Afinitor

Generic Name: everolimus (Oral route)

e-ver-OH-li-mus

Oral route(Tablet)

Zortress(R): Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of transplant patients should prescribe everolimus. Reduced doses of cyclosporine should be used in combination with everolimus in order to reduce renal dysfunction and monitoring of cyclosporine and everolimus whole blood trough concentrations is recommended. The use of everolimus has resulted an increase risk of graft loss within the first 30 days post-transplantation .

Commonly used brand name(s)

In the U.S.

• Afinitor


• Zortress

Available Dosage Forms:

• Tablet

Therapeutic Class: Immune Suppressant

Uses For Afinitor

Everolimus is used to treat advanced (late-stage) kidney cancer in patients who have already been treated with other medicines (e.g., sorafenib, sunitinib) that did not work well.

Everolimus belongs to the group of medicines known as antineoplastics or cancer medicines. It works by interfering with the growth of cancer cells, which are eventually destroyed. Since the growth of normal body cells may also be affected, other unwanted effects will also occur. Some of these may be serious and must be reported to your doctor, while others may cause concern but may not be serious.

Everolimus is also used together with other medicines to lower the body's natural immunity in patients who receive kidney transplants. When a patient receives an organ transplant, the body's white blood cells will try to get rid of (reject) the transplanted organ. Everolimus works to suppress the immune system and prevents the white blood cells from getting rid of the transplanted organ.

This medicine is also used to treat subependymal giant cell astrocytoma (SEGA), a brain tumor seen in patients with an inherited condition called tuberous sclerosis (TS).

Everolimus is also used to treat a type of pancreatic cancer called pancreatic neuroendocrine tumor (PNET), that has advanced, metastatic (cancer that has spread), or cannot be treated with surgery.

Before you begin treatment with everolimus, you and your doctor should talk about the benefits this medicine will do as well as the risks of using it.

This medicine is available only with your doctor's prescription.

Before Using Afinitor

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of everolimus in the pediatric population. Safety and efficacy have not been established.

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of everolimus to treat SEGA in children. However, safety and efficacy have not been established in children younger than 3 years of age.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of everolimus in the elderly.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	D	Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Adenovirus Vaccine Type 4, Live


• Adenovirus Vaccine Type 7, Live


• Amprenavir


• Aprepitant


• Atazanavir


• Bacillus of Calmette and Guerin Vaccine, Live


• Carbamazepine


• Clarithromycin


• Cyclosporine


• Diltiazem


• Efavirenz


• Erythromycin


• Fluconazole


• Fosamprenavir


• Indinavir


• Influenza Virus Vaccine, Live


• Itraconazole


• Ketoconazole


• Lovastatin


• Measles Virus Vaccine, Live


• Mumps Virus Vaccine, Live


• Nefazodone


• Nelfinavir


• Nicardipine


• Phenobarbital


• Phenytoin


• Poliovirus Vaccine, Live


• Posaconazole


• Rifabutin


• Rifampin


• Rifapentine


• Ritonavir


• Rotavirus Vaccine, Live


• Rubella Virus Vaccine, Live


• Saquinavir


• Simvastatin


• Smallpox Vaccine


• St John's Wort


• Telithromycin


• Typhoid Vaccine


• Varicella Virus Vaccine


• Verapamil


• Voriconazole


• Yellow Fever Vaccine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Blood clotting problems or


• Diabetes or


• Hepatitis B infection, history of or


• Hyperglycemia (high sugar in the blood) or


• Hyperlipidemia (high cholesterol in the blood) or


• Hypertriglyceridemia (high fat in the blood) or


• Hypoxia (low oxygen in the blood) or


• Lung or breathing problems or


• Lymphoma (cancer of the lymph glands) or


• Proteinuria (protein in the urine) or


• Skin cancer—Use with caution. May make these conditions worse.

• Galactose intolerance or


• Glucose-galactose malabsorption (a rare genetic disorder) or


• Lactose intolerance or


• Lapp lactase deficiency (a rare genetic disorder) or


• Liver disease, severe—Should not be used in patients with these conditions.

• Infection (e.g., bacteria, fungus, virus, or protozoa)—May decrease your body's ability to fight infection.

• Liver disease, mild to moderate—Use with caution. You may require a smaller dose. Talk with you doctor if you have concerns about this.

Proper Use of everolimus

This section provides information on the proper use of a number of products that contain everolimus. It may not be specific to Afinitor. Please read with care.

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

If you have a kidney transplant, you might have to take this medicine for the rest of your life to prevent rejection of the kidney. Do not change your dose or stop taking this medicine without first checking with your doctor.

This medicine comes with a Medication Guide and a patient information leaflet. Read the information carefully and make sure you understand it before taking this medicine. If you have any questions, talk to your doctor.

Everolimus works best when there is a constant amount in the blood. You can keep the amount constant by taking the dose at the same time each day.

You may take this medicine with or without food. However, you should take it the same way (with or without food) each time.

Swallow the tablet whole with a glass of water. Do not break, crush, or chew it. If you accidentally break or crush the tablet, wash your hands with water right away.

If you cannot swallow the tablets, you may dissolve the tablets in a glass (30 mL) of water. Gently stir it before drinking the medicine. Rinse the glass with the same amount of water and swallow it immediately.

Grapefruits and grapefruit juice may increase the effects of everolimus by increasing the amount in the body. You should not eat grapefruit or drink grapefruit juice while you are taking this medicine.

If you have a kidney transplant, everolimus will be given together with another medicine that suppresses the immune system called cyclosporine. It should be taken at the same time with the cyclosporine capsules.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  
  • For advanced kidney cancer:
    
    • Adults—10 milligrams (mg) once a day. Your doctor may adjust your dose if needed.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For brain tumor or subependymal giant cell astrocytoma (SEGA):
    
    • Adults and children 3 years of age and older—Dose is based on body size and must be determined by your doctor. The starting dose is 2.5 to 7.5 milligrams (mg) once a day. Your doctor may adjust your dose if needed.
    
    
    • Children younger than 3 years of age—Use and dose must be determined by your doctor.
    
    
  
  
  • To prevent kidney transplant rejection:
    
    • Adults—At first, 0.75 milligram (mg) two times per day, spaced 12 hours apart. Your doctor may adjust your dose if needed.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For advanced pancreatic cancer or pancreatic neuroendocrine tumor (PNET):
    
    • Adults—10 milligrams (mg) once a day. Your doctor may adjust your dose if needed.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you miss a dose of this medicine, you may still take it up to 6 hours after the time you normally take it. However, if it is more than 6 hours, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Protect the medicine from direct light. Keep your medicine in the original package until you are ready to use it.

Precautions While Using Afinitor

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control while you are using this medicine and for at least 8 weeks after stopping treatment. If you think you have become pregnant while using the medicine, tell your doctor right away.

If you are male and plan to have children, talk with your doctor before using this medicine. This medicine may decrease fertility in men.

This medicine may cause a serious lung problem called noninfectious pneumonitis. Stop using this medicine and check with your doctor right away if you have chest pain, chills, a cough, fever, shortness of breath, or troubled breathing.

Check with your doctor right away if you develop the following symptoms while using this medicine: agitation; coma; confusion; decreased urine output; depression; dizziness; headache; hostility; irritability; lethargy; muscle twitching; nausea; rapid weight gain; seizures; stupor; swelling of the face, ankles, or hands; or unusual tiredness or weakness. These may be symptoms of a serious kidney problem.

While you are being treated with everolimus, and after you stop taking it, it is important to talk to your doctor about the immunizations (vaccines) you should receive. Do not get any vaccine without your doctor's approval. Everolimus may lower your body's resistance and there is a chance you might get the infection the vaccine is meant to prevent. In addition, other persons living in your household should not receive certain vaccines since there is a chance they could pass the infection on to you. Talk to your doctor if you have questions about this.

Everolimus can temporarily lower the number of white blood cells in your blood, which increases the chance of getting an infection and prevents you from healing correctly after an injury. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.


• Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in the urine or stools; or pinpoint red spots on your skin.


• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.


• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.


• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.


• Avoid contact sports or other situations where bruising or injury could occur.

This medicine may increase your risk for getting skin cancer. When you begin taking this medicine:

• Stay out of direct sunlight, especially between the hours of 10:00 a.m. and 3:00 p.m., if possible.


• Wear protective clothing, including a hat, and sunglasses.


• Apply a sunblock product that has a skin protection factor (SPF) of at least 15, or higher if you have a fair complexion.


• Apply a sunblock lipstick that has an SPF of at least 15 to protect your lips.


• Do not use sunlamps, tanning beds, or tanning booths.


• If you have any questions about this, check with your doctor.

Everolimus may cause a serious type of allergic reaction called angioedema. This may occur more often when it is used with certain heart and blood pressure medicines called ACE inhibitors (e.g., captopril [Capoten®], enalapril [Vasotec®], fosinopril [Monopril®], quinapril [Accupril®], or ramipril [Altace®]). Stop taking this medicine and tell your doctor right away if you have a rash; itching; a large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs; trouble with breathing; or chest tightness while you are using this medicine.

If you have a kidney transplant, this medicine may increase your risk for having a blood clot in the new kidney. This usually occurs within the first 30 days after the kidney transplant. Check with your doctor right away if you are making less urine, or if you have pain in your groin, lower back, side, or stomach; dark-colored urine; a fever; or nausea or vomiting.

If you are taking this medicine after a kidney transplant, it may increase your risk for developing a rare and serious virus infection called BK virus-associated nephropathy (BKVAN). The BK virus may affect how your kidneys work and cause a transplanted kidney to fail. Check with your doctor right away if you are having more than one of these symptoms: bloody urine; a decreased frequency or amount of urine; increased thirst; loss of appetite; lower back or side pain; nausea; swelling of the face, fingers, or lower legs; trouble with breathing; unusual tiredness or weakness; vomiting; or weight gain.

Everolimus may cause mouth ulcers and sores in some patients. Tell your doctor right away if you have pain, discomfort, or open sores in your mouth while you are using this medicine. You may use a special mouthwash or mouth gel to treat these ulcers. Ask your doctor what type of products to use.

This medicine may affect blood sugar levels. If you notice a change in the results of your blood or urine sugar tests or if you have any questions, check with your doctor.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (e.g., St. John's wort) or vitamin supplements.

Afinitor Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Bloating or swelling of the face, arms, hands, lower legs, or feet


• bloody nose


• chest pain


• cough or hoarseness


• cracked lips


• decreased weight


• diarrhea


• difficult or labored breathing


• difficulty with swallowing


• fever or chills


• general feeling of discomfort or illness


• lower back or side pain


• painful or difficult urination


• rapid weight gain


• shortness of breath


• sores, ulcers, or white spots on the lips, tongue, or inside the mouth


• swelling or inflammation of the mouth


• thickening of bronchial secretions


• tightness in the chest


• tingling of the hands or feet


• troubled with breathing


• unusual weight gain or loss


• wheezing

Less common

• Bleeding after defecation


• bleeding gums


• bloody urine


• blurred vision


• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings


• coughing up blood


• decreased frequency or amount of urine


• decreased urine output


• dilated neck veins


• dry mouth


• extreme fatigue


• fast, pounding, or irregular heartbeat or pulse


• flushed, dry skin


• fruit-like breath odor


• headache


• increased blood pressure


• increased hunger


• increased menstrual flow or vaginal bleeding


• increased thirst


• increased urination


• irregular breathing


• loss of appetite


• loss of consciousness


• nausea


• nervousness


• nosebleeds


• paralysis


• pounding in the ears


• prolonged bleeding from cuts


• red or black, tarry stools


• red or dark brown urine


• runny nose


• slow heartbeat


• sore throat


• stomachache


• sweating


• uncomfortable swelling around the anus


• unexplained weight loss


• unusual tiredness or weakness


• vomiting


• weight gain

Incidence not known

• Agitation


• coma


• confusion


• depression


• dizziness


• hostility


• irritability


• lethargy


• muscle twitching


• rapid weight gain


• seizures


• stupor


• swelling of the face, ankles, or hands

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach pain


• change in taste


• dry skin


• itching skin


• lack or loss of strength


• loss of taste


• pain in the arms or legs


• rash


• sleeplessness


• trouble with sleeping


• unable to sleep

Less common

• Back pain


• blistering, peeling, redness, or swelling of the palms, hands, or bottoms of the feet


• bumps on the skin


• burning, dry, or itching eyes


• discharge or excessive tearing


• discoloration of the fingernails or toenails


• excess air or gas in the stomach or intestines


• flushing or redness of the skin


• full feeling


• jaw pain


• numbness, pain, tingling, or unusual sensations in the palms of the hands or bottoms of the feet


• passing gas


• redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid


• sleepiness or unusual drowsiness


• unusually warm skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

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

See also: Afinitor side effects (in more detail)

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More Afinitor resources

• Afinitor Side Effects (in more detail)
• Afinitor Dosage
• Afinitor Use in Pregnancy & Breastfeeding
• Drug Images
• Afinitor Drug Interactions
• Afinitor Support Group
• 1 Review for Afinitor - Add your own review/rating

• Afinitor Monograph (AHFS DI)


• Afinitor Consumer Overview


• Afinitor MedFacts Consumer Leaflet (Wolters Kluwer)


• Afinitor Prescribing Information (FDA)


• Everolimus Professional Patient Advice (Wolters Kluwer)


• Zortress Prescribing Information (FDA)


• Zortress MedFacts Consumer Leaflet (Wolters Kluwer)


• Zortress Consumer Overview

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