Afinitor

Afinitor is a prescription medication used to treat certain types of cancer in the pancreas, kidney, brain, and breast.

Afinitor belongs to a group of drugs called kinase inhibitors. It works by stopping cancer cells from reproducing and by decreasing blood supply to cancer cells.

Afinitor comes in tablet form and is usually taken once daily with a glass of water.

Common side effects include mouth ulcers, infections, and cough.

Afinitor is a prescription medicine used to treat:

• postmenopausal women with a type of breast cancer known as advanced hormone receptor-positive, HER2-negative breast cancer, along with Aromasin (exemestane) after treatment with other medication has not worked.
• adults with a type of pancreatic cancer known as pancreatic neuroendocrine tumor (PNET) that has progressed and can not be treated with surgery.  
• adults with a type of advanced kidney cancer known as renal cell carcinoma (RCC) when treatment with other medications has not worked.
• people with the following types of tumors that are seen with a genetic condition called tuberous sclerosis complex (TSC):
  • adults with a type of kidney tumor called renal angiomyolipoma, when the tumor does not need surgery right away.
  • adults and children with a type of brain tumor called subependymal giant cell astrocytoma (SEGA), when the tumor cannot be removed with surgery.

• Novartis Pharmaceuticals Corporation

Afinitor can cause serious side effects. See “Drug Precautions”.

Common side effects of Afinitor in people with advanced hormone receptor-positive, HER 2-negative breast cancer, advanced pancreatic neuroendocrine tumors, and advanced kidney cancer include:

• Mouth ulcers. Afinitor can cause mouth ulcers and sores. Tell your healthcare provider if you have pain, discomfort, or open sores in your mouth. Your healthcare provider may tell you to use a special mouthwash or mouth gel that does not contain alcohol, peroxide, iodine, or thyme.
• Infections
• Feeling weak or tired
• Cough, shortness of breath
• Diarrhea and constipation
• Rash, dry skin, and itching
• Nausea and vomiting
• Fever
• Loss of appetite, weight loss
• Swelling of arms, hands, feet, ankles, face or other parts of the body 
• Abnormal taste
• Dry mouth
• Inflammation of lining of the digestive system
• Headache
• Nose bleeds
• Pain in arms and legs, mouth and throat, back or joints 
• High blood glucose
• High blood pressure
• Difficulty sleeping
• Hair loss
• Muscle spasms
• Feeling dizzy
• Nail disorders

Common side effects of Afinitor in people with SEGA or renal angiomyolipoma with TSC include:

• Mouth ulcers. Afinitor can cause mouth ulcers and sores. Tell your healthcare provider if you have pain, discomfort, or open sores in your mouth. Your healthcare provider may tell you to use a special mouthwash or mouth gel that does not contain alcohol, peroxide, iodine, or thyme.
• Infections
• Nausea and vomiting
• Diarrhea and constipation
• Swelling of your hands, arms, legs, and feet
• Joint pain
• Cough
• Skin problems (such as rash, acne, or dry skin)
• Fever
• Feeling tired
• Anxiety, aggression, and other abnormal behaviors
• Absence of menstrual periods (menstruation). You may miss 1 or more menstrual periods. Tell your healthcare provider if this happens.
• Low red blood cells, white blood cells or platelets
• Increased blood cholesterol level and certain other blood tests
• Increased blood sugar levels
• Decreased blood phosphate levels

Tell your doctor if you have any side effect that bothers you or does not go away.

These are not all the possible side effects of Afinitor. For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088. 

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• St. John’s wort 
• Medicine for: 
        ○  Fungal infections 
        ○  Bacterial infections 
        ○  Tuberculosis
        ○  Seizures 
        ○  HIV-AIDS 
        ○  Heart conditions or high blood pressure
• Medicines that suppress your immune system

This is not a complete list of Afinitor drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with Afinitor including the following:

• Lung or breathing problems that may be severe, and can even lead to death. Tell your doctor right away if you have any of these symptoms:
  • New or worsening cough
  • Shortness of breath
  • Chest pain
  • Difficulty breathing or wheezing
• Increased risk of developing an infection, such as pneumonia, or a bacterial, fungal or viral infection. Viral infections may include active hepatitis B in people who have had hepatitis B in the past (reactivation). In some people these infections may be severe, and can even lead to death. You may need to be treated as soon as possible.
  • Tell your doctor right away if you have a temperature of 100.5˚F or above, chills, or do not feel well.
  • Symptoms of hepatitis B or infection may include the following:
    • Fever
    • Skin rash
    • Joint pain and inflammation
    • Tiredness
    • Loss of appetite
    • Nausea
    • Pale stool or dark urine
    • Yellowing of the skin
    • Pain in your upper right side
• Possible increased risk for a type of allergic reaction called angioedema, in people who take an Angiotensin-Converting Enzyme (ACE) inhibitor medicine during treatment with Afinitor. Talk with your healthcare provider before taking Afinitor if you are not sure if you take an ACE inhibitor medicine. Get medical help right away if you have trouble breathing or develop swelling of your tongue, mouth, or throat during treatment with Afinitor. 
• Kidney failure which may be severe and can even lead to death. Your doctor will likely do tests to check your kidney function before and during your treatment with Afinitor. 
• Delayed wound healing. Afinitor can cause incisions to heal slowly or not heal well. Call your healthcare provider right away if you have any of the following symptoms:
  • your incision is red, warm or painful
  • blood, fluid, or pus in your incision
  • your incision opens up
  • swelling of your incision

If you have any of the serious side effects listed above, you may need to stop taking Afinitor for a while or use a lower dose. Follow your doctor’s instructions.

Do not take Afinitor if you are allergic to Afinitor or to any of its ingredients. Talk to your doctor before taking this medicine if you are allergic to:

• sirolimus (Rapamune)
• temsirolimus (Torisel)

You should not drink grapefruit juice or eat grapefruit during your treatment with Afinitor. It may make the amount of Afinitor in your blood increase to a harmful level.

Before taking Afinitor, tell your healthcare provider about all of your medical conditions, including if you:

• Have or have had kidney problems
• Have or have had liver problems
• Have diabetes or high blood sugar
• Have high blood cholesterol levels
• Have any infections
• Previously had hepatitis B
• Are scheduled to receive any vaccinations. You should not receive a “live vaccine” or be around people who have recently received a “live vaccine” during your treatment with Afinitor. If you are not sure about the type of immunization or vaccine, ask your healthcare provider. 
• Are pregnant, or could become pregnant. Afinitor can cause harm to your unborn baby. You should use effective birth control while using Afinitor and for 8 weeks after stopping treatment. Talk to your healthcare provider about birth control options while taking Afinitor.
• Are breastfeeding or plan to breastfeed. It is not known if Afinitor passes into your breast milk. You and your healthcare provider should decide if you will take Afinitor, or breastfeed. You should not do both.

Tell your healthcare provider about all of the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant. 

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy. 

Afinitor falls into category D. Based on how the medication works, Afinitor can cause harm to an unborn baby when used by a pregnant woman.

It is not known if Afinitor crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using Afinitor.

Take Afinitor exactly as your healthcare provider tells you to.

• Your healthcare provider will prescribe the dose of Afinitor that is right for you. Take Afinitor exactly as prescribed.
• Your healthcare provider may change your dose of Afinitor or tell you to temporarily interrupt dosing, if needed.
• Do not CONFUSE Afinitor and Afinitor Disperz.
• Use scissors to open the blister pack.
• Swallow Afinitor tablets whole with a glass of water. Do not take any tablet that is broken or crushed.
• Take Afinitor 1 time each day at about the same time.
• Take Afinitor the same way each time, either with food or without food.
• If you take too much Afinitor contact your healthcare provider or go to the nearest hospital emergency room right away. Take the pack of Afinitor with you.
• If you miss a dose of Afinitor, you may still take it up to 6 hours after the time you normally take it. If it is more than 6 hours after you normally take your Afinitor, skip the dose for that day. The next day, take Afinitor at your usual time. Do not take 2 doses to make up for a missed dose. If you are not sure about what to do, call your healthcare provider.
• You should have blood tests before you start Afinitor and as needed during your treatment. These will include tests to check your blood cell count, kidney and liver function, cholesterol, and blood sugar levels.
• If you take Afinitor to treat SEGA, you will also need to have blood tests regularly to measure how much medicine is in your blood. This will help your healthcare provider decide how much Afinitor you need to take.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your liver function
• your weight
• your height

The recommended dose of Afinitor for advanced hormone receptor-positive, HER2-negative breast cancer, advanced PNET, advanced RCC, and renal angiomyolipoma with TSC is 10 mg by mouth once daily.

The recommended dose of Afinitor in SEGA with TSC is 4.5 mg/m² once daily. 

If you take too much Afinitor, call your local Poison Control Center or seek emergency medical attention right away.

• Store Afinitor at 59°–86°F (15°–30°C). 
• Store in the original container, protect from light and moisture.
• Keep this and all drugs out of the reach of children.

WARNING: MALIGNANCIES AND SERIOUS INFECTIONS, KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; AND MORTALITY IN HEART TRANSPLANTATION

Malignancies and Serious Infections

• Only physicians experienced in immunosuppressive therapy and management of transplant patients should prescribe Afinitor. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient. 
• Increased susceptibility to infection and the possible development of malignancies such as lymphoma and skin cancer may result from immunosuppression. 

Kidney Graft Thrombosis

• An increased risk of kidney arterial and venous thrombosis, resulting in graft loss, was reported, mostly within the first 30 days post-transplantation. 

Nephrotoxicity

• Increased nephrotoxicity can occur with use of standard doses of cyclosporine in combination with Afinitor. Therefore reduced doses of cyclosporine should be used in combination with Afinitor in order to reduce renal dysfunction. It is important to monitor the cyclosporine and Afinitor whole blood trough concentrations.

Mortality in Heart Transplantation

• Increased mortality, often associated with serious infections, within the first three months post-transplantation was observed in a clinical trial of de novoheart transplant patients receiving immunosuppressive regimens with or without induction therapy. Use in heart transplantation is not recommended.