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Afinitor: Uses, Side Effects and Dosage

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Prescription (Rx) Current status: Cancelled Post Market
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7.5 mg
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Source: Health Canada – Drug Product Database (DPD) and product monographs · About this document

Patient Medication Information: uses, side effects, how to take - Afinitor

ABOUT THIS MEDICATION

What the medication is used for:

AFINITOR is used in the treatment of:

  • hormone receptor-positive, HER2-negative advanced

    breast cancer in postmenopausal women in whom certain other medicines (letrozole or anastrozole) no longer keep the disease under control. It is given together with a medicine called exemestane. It is not known whether AFINITOR prolongs overall survival or improves the quality of life of patients with advanced breast cancer.

  • a type of pancreatic cancer known as pancreatic

    neuroendocrine tumour (PNET), that has progressed and cannot be treated with surgery.

  • a type of cancer known as neuroendocrine tumour (NET)

    of gastrointestinal or lung origin that has progressed and cannot be treated with surgery.

  • metastatic kidney cancer (when cancer cells have spread

    from the kidney to other parts of the body) after failure of treatment with sunitinib or sorafenib. It is not known whether AFINITOR prolongs overall survival or improves the quality of life of patients with kidney cancer.

  • adult patients with a genetic condition called tuberous

    sclerosis complex (TSC) who have angiomyolipoma of the kidney (a kidney tumour) and do not require immediate surgery.

AFINITOR DISPERZ is used in the treatment of:

  • seizures associated with TSC in children and adults

    whose seizures are not controlled well by antiepileptic medicines. AFINITOR DISPERZ is the only formulation that should be used for the treatment of patients with seizures associated with TSC.

AFINITOR and AFINITOR DISPERZ are used in the treatment of:

  • patients with subependymal giant cell astrocytoma

    (SEGA), a brain tumour seen with a genetic condition

    called tuberous sclerosis complex (TSC), who are not suitable for surgery.

What it does:

Everolimus in AFINITOR and AFINITOR DISPERZ works by blocking a specific enzyme that is involved in tumour cell growth and division. This may help to slow down the growth and spread of kidney cancer cells and of pancreatic neuroendocrine cells and may reduce the size of brain tumours (SEGA), kidney tumours (angiomyolipomas) that are associated with a genetic disorder called tuberous sclerosis complex (TSC). When given together with exemestane, everolimus in AFINITOR may slow down the growth and spread of breast cancer cells. Everolimus in AFINITOR DISPERZ may decrease the frequency of seizures in patients with TSC.

When it should not be used:

If you are allergic (hypersensitive) to everolimus, or sirolimus (RAPAMUNE®), temsirolimus (TORISEL®), or any of the other ingredients in AFINITOR or AFINITOR DISPERZ listed below in the What the nonmedicinal ingredients are section.

What the medicinal ingredient is:

Everolimus

What the nonmedicinal ingredients are:

AFINITOR: Butylated hydroxytoluene (E321), crospovidone, hypromellose, lactose anhydrous, lactose monohydrate and magnesium stearate.

AFINITOR DISPERZ: Butylated hydroxytoluene (E321), cellulose microcristalline, crospovidone, hypromellose, lactose monohydrate, magnesium stearate, mannitol and silica colloidal anhydrous.

What dosage forms it comes in:

AFINITOR

AFINITOR tablets are supplied as 2.5 mg, 5 mg, 7.5 mg and 10 mg tablets that are white to slightly yellowish, elongated, with a bevelled edge and no score.

Each 2.5 mg tablet contains 2.5 mg everolimus and is engraved with “LCL” on one side and “NVR” on the other.

Each 5 mg tablet contains 5 mg everolimus and is engraved with “5” on one side and “NVR” on the other.

Each 7.5 mg tablet contains 7.5 mg everolimus and is engraved with “7P5” on one side and “NVR” on the other.

Each 10 mg tablet contains 10 mg everolimus and is engraved with “UHE” on one side and “NVR” on the other.

For 2.5 mg, 5 mg and 10 mg, each blister pack contains 10 tablets and there are 3 blister packs in a carton.

For 7.5 mg, each blister pack contains 7 tablets and there are 4 blister packs in a carton.

AFINITOR DISPERZ (for treatment of SEGA and/or seizures associated with TSC)

AFINITOR DISPERZ tablets for oral suspension are supplied as 2 mg, 3 mg and 5 mg tablets for oral suspension that are white to slightly yellowish, round, flat tablets with a bevelled edge and no score.

Each 2 mg tablet for oral suspension contains 2 mg everolimus and is engraved with “D2” on one side and “NVR” on the other.

Each 3 mg tablet for oral suspension contains 3 mg everolimus and is engraved with “D3” on one side and “NVR” on the other.

Each 5 mg tablet for oral suspension contains 5 mg everolimus and is engraved with “D5” on one side and “NVR” on the other.

Each blister pack contains 10 tablets for oral suspension and there are 3 blister packs in each carton.

WARNINGS AND PRECAUTIONS

Serious Warnings and Precautions Hormone receptor-positive, HER2-negative advanced breast cancer, advanced NET and metastatic kidney cancer: AFINITOR should be prescribed and managed only by a doctor experienced in anticancer drugs.

Angiomyolipoma of the kidney associated with TSC: AFINITOR tablets should be prescribed and managed only by a doctor experienced in treating patients with tuberous sclerosis complex.

The best possible duration of treatment with AFINITOR for patients with angiomyolipoma of the kidney associated with TSC is not known. Absence of menstrual periods in females who previously had periods (secondary amenorrhoea) has been observed in some female patients receiving AFINITOR and is a potential risk.

SEGA associated with TSC: AFINITOR and AFINITOR DISPERZ should be prescribed and managed only by a doctor experienced in treating patients with tuberous sclerosis complex. The best possible duration of treatment with AFINITOR or AFINITOR DISPERZ for patients with SEGA is not known; however, SEGA re-growth has been seen once therapy is stopped.

AFINITOR or AFINITOR DISPERZ are not to be used in children and adolescents (below 18 years of age) who have liver problems.

Information available from studies in animals suggests that there is a risk of delayed development in patients taking everolimus. AFINITOR and AFINITOR DISPERZ are not interchangeable. See PROPER USE OF THIS MEDICATION.

Serious side effects which have been reported with the use of AFINITOR include:

  • Non-infectious pneumonitis (including interstitial lung

    disease)

  • Infections
  • Kidney failure

BEFORE you use AFINITOR or AFINITOR DISPERZ talk to your doctor or pharmacist if you:

  • have any problems with your liver or have previously had any liver disease
  • have any infections. AFINITOR or AFINITOR DISPERZ can make you more likely to get an infection. Some infections have resulted in death in both adults and children.
  • have had hepatitis B, because it may be reactivated during your treatment with AFINITOR or AFINITOR DISPERZ
  • have diabetes (high level of sugar in the blood)
  • have high cholesterol or triglyceride levels
  • have low blood cell count
  • are going to have surgery, if you have had a recent surgery or if you still have an unhealed wound following surgery. AFINITOR or AFINITOR DISPERZ might affect the way your wound heals.
  • are pregnant, think you may be pregnant, or are planning to become pregnant. AFINITOR and AFINITOR DISPERZ are not recommended during pregnancy, as it could harm an unborn baby.

  • are breastfeeding. Do not breastfeed during treatment with

    AFINITOR or AFINITOR DISPERZ and for two weeks after the last dose of AFINITOR or AFINITOR DISPERZ, as it could harm a breastfed baby.

  • need to receive a vaccine or come in contact with those who have received a live vaccine. For paediatric patients with TSC, consider completing the recommended childhood series of live virus vaccinations prior to the start of therapy according to local treatment guidelines.
  • have kidney problems as kidney failure has been reported in some patients taking AFINITOR
  • are taking medication that has an effect on blood clotting or may increase the risk of bleeding, or if you have a history of bleeding disorder. Taking AFINITOR or AFINITOR DISPERZ might make your bleeding worse.

  • are allergic to or suspect you are allergic to any ingredient in

    AFINITOR or AFINITOR DISPERZ that could result in swelling of the airways and tongue and/or difficulty in breathing.

  • are taking other medicines.

Hormone receptor-positive, HER2-negative advanced breast cancer, advanced NET and metastatic kidney cancer: AFINITOR is not to be used in children or adolescents under 18 years of age.

Angiomyolipoma of the kidney associated with TSC: AFINITOR and AFINITOR DISPERZ are not to be used in children or adolescents under 18 years of age with angiomyolipoma of the kidney associated with TSC.

SEGA associated with TSC: AFINITOR and AFINITOR DISPERZ can be used in children and adolescents (below 18 years of age) who have normal liver function.

Seizures associated with TSC: AFINITOR DISPERZ can be used in patients two years of age and older who have normal liver function.

What you should know during AFINITOR or AFINITOR DISPERZ treatment

Women of child-bearing potential: AFINITOR or AFINITOR DISPERZ could harm an unborn baby or a breast-fed baby. You should use a highly effective contraceptive method during treatment with AFINITOR and for 8 weeks after treatment has stopped, even if you have not yet had a first menstrual period. Absence of periods (amenorrhoea) may develop during treatment with AFINITOR or AFINITOR DISPERZ, but pregnancy may still occur and use of a highly effective contraceptive method should continue. If you think you may have become pregnant, ask your doctor for advice. If you experience irregular or delayed periods or absence of periods (amenorrhoea) ask your doctor for advice.

Fertility: AFINITOR or AFINITOR DISPERZ may affect your ability to become pregnant or father a child (fertility). Absence of menstrual periods in females who had periods (secondary amenorrhoea) has been observed in some female patients receiving AFINITOR. Abnormal levels of reproductive hormones required for the development of sperm and absence of sperm were observed in male patients.

Monitoring during your treatment with AFINITOR or AFINITOR DISPERZ:

You will have regular blood tests during treatment. These will monitor the amount of blood cells (white blood cells, red blood cells and platelets) in your body, your kidney function (levels of creatinine, blood urea nitrogen or urinary protein), liver function (level of liver enzymes) as well as your cholesterol, triglyceride and blood sugar levels.

If you receive AFINITOR or AFINITOR DISPERZ for the treatment of SEGA, regular blood tests are necessary to measure how much everolimus is in your blood since this will help your doctor decide how much AFINITOR or AFINITOR DISPERZ you need to take.

If you receive AFINITOR DISPERZ for the treatment of seizures associated with TSC, regular blood tests are necessary to measure how much everolimus is in your blood. This will help your doctor decide how much AFINITOR DISPERZ you need to take.

INTERACTIONS WITH THIS MEDICATION

Tell your doctor or pharmacist before taking AFINITOR or AFINITOR DISPERZ if you are taking or have recently taken any other medicines, including medicines obtained without a prescription. This includes in particular:

  • drugs to treat infections (antifungals like ketoconazole,

    itraconazole; voriconazole or fluconazole; antibiotics like clarithromycin, telithromycin or erythromycin)

  • drugs to treat tuberculosis, such as rifampicin or rifabutin
  • St. John’s wort (also known as Hypericum perforatum)

  • drugs to stop seizures or fits (anticonvulsants like phenytoin,

    carbamazepine, oxcarbazepine or phenobarbital)

  • drugs to treat AIDS/HIV like ritonavir, amprenavir,

    fosamprenavir, efavirenz, or nevirapine

  • drugs to treat heart conditions or high blood pressure (such as

    verapamil or diltiazem)

  • angiotensin-converting enzyme (ACE) inhibitors, medicines

    used to treat high blood pressure or other cardiovascular problems

    • a class of medications called “statins” (like atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin or simvastatin) to treat high levels of lipids or cholesterol in the blood
    • cyclosporine, a medicine to stop the body from rejecting organ transplants
    • aprepitant, a medicine to prevent nausea and vomiting
    • midazolam, a medicine used to treat acute seizures, or used as a sedative before or during surgery or a medical procedure
    • drugs containing pimozide, quinidine or ergotamine, as the concentration of these drugs in your blood may be affected if these drugs are taken together with AFINITOR or AFINITOR DISPERZ

For patients with SEGA who are taking anti-seizure medications, a change in anti-seizure medication dose (up or down) may require a change in AFINITOR or AFINITOR DISPERZ dose.

For patients with seizures associated with TSC who are taking anti-seizure medications, a change in anti-seizure medication dose (up or down) may require a change in AFINITOR DISPERZ dose.

While you are taking AFINITOR or AFINITOR DISPERZ you should never start a new medicine without checking first with the doctor who prescribed AFINITOR or AFINITOR DISPERZ. This includes prescribed medicines, over the counter medicines and herbal or alternative medicines.

PROPER USE OF THIS MEDICATION

AFINITOR and AFINITOR DISPERZ are not interchangeable. Make sure you are using the correct tablets prescribed for you and check with the pharmacist. Do not mix use of the two formulations. Do not switch use of the products without direction by your doctor.

Your doctor will tell you exactly how many tablets of AFINITOR or AFINITOR DISPERZ to take. Follow your doctor’s instructions carefully.

AFINITOR and AFINITOR DISPERZ should be taken at about the same time each day (preferably in the morning), either consistently on an empty stomach or consistently with food.

AFINITOR

AFINITOR tablets should be taken by mouth, once daily. Swallow the tablets whole, with a glass of water. Do not chew or crush the tablets.

AFINITOR DISPERZ (for treatment of SEGA or seizures associated with TSC)

Do not chew, crush, or swallow the AFINITOR DISPERZ tablets for oral suspension. Mix AFINITOR DISPERZ in tap water or non-sparkling water only, to prepare the suspension. Do not use juice or any other liquids (see Preparation of suspension). Take AFINITOR DISPERZ tablets as a suspension only. You can prepare the suspension in an oral syringe or in a small drinking glass. The suspension must be taken right away. If you do not take the dose within 60 minutes after it has been prepared, throw away the dose and prepare a new dose of AFINITOR DISPERZ.

Instructions for use and handling of AFINITOR DISPERZ

Caregivers are advised to avoid contact with suspensions of AFINITOR DISPERZ. As AFINITOR DISPERZ can cause harm to an unborn baby, the suspension should be prepared, when possible, by an adult who is not pregnant or planning to become pregnant. Wash hands thoroughly before and after preparation of the suspension.

Preparation of suspension

Supplies needed to prepare the suspension in an oral syringe

  • Blister card with AFINITOR DISPERZ tablets for oral suspension
  • Scissors to open the blister card
  • 2 clean drinking glasses
  • Approximately 30 mL of water
  • 10 mL oral syringe (for one time use)

Supplies needed to prepare the suspension in a small drinking glass

  • Blister card with AFINITOR DISPERZ tablets for oral suspension
  • Scissors to open the blister card
  • 30 mL dose cup for measuring water (you can ask your pharmacist for this)
  • 1 clean drinking glass (maximum size 100 mL)
  • Water to prepare the suspension
  • Spoon for stirring

Preparing a dose of AFINITOR DISPERZ suspension using an oral syringe

  1. 1. Wash and dry your hands before preparing the medication.
  1. 2. Take a 10 mL oral syringe and pull back on the plunger. Remove the plunger from the barrel of the syringe.
  1. 3. Use scissors to open the blister card along the dotted lines. Remove the prescribed number of tablets for oral suspension from the blister card. Place the tablets for oral suspension (maximum of five 2 mg tablets, three 3 mg tablets, or two 5 mg tablets) into the oral syringe immediately.
  1. 4. Re-insert the plunger into the barrel of the oral syringe and push the plunger until it comes into contact with the tablets for oral suspension.
  1. 5. Fill a drinking glass with water and pull up about 5 mL of water into the oral syringe by slowly pulling back on the plunger.

Note: The amount of water in the syringe does not need to be accurate. All tablets for oral suspension should be covered by water. In case tablets for oral suspension remain in the dry upper part of the syringe, make them move into the water by gentle tapping.

  1. 6. Hold the oral syringe with the tip pointing up. Pull back on the plunger to draw back about 4 mL of air.
  1. 7. Place the filled oral syringe in the clean, empty glass with the tip pointing up. Allow the tablets for oral suspension 3 minutes to break apart. Make sure to proceed further only when the 3 minutes are over and when the tablets for oral suspension have completely broken apart.
  1. 8. Slowly turn the oral syringe up and down five times just before giving the dose. Do not shake the oral syringe.
  1. 9. Hold the oral syringe in an upright position (with the tip up). Carefully remove most of the air by pushing up gently on the plunger.
  1. 10. Give the full contents of the oral syringe slowly and gently into the mouth right away, within 60 minutes of preparing it.
  1. 11. Carefully remove the oral syringe from patient’s mouth.
  1. 12. Insert the tip of the oral syringe into the drinking glass that is filled with water and pull up about 5 mL of water by slowly pulling back on the plunger.
  1. 13. Hold the oral syringe with the tip pointing up and use the plunger to draw back about 4 mL of air.
  1. 14. With the tip of the oral syringe still pointing up, swirl the contents by gently rotating the syringe in a circular manner to suspend any remaining particles of the medication.
  1. 15. While holding the oral syringe in an upright position (with the tip up), carefully remove most of the air by pushing up gently on the plunger.
  1. 16.

    Dispense the full contents of the oral

    syringe slowly and gently into the mouth of the patient.

  2. 17.

    Carefully remove the syringe from the

    patient’s mouth. If the total prescribed dose is more than 10 mg, repeat steps 2 to 17 to finish giving the dose.

  3. 18.

    Throw away the original syringe in

    your household trash.

  1. 19. Wash your hands.

Preparing a dose of AFINITOR DISPERZ suspension using a small drinking glass

  1. 1.

    Wash and dry your hands before

    preparing the medication.

  1. 2.

    Add about 25 mL of water to the 30

    mL dose cup. The amount of water added does not need to be exact.

  1. 3.

    Pour the water from the dose cup into

    a small drinking glass (maximum size 100 mL).

  1. 4.

    Use scissors to open the blister card

    along the dotted line and remove the prescribed number of tablets for oral suspension from the blister card.

  2. 5.

    Add the prescribed number of tablets

    for oral suspension into the water (maximum of five 2 mg tablets, three 3-mg tablets, or two 5 mg tablets).

  1. 6.

    Wait 3 minutes to allow the tablets

    for oral suspension to break apart.

  1. 7.

    Gently stir the contents of the glass

    with a spoon.

  1. 8.

    Drink the full amount of the

    suspension right away, within 60 minutes of preparing it.

  1. 9.

    Refill the glass with the same amount

    of water (about 25 mL). Stir the contents with the same spoon.

  1. 10.

    Drink the full amount right away so

    that you take any remaining medicine.

    If the total prescribed dose is more than 10 mg, repeat steps 2 to 10 to

finish taking the dose.
  1. 11. Wash the glass and the spoon thoroughly with water. Wipe the glass and spoon with a clean paper towel and store them in a dry and clean place until your next dose.
  1. 12. Wash your hands.

Do not drink grapefruit juice or eat grapefruit, star fruit or Seville oranges. It may increase the amount of AFINITOR or AFINITOR DISPERZ in the blood, possibly to a harmful level.

Continue taking AFINITOR or AFINITOR DISPERZ as long as your doctor tells you.

Usual dose:

Hormone receptor-positive, HER2-negative advanced breast cancer, NET, metastatic kidney cancer and angiomyolipoma of the kidney associated with TSC: The usual dose is 10 mg, to be taken by mouth once daily, at about the same time each day (preferably in the morning). AFINITOR should be taken either consistently with food or consistently without food.

A higher or lower dose may be recommended by your doctor based on your individual treatment needs (e.g. if you have liver problems or if you are taking certain additional medicines).

SEGA associated with TSC: Your doctor will determine the starting dose of AFINITOR or AFINITOR DISPERZ you need to take depending on your body size, the health of your liver and other medicines you are taking. Blood tests are necessary during treatment with AFINITOR or AFINITOR DISPERZ to measure the amount of everolimus in your blood and find the best daily dose for you.

Your doctor might need to reduce your dose of AFINITOR or AFINITOR DISPERZ, or to interrupt or discontinue your treatment with AFINITOR or AFINITOR DISPERZ (e.g., if you have lung or breathing problems, mouth ulcers).

Seizures associated with TSC: Your doctor will determine the starting dose of AFINITOR DISPERZ you need to take depending on your body size, the health of your liver and other medicines you are taking. Blood tests are necessary during treatment with AFINITOR DISPERZ to measure the amount of everolimus in your blood and find the best daily dose for you.

Your doctor might need to reduce your dose of AFINITOR DISPERZ, or to interrupt or discontinue your treatment with AFINITOR DISPERZ for a variety of reasons. For example, if you have lung or breathing problems, mouth sores/ulcers, etc.

Overdose:

In case of drug overdose, contact a health care practitioner, hospital emergency department or regional Poison Control Centre immediately, even if there are no symptoms.

Missed Dose:

If you forget to take AFINITOR or AFINITOR DISPERZ, you may still take it up to 6 hours after the time you normally take it.

If you remember more than 6 hours after you normally take your AFINITOR or AFINITOR DISPERZ, skip the dose for that day. The next day, take AFINITOR or AFINITOR DISPERZ at your usual time. Do not take a double dose to make up for the one that you missed.

SIDE EFFECTS AND WHAT TO DO ABOUT THEM

Like all medicines, AFINITOR and AFINITOR DISPERZ can cause side effects.

Treatment of hormone receptor-positive, HER2-negative advanced breast cancer, advanced NET and metastatic kidney cancer

Very common side effects:

These side effects may affect more than 1 in 10 patients.

  • Lung or breathing problems (pneumonitis)
  • Infections
  • Loss of appetite
  • Disturbed taste (dysgeusia)
  • Dry mouth
  • Headache
  • Cough
  • Nose bleeds (epistaxis)
  • Breathlessness (dyspnoea)
  • Dizziness

  • Mouth ulcers: AFINITOR can cause mouth ulcers and sores.

    Your doctor may tell you to use a special mouthwash or mouth gel that does not contain alcohol or peroxide that may require a prescription. Tell your doctor if you have pain, discomfort, or open sores in the mouth.

  • Stomach upsets like feeling sick (nausea), being sick

    (vomiting), diarrhoea, constipation

  • Hair loss
  • Rash
  • Dry skin
  • Itching (pruritus)
  • Nail disorders
  • Feeling weak or tired
  • Mucosal inflammation

  • Swelling of arms, hands, feet, ankles, face or other part of the

    body (signs of oedema)

  • Fever
  • Loss of weight
  • Low red blood cell count (anaemia)
  • High blood glucose
  • High cholesterol
  • High triglycerides
  • High blood pressure
  • Low level of potassium in the blood (hypokalaemia)
  • High level of phosphate in the blood
  • Pain in arm and leg, mouth and throat, back or joints

  • Trouble sleeping (insomnia)

    If any of these affects you severely, tell your doctor.

    Common side effects:

    These side effects may affect between 1 and 10 in every 100 patients.

    • Blockade or obstruction of a blood vessel (vein) in the legs

      (deep vein thrombosis). Symptoms may be swelling and/or pain in one of your legs, usually your calf, and redness or warm skin in the affected area.

    • Chest pain, cough, hiccups and rapid breathing (signs of fluid collection between the layers of tissue that line the lungs and chest cavity)
    • High level of sugar in the blood (diabetes)
    • Worsening of diabetes
    • Dehydration
    • Pulmonary embolism (a condition that occurs when one or more arteries in your lungs become blocked). Symptoms may be sudden onset of shortness of breath, chest pain or coughing up blood). Talk to your doctor right away if this occurs.
    • Coughing up blood (haemoptysis)
    • Heartburn (dyspepsia)
    • Difficulty in swallowing (dysphagia)
    • Acne

    • Rash/pain on the palms of your hands or soles of your feet

      (hand foot syndrome)

    • Skin reddening (erythema)
    • Protein in the urine
    • Kidney failure
    • Pain in abdomen, chest or jaw
    • Low lymphocyte, platelet or white blood cell count
    • Excess fluid around lung
    • Haemorrhoids or bleeding
    • Low blood phosphate or calcium
    • Tingling sensation/feeling of numbness
    • Muscle spasm
    • Chills
    • Swelling of eyelids
    • Runny nose
    • High level of liver enzymes

    • Heart problems, tachycardia or rapid heartbeat, heart failure

      (breathlessness, difficulty breathing when lying down, swelling of the feet or legs)

    • Pink eye
    • Swelling of gums (gingivitis)
    • Feeling depressed
    • Loss of taste (ageusia)

If any of these affects you severely, tell your doctor.

Uncommon side effects:

These side effects may affect between 1 and 10 in every 1,000 patients.

  • A type of anaemia called pure red cell aplasia
  • Onset of diabetes
  • Abnormal wound healing
  • Absence of menstrual periods (amenorrhoea)
  • Loss of hearing

If any of these affects you severely, tell your doctor.

Treatment of angiomyolipoma of the kidney associated with TSC

Very common side effects:

These side effects may affect more than 1 in 10 patients.

  • Low level of red blood cells (anaemia)
  • Low level of white blood cells (leukopenia)

  • High level of cholesterol in the blood

    (hypercholesterolaemia)

  • Mouth ulcers. AFINITOR® can cause mouth ulcers and

    sores. Tell your doctor if you have pain, discomfort, or open sores in your mouth. You might need treatment with a mouthwash or gel. Some mouthwashes and gels can make ulcers worse, so do not try anything without checking with your doctor first.

  • Middle ear infection
  • Stomach upsets like feeling sick (nausea)
  • Being sick (vomiting)
  • Diarrhoea
  • Abdominal pain

  • Swelling of arms, hands, feet, ankles or other part of the

    body (signs of oedema)

  • Upper respiratory tract infection
  • Acne
  • Skin rash
  • Itchy rash (eczema)

  • High level of an enzyme, called blood lactate

    dehydrogenase, in the blood that gives information about the health of certain organs

  • Low level of phosphate in the blood (hypophosphatemia)
  • Joint pain
  • Headache
  • Cough

  • Menstruation disorders such as absence of periods

    (amenorrhoea), irregular periods, heavy periods (menorrhagia)

Common side effects:

These side effects may affect between 1 and 10 in every 100 patients.

  • Rash, itching, hives, difficulty breathing or swallowing,

    dizziness, signs of serious allergic reaction (hypersensitivity)

  • Menstruation disorders such as vaginal bleeds, delayed

    periods, or infrequent periods (oligomenorrhoea)

  • Rash with pus-filled blister

  • Rash with small, fluid-filled blisters on the mouth (mouth

    herpes)

  • Fever, coughing, difficulty breathing, wheezing, signs of

    inflammation of the lung (pneumonia)

  • Inflammation of the sinuses and nasal passages (sinusitis).

    Symptoms may include headache, pressure in the eyes, nose or cheek area

  • Low level of platelets (thrombocytopenia)

  • A special lung functional test result decreased (carbon

    monoxide test)

    • High level of an enzyme called blood alkaline

      phosphatase, in the blood that gives information about the health of certain organs

    • High level of an enzyme, called blood gamma-

      glutamyltransferase, in the blood that gives information about the health of your liver

    • High level of lipids in the blood (hyperlipidaemia)
    • Decreased appetite
    • Low level of iron (iron deficiency)
    • Severe headache often accompanied by nausea, vomiting and sensitivity to light (migraine)
    • Disturbed taste (dysgeusia)
    • Loss of taste (ageusia)
    • Nose bleeds (epistaxis)
    • Excess amount of gas in the bowels (flatulence)
    • An inflammatory condition of the skin characterized by redness, itching, and oozing liquid-filled cysts which become scaly, crusted, or hardened (dermatitis acneiform)
    • Dry skin
    • Fever, coughing, difficulty breathing, wheezing, signs of inflammation of the lung (pneumonitis)
    • Feeling depressed
    • Sudden, severe increase in blood pressure
    • Inability to sleep (insomnia)
    • Aggression
    • Mouth pain
    • Higher level of ovulation triggering hormone (blood luteinising hormone increased)
    • Higher level of female reproductive hormone (blood follicle stimulating hormone increased)

    • Swollen, bleeding gums, signs of gum inflammation

      (gingivitis)

    • Bad pain in the lower abdomen and pelvic area that may be sharp, with menstrual irregularities (ovarian cyst)

If any of these affects you severely, tell your doctor.

Treatment of SEGA associated with TSC

Very common side effects:

These side effects may affect more than 1 in 10 patients.

  • Infections, such as inflammation of the sinuses and nasal passages (sinusitis), middle or outer ear infection, gastric infection, sore throat and runny nose, skin infections, ringworm (a fungus infection of the skin), infections of the hair follicle, urinary tract infection, conjunctivitis, upper respiratory tract infection, pneumonia.

  • Mouth ulcers: AFINITOR® can cause mouth ulcers and sores.

    Tell your doctor if you have pain, discomfort, or open sores in the mouth. Your doctor may tell you to use a special mouthwash or mouth gel that does not contain alcohol or peroxide.

  • High level of cholesterol in the blood
  • High levels of fats in the blood (raised triglycerides)
  • Cough
  • Diarrhoea and constipation
  • Skin problems (such as rash, acne, dry skin or scratching of the skin)
  • Fever

  • Low white blood cells (a type of blood cell that fights

    infections; your doctor will check periodically)

  • Vomiting
  • Stomach pain
  • Seizure
  • Headache
  • Dizziness
  • Stuffy or runny nose
  • Change in personality
  • Loss of appetite
  • High level of sugar in the blood (hyperglycemia)
  • High blood pressure (hypertension)
  • Sore throat and runny nose (nasopharyngitis)

If any of these affects you severely, tell your doctor.

Common side effects:

These side effects may affect between 1 and 10 in every 100 patients.

  • Abscess of limb
  • Bronchitis viral
  • Low level of red blood cells (anaemia)
  • Aggression
  • Inability to sleep (insomnia)
  • Feeling agitated
  • Fits (convulsions)
  • Nose bleeds
  • Throat inflammation
  • Inflammation of the stomach lining (gastritis)
  • A pink itchy rash on your body called pityriasis rosea
  • Protein in the urine

  • Menstruation disorders, such as absence of periods

    (amenorrhoea), irregular periods

  • Feeling tired
  • Irritability
  • Trouble walking (gait disturbance)
  • Decrease antibody levels in the blood (ask your doctor)
  • Increased low density lipoprotein in the blood
  • Pain in the mouth
  • Pain in the mouth or throat

  • Rash of small fluid-filled blisters, appearing on reddened skin,

    signs of viral infection that can be potentially severe (herpes zoster)

  • Higher level of ovulation triggering hormone (blood

    luteinising hormone increased)

  • Urinary tract infection

  • Swollen, bleeding gums, signs of gum inflammation

    (gingivitis)

  • Weight loss
  • Abnormal kidney function test results
  • Abdominal pain
  • Decrease of a special protein (fibrinogen) that helps blood clot
  • Bacterial skin infection
  • Absence of sperms

If any of these affects you severely, tell your doctor.

Treatment of seizures associated with TSC:

Very common side effects:

  • Mouth ulcers. AFINITOR® can cause mouth ulcers and sores. Tell your doctor if you have pain, discomfort, or open sores in your mouth. You might need treatment with a mouthwash or gel. Some mouthwashes and gels can make ulcers worse, so do not try anything without checking with your doctor first
  • Diarrhoea
  • Throwing up (vomiting)
  • Sore throat and runny nose (nasopharyngitis)
  • Upper respiratory tract infection
  • Fever
  • Cough
  • Low level of white blood cells which help fight infections (leukopenia, lymphopenia, neutropenia). This could increase chances of contracting different types of infection.
  • Low level of red blood cells (anaemia)

  • Low level of blood cells called platelets

    (thrombocytopenia) which are responsible to control bleeding. This could increase risk of bleeding.

  • High level of fat called cholesterol in the blood

    (hypercholesterolaemia)

  • High level of fats in the blood called triglycerides

    (Hypertriglyceridemia)

  • Increased levels of enzymes liver enzymes in the blood which give information about health of liver.
  • High level of sugar in the blood (hyperglycemia)
  • High level of an enzyme called alkaline phosphatase, in the blood that gives information about the health of certain organs mainly liver and bones.

Common side effects:

  • Rash
  • Constipation
  • Feeling sick (nausea)
  • Gas in the stomach and bowels (flatulence)
  • Inflammation of the stomach lining (gastritis)
  • Abdominal pain
  • Feeling tired
  • Sore throat (pharyngitis)

  • Inflammation of the tissue in one or both lungs

    (pneumonia), with cough, fever and difficulty in breathing

  • Inflammation of the lining of the sinuses (hollow spaces in the bones of the face around nose) (sinusitis)
  • Urinary tract infection

  • Infection of stomach and intestines by a virus

    (gastroenteritis and intestinal flu)

  • Inflammation and swelling of gums(gingivitis)
  • Ear infection
  • Skin inflammation (cellulitis)
  • High level of an enzyme, called blood lactate dehydrogenase, in the blood that gives information about the health of certain organs
  • Higher level of ovulation triggering hormone (blood luteinising hormone increased)
  • Decreased appetite
  • Headache
  • Irritability
  • Aggression
  • Inability to sleep (insomnia)
  • Protein in the urine
  • Absence of periods (amenorrhoea) or irregular periods or heavy periods (menorrhagia)
  • Nose bleeds (epistaxis)
  • Fever, coughing, difficulty breathing, wheezing, signs of inflammation of the lung (pneumonitis)
  • Acne
  • Dry skin
  • High blood pressure (hypertension)

  • Low level of a chemical called phosphate in the blood

    (hypophosphatemia), which is responsible for health of bones, teeth and muscles.

If any of these affects you severely, tell your doctor.

SERIOUS SIDE EFFECTS, HOW OFTEN THEY HAPPEN AND WHAT TO DO ABOUT THEM
Symptom / effect

Talk with your

doctor or pharmacist

Stop taking drug and call your doctor or pharmacist

Only if

severe

In all cases
Very commonPain, discomfort or sores in the mouth√
Common

Lung or breathing problems

(pneumonitis, pulmonary

embolism, acute respiratory

syndrome)

(cough, chest

pain, shortness of breath)

√
Fever or chills or other signs of an infection as you might need urgent treatment√

Increased

frequency in

urination; kidney failure

√
SERIOUS SIDE EFFECTS, HOW OFTEN THEY HAPPEN AND WHAT TO DO ABOUT THEM

Symptom / effect

Rash, itching, hives, difficulty breathing or swallowing, dizziness, signs of serious allergic reaction (swelling of the face, lips, tongue or throat) (hypersensitivity) Coughing up blood

Talk with your doctor or pharmacistStop taking drug and call your doctor or pharmacist
Only if severeIn all cases
√
√
UncommonSwelling and/or pain, and redness or warm skin in your leg, usually affecting the calf (deep vein thrombosis)√
Blood in urine√
Unexpected vaginal bleeding√

Severe abdominal pain, vomiting blood, black or bloody stools, swelling of the abdomen, constipation

(gastrointestinal bleeding)

√
Hepatitis B reactivation with symptoms of fever, skin rash, joint pain and inflammation, tiredness, loss of appetite, nausea, yellowing of the skin, pain in the upper abdomen, pale stool or dark urine√

Swelling of the airways or tongue, with or without respiratory impairment

(angioedema)

√
SERIOUS SIDE EFFECTS, HOW OFTEN THEY HAPPEN AND WHAT TO DO ABOUT THEM

Symptom / effect

Fever, chills,

rapid breathing and heart rate, rash, and possibly confusion and disorientation (signs of serious infection, also known as sepsis)

Talk with your

doctor or pharmacist

Stop taking drug and call your doctor or pharmacist

Only if

severe

In all cases
√

Reported from post-

marketing

with unknown frequency

Severe headache, weakness or

paralysis of limbs or face, difficulty speaking, sudden loss of

consciousness (bleeding in the brain)

√

Muscle pain,

tenderness and weakness that you cannot explain

√

Brownish or

discoloured urine

√

This is not a complete list of side effects. For any unexpected effects while taking AFINITOR or AFINITOR DISPERZ, contact your doctor or pharmacist.

HOW TO STORE IT

Do not use after the expiry date shown on the box.

Store at room temperature (15–30°C). Store in the original package to protect from light and moisture.

Keep out of the reach and sight of children and pets.

You can report any suspected adverse reactions associated with the use of health products to the Canada Vigilance Program by one of the following 3 ways:

  • Report online at www.healthcanada.gc.ca/medeffect
  • Call toll-free at 1-866-234-2345

  • Complete a Canada Vigilance Reporting Form and:

    • Fax toll-free to 1-866-678-6789, or

    • Mail to: Canada Vigilance Program Health Canada

      Postal Locator 1908C

      Ottawa, ON K1A 0K9

Postage paid labels, Canada Vigilance Reporting Form and the adverse reaction reporting guidelines are available on the MedEffect™ Canada Web site at

www.healthcanada.gc.ca/medeffect.

NOTE: Should you require information related to the management of side effects, contact your health professional. The Canada Vigilance Program does not provide medical advice.

MORE INFORMATION

This document plus the full product monograph, prepared for health professionals can be found at:

http://www.novartis.ca

or by contacting the sponsor,

Novartis Pharmaceuticals Canada Inc. at:

1-800-363-8883

Novartis Pharmaceuticals Canada Inc.

385 Bouchard Blvd.

Dorval, Quebec, H9S 1A9

Last revised: November 16, 2017

AFINITOR, AFINITOR DISPERZ and SANDOSTATIN LAR are registered trademarks of Novartis Pharmaceuticals Canada Inc.

RAPAMUNE and TORISEL are registered trademarks of Pfizer Canada Inc.

About this document

Source: Health Canada – Drug Product Database (DPD) and product monographs · DIN (Drug Identification Number): 02450267

Revision date stated in the text: November 16, 2017

Found a mistake? Write to us via the contact page.

The information on this site does not replace the advice of a doctor or pharmacist.

Drug information for Afinitor

Rx or OTC
Prescription (Rx)?
DIN 02450267
Schedule(s) PRESCRIPTION
Active ingredient(s) Everolimus 7.5 MG
Dosage form(s) Tablet
Route(s) of administration Oral
Drug class (WHO ATC)
  1. L Antineoplastic and immunomodulating agents
    1. L04 Immunosuppressants
      1. L04A Immunosuppressants
        1. L04AH02 Everolimus
Company NOVARTIS PHARMACEUTICALS CANADA INC
Current status Cancelled Post Market
Current status date July 9, 2018

Source: Health Canada – Drug Product Database (DPD) and product monographs, data as of November 1, 2026. Data from the Health Canada Drug Product Database, as published there. Not a substitute for the advice of a doctor or pharmacist.