), itraconazole (Sporanox), and voriconazole (Vfend)
  • The anti-nausea drug aprepitant (Emend)
  • Certain blood pressure medicines, like diltiazem (Cardizem) and verapamil (Calan)
  • HIV drugs such as indinavir, ritonavir, fosamprenavir, nelfinavir, atazanavir, and others
  • St. John's wort (herbal dietary supplement)

Other drugs may lessen the actions of everolimus so that it doesn't work as well:

  • Anti-seizure drugs carbamazepine (Tegretol), phenobarbital, and phenytoin (Dilantin)
  • TB drugs rifampin (Rifadin, Rimactane) and rifabutin (Mycobutin)
  • The corticosteroid drug dexamethasone (Decadron)

Don't start or stop taking any drugs while you are taking everolimus without talking with your doctor first. Your dose of everolimus may need to be adjusted before or after the change.

Any drugs or supplements that interfere with blood clotting can raise the risk of bleeding during treatment with everolimus. These include:

  • Vitamin E
  • Non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), and many others
  • Warfarin (Coumadin)
  • Ticlopidine (Ticlid)
  • Clopidogrel (Plavix)
  • Rivaroxaban (Xarelto)
  • Apixaban (Eliquis)
  • Dabigatran (Pradaxa)
  • Fondaparinux (Arixtra)
  • Any type of heparin injections, such as enoxaparin (Lovenox), dalteparin (Fragmin), or tinzaparin (Innohep)

Note that many cold, flu, fever, and headache remedies contain aspirin or ibuprofen. Ask your pharmacist if you aren't sure what's in the medicines you take.

Check with your doctor, nurse, or pharmacist about any other medicines, herbs, and supplements you are taking, and ask if alcohol can cause problems with this medicine.

Interactions with foods

Do not eat grapefruit or drink grapefruit juice without checking with your doctor, nurse, or pharmacist first. These foods may change the level of everolimus in your blood.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Everolimus (as Afinitor) is a tablet taken once a day at about the same time each day. It may be taken with or without food. The dose (and number of tablets) depends on what disease is being treated and in some cases is based on your height and weight.

Use scissors to open the blister package when you are ready to take your dose. The tablets should be swallowed whole with a glass of water. Do not crush or chew the tablets. If any pills are broken, do not take them.

For patients who cannot swallow tablets whole, special tablets (called Afinitor Disperz) can be stirred into a small amount of water. Be sure to follow the instructions you are given if taking the tablets this way.

In some cases (based on certain side effects), the dose may need to be changed or the drug not given for a time.

Take this drug exactly as directed by your doctor. If you do not understand the instructions, ask your doctor or nurse to explain them to you. Keep the medicine in its original package, out of the reach of children, pets, and others.

Precautions

This drug may interact with a number of other drugs or supplements (see section “Interactions with drugs”). Be sure your doctor knows all the drugs and supplements you are taking. Do not start or stop taking any drug without checking with your doctor.

This drug can cause allergic reactions in some people when it is given. Serious reactions are rare but can be dangerous. Symptoms can include feeling lightheaded or dizzy (due to low blood pressure), chest tightness or pain, trouble breathing or swallowing, flushing, back pain, or swelling of the face, tongue, or throat. Tell your doctor or nurse right away if you notice any of these symptoms after taking the drug.

Some people may develop lung disease (pneumonitis) during treatment with this drug, which in some cases may be severe. Tell your doctor right away if you notice any possible symptoms of lung problems, such as wheezing, pain in the chest, shortness of breath, or a new or worsening cough. If you develop this problem, your dose may need to be lowered or the drug stopped.

This drug may cause pain or sores in the mouth or on the lips. This can sometimes lead to bleeding, fungus infections, or trouble eating. Your doctor or nurse can suggest ways to reduce this, such as changing the way you eat or how you brush your teeth. If needed, your doctor can prescribe medicine to help with the pain. Don't use mouthwashes that contain alcohol, peroxide, iodine, or thyme, as they may make this worse.

This drug may affect your body's ability to heal wounds. Be sure your doctor knows if you have had surgery within the past few weeks. This drug may need to be stopped for a time before any scheduled surgery.

Your doctor will probably test your blood throughout your treatment, looking for possible effects of the drug on blood counts or on blood chemistry levels. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to reduce or delay your next dose of this drug, or even stop it altogether. Keep all your appointments for lab tests and doctor visits.

This drug may lower your white blood cell counts, which can increase your chance of getting an infection. Be sure to let your doctor or nurse know right away if you have any signs of infection, such as fever (100.5° or higher), chills, pain when passing urine, new onset of cough, or bringing up sputum (phlegm).

This drug can increase your risk of getting a serious infection even if your white blood cell count is normal. This risk is higher if you are also taking drugs that suppress the immune system, such as bone marrow transplant drugs or corticosteroids like prednisone or dexamethasone. Many different kinds of infections can occur, including a certain kind pneumonia (called Pneumocystis). If your doctor thinks that your risk is very high, you may be given medicines to prevent Pneumocystis infection. Report any symptoms of infection, including cough or breathing problems to your doctor right away

This drug can cause inactive viral infections, such as those with hepatitis B, to become active again. Your doctor may check your blood for signs of a prior hepatitis infection before starting this drug to see if it is safe. Let your doctor know if you have any symptoms of hepatitis while on this drug, such as yellowing of the skin and eyes (jaundice), abdominal (belly) pain, poor appetite, weight loss, fatigue, nausea, dark urine, and itching.

This drug may lower your platelet count in the weeks after it is given, which can increase your risk of bleeding. Speak with your doctor before taking any drugs or supplements that might affect your body's ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin), or vitamin E. Tell your doctor right away if you have unusual bruising, or bleeding such as nosebleeds, bleeding gums when you brush your teeth, or black, tarry stools.

Do not get any immunizations (vaccines), either during or after treatment with this drug, without your doctor's OK. Everolimus may affect your immune system. This could make vaccinations ineffective, or even lead to serious infections if you get a live virus vaccine during or soon after treatment. Try to avoid people who have recently received a live virus vaccine, such as the nasal influenza, measles, mumps, rubella, BCG, yellow fever, varicella, typhoid (TY21a), and oral polio vaccines. Check with your doctor about this.

This drug may cause kidney damage, leading to abnormal blood test results or a finding of protein in the urine. Your doctor will check blood tests of kidney function and urine tests for protein before and during treatment. The dose of everolimus may need to be lowered or the drug may need to be stopped if this becomes a problem.

Everolimus drug is cleared by the liver, so people with liver problems may need to take a reduced dose of this drug (see “Tell your doctor…”).

Everolimus may raise your blood sugar (glucose) levels. Tell your doctor if you have ever had diabetes or high blood sugar, or if you have symptoms that can be caused by high blood sugar, such as feeling thirsty all the time or having to urinate more often than normal. Your doctor may check your blood sugar levels while you are taking this drug.

This drug may also raise your blood cholesterol and/or triglyceride levels. Your doctor may check these levels before and during treatment.

This drug can harm the fetus if taken during pregnancy. Women should avoid pregnancy during treatment and for at least 8 weeks afterward. Check with your doctor about what kinds of birth control can be used with this medicine. In pregnant women, treatment with this drug should be used only if the potential benefit to the mother outweighs the potential risk to the fetus.

Possible side effects

You will probably not have most of the following side effects, but if you have any talk to your doctor or nurse. They can help you understand the side effects and cope with them.

Common

  • Mouth sores*
  • Nausea
  • Diarrhea
  • Infection*
  • Skin rash
  • Feeling tired
  • Swelling in the hands or feet
  • Cough*
  • Shortness of breath*
  • Headache
  • Joint pain
  • Low red blood cell counts (anemia) with symptoms like tiredness and shortness of breath
  • Low blood platelet counts with higher risk of bleeding*
  • Low white blood cell counts, with increased risk of infection*
  • High blood sugar levels*
  • High blood cholesterol levels*
  • Loss of appetite
  • Altered taste
  • Weight loss
  • Abnormal blood test results suggesting drug may be affecting the liver or kidneys (Your doctor will discuss the importance of this finding, if any.)*

Less common

  • Breathing problems; scarring or damage to the lungs*
  • Vomiting
  • Constipation
  • Feeling weak
  • Swelling in the hands or feet
  • Nosebleeds
  • Fever*
  • Back pain
  • Dry or itchy skin
  • Dry mouth
  • Trouble sleeping
  • High blood pressure
  • Changes in fingernails or toenails
  • Change in menses, such has periods stopping, heavy periods, or spotting between periods

Rare

  • Stomach pain
  • Serious bleeding (hemorrhage)
  • Kidney failure*
  • Seizures
  • Fluid buildup near the lungs
  • Allergic reaction*
  • Possibility of a higher risk of a second cancer in the future
  • Death due to lung problems, infection, kidney failure, or other cause

*See the “Precautions” section for more detailed information.

There are other side effects not listed above that can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved in 2009.

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.


Last Medical Review: 09/16/2014
Last Revised: 09/16/2014