Afinitor (Everolimus) - Oral

Warning:

Radiation sensitization and recall can occur in people treated with radiation prior to, during, or subsequent to Afinitor treatment. Inform your healthcare provider if you have had or are planning to receive radiation therapy.

What Is Afinitor?

Afinitor (everolimus) is an oral prescription drug used to treat several types of cancer, including breast cancer, kidney cancer, and multiple types of neuroendocrine cancers. Afinitor is approved by the Food and Drug Administration (FDA) for people 1 and older. However, it is most commonly used in females 60 and older.

Afinitor is classified as a rapalog. Rapalogs are closely related to the initial drug in this category of medications that scientists first developed, called rapamycin (an immunosuppressant drug).

Rapalogs work by blocking a protein that usually activates many other proteins involved in cell growth. As such, rapalogs can be helpful in treating cancer, where cell growth can become uncontrollable.

Afinitor is further categorized as a mammalian target of rapamycin (mTOR) inhibitor, which comes from the name of the specific protein that they block. Rapalogs are the first-generation form of mTOR inhibitors.

While not available for purchase as a generic product, Afinitor is available as a tablet you take by mouth (oral).

Afinitor's primary ingredient, everolimus, is also present in another similar brand-name drug—Afinitor Disperz. Afinitor Disperz is administered as a drug dissolved in water (liquid suspension).

This article will focus on the oral use of everolimus, commonly referred to as Afinitor (a brand-name version of the drug).

Drug Facts

Generic Name: Everolimus

Brand Name(s): Afinitor, Afinitor Disperz, Zortress

Drug Availability: Prescription

Therapeutic Classification: Immune suppressant

Available Generically: No

Controlled Substance: N/A

Administration Route: Oral

Active Ingredient: Everolimus

Dosage Form(s): Tablet, liquid suspension

What Is Afinitor Used For?

Afinitor is FDA-approved for several different types of cancer, including:

  • Some types of breast cancer, such as advanced hormone receptor-positive, HER2-negative advanced breast cancer in combination with Aromasin (exemestane) after the failure of treatment with Femara (letrozole) or Arimidex (anastrozole).
  • Multiple types of neuroendocrine cancer, such as progressive neuroendocrine tumors of pancreatic origin (PNET) or adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable (cannot be removed via surgery), in locally advanced, or metastatic stages of severity.
  • Some types of kidney cancer, such as renal cell carcinoma (RCC). RCC is a type of kidney cancer that begins in the linings of small tubes found in the kidneys and is most commonly diagnosed in older males.

Nonetheless, cancer treatment is very complex, and Afinitor is not approved for every specific situation in these cancer types. 

Afinitor may only be an approved treatment if you have an even more specific subtype of cancer, if your cancer has spread, and if you’ve already tried other treatments.

Additionally, Afinitor is FDA-approved for some people with a condition called tuberous sclerosis complex (TSC). This condition can cause benign (noncancerous) growth in different parts of the body. Afinitor can treat these benign growths in the brain.

Examples of these benign growths treated by Afinitor include subependymal giant cell astrocytoma (SEGA) or growths found in the kidneys, like renal angiomyolipoma.

Afinitor is also FDA-approved in people who have had kidney transplants. This helps prevent organ rejection, in which the immune system attacks the donated organ. When used for this purpose, the drug is marketed and sold as Zortress.

How to Take Afinitor

Here is an overview of how to take safely take Afinitor to ensure it is effective.

Afinitor comes as a tablet you take by mouth and as a tablet to suspend in water to take orally. It is usually taken once a day to treat kidney tumors, SEGA, or seizures in people who have TSC, advanced RCC, or breast, pancreatic, intestine, stomach, or lung cancer.

When it is taken to prevent transplant rejection, Afinitor is usually taken twice a day (every 12 hours) at the same time as cyclosporine (a cancer medication).

For consistency, Afinitor should either always be taken with food or without it. Take it at around the same time every day.

Afinitor tablets come in individual blister packs that can be opened with scissors. Do not open a blister pack until you are ready to swallow the tablet.

You should take either Afinitor tablets or Afinitor Disperz tablets for oral suspension. Do not take a combination of the two.

Swallow the tablets whole with a glass of water. Do not split, chew, or crush them. Do not take tablets that have been crushed or broken.

If you are using tablets for oral suspension, you must mix them with water before you take them. Do not swallow the tablets whole. Do not mix them with juice or any liquid other than water.

Do not prepare the mixture more than 60 minutes before you plan to take it. Dispose of the mixture if it is not used within 60 minutes.

Storage

Store Afinitor at room temperature, away from heat and excess moisture (such as in the bathroom). Be sure to keep the medication out of reach of children and pets.

If you plan to travel with Afinitor, learn about your final destination's regulations. Make a copy of your Afinitor prescription and take it with you.

If possible, keep your medication in its original container from your pharmacy with your name on the label. If you have any questions about traveling with your medication, ask your healthcare provider.

Discard all unused and expired medications. Do not pour them down the drain or toilet. Ask your pharmacist or provider about the best ways to dispose of Afinitor. You can also look for drug take-back programs in your area.

Off-Label Uses

Afinitor is FDA-approved to treat very specific subtypes of cancer. In the example of breast cancer, it is technically only approved for people whose cancer has certain characteristics—such as being HER2-negative and hormone receptor-positive.

However, Afinitor is sometimes prescribed off-label for people who do not strictly meet these criteria. For example, someone with a different type of breast cancer, or a different type of cancer, like lung cancer.

Off-label use is relatively common in cancer treatment. Sometimes, the evidence suggests that a drug is helpful even if the full set of studies required for FDA approval has not been done. You can ask your healthcare provider if your prescription is considered off-label use. In some cases, this can affect reimbursement from your health insurance.

How Long Does Afinitor Take to Work?

Afinitor starts working in your body within a few hours after you take your first pill.

However, Afinitor will not necessarily cure your cancer—especially if it has already spread. However, it may prolong the time you will live after you are diagnosed.

What Are the Side Effects of Afinitor?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your pharmacist or healthcare provider. You may report side effects to the Food and Drug Administration (FDA) at fda.gov/medwatch or 1-800-FDA-1088.

Common Side Effects

Some of the more common potential side effects from everolimus treatment are:

To prevent sore mouth, your healthcare provider may recommend using a special mouthwash with dexamethasone, a type of corticosteroid.

Severe Side Effects

Radiation sensitization and recall can occur in people treated with radiation prior to, during, or subsequent to Afinitor treatment.

Tell your healthcare provider if you have had or are planning to receive radiation therapy.

Some of the potentially serious side effects of everolimus include:

  • Severe Infections
  • Dangerous allergic reaction
  • Inflammation of the lungs
  • Angioedema (severe swelling underneath the skin, which might affect breathing)
  • Increased blood sugar, causing temporary issues from diabetes
  • Increased blood fats, which might increase your risk of heart attack or stroke
  • Kidney damage

Your healthcare provider might recommend periodic blood tests to monitor you for these possible problems.

While you are on Afinitor, you’ll need to avoid getting certain types of vaccines (live vaccines). You may get a bad infection if you are vaccinated during this time.

Some vaccines to avoid while you are taking Afinitor are:

Ask your healthcare provider if you are not sure if a certain vaccine falls into this category.

Report Side Effects

Afinitor may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your healthcare provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (1-800-332-1088).

Dosage: How Much Afinitor Should I Take?

Drug Content Provided and Reviewed by IBM Micromedex®

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 breast cancer:
      • Adults—10 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For advanced neuroendocrine tumors:
      • Adults—10 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For angiomyolipomas:
      • Adults—10 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For brain tumors (SEGA):
      • Adults and children 1 year of age and older—Dose is based on body size and must be determined by your doctor. The starting dose is 4.5 milligrams (mg) per square meter (m(2)) of body size once a day. Your doctor may adjust your dose as needed.
      • Children younger than 1 year of age—Use is not recommended.
    • For kidney cancer:
      • Adults—10 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For kidney transplant rejection:
      • Adults—At first, 0.75 milligram (mg) 2 times per day, taken about 12 hours apart. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
    • For liver transplant rejection:
      • Adults—At first, 1 milligram (mg) 2 times per day, taken about 12 hours apart. Your doctor may adjust your dose as needed.
      • Children—Use and dose must be determined by your doctor.
  • For oral dosage form (tablets for suspension):
    • For brain tumors (SEGA):
      • Adults and children 1 year of age and older—Dose is based on body size and must be determined by your doctor. The starting dose is 4.5 milligrams (mg) per square meter (m(2)) of body size once a day. Your doctor may adjust your dose as needed.
      • Children younger than 1 year of age—Use is not recommended.
    • For partial-onset seizures:
      • Adults and children 2 years of age and older—Dose is based on body size and must be determined by your doctor. The starting dose is 5 milligrams (mg) per square meter (m(2)) of body size once a day. Your doctor may adjust your dose as needed.
      • Children younger than 2 years of age—Use is not recommended.

Modifications

The following modifications should be kept in mind when using Afinitor:

Severe allergic reaction: Do not use if allergic to Afinitor or any of its ingredients. Ask your pharmacist for a complete list of ingredients if you're unsure.

Pregnancy: Afinitor/Afinitor Disperz can cause fetal harm when given to pregnant people. There are limited case reports of Afinitor use in pregnant people, and they are not enough to properly inform about the risks of birth defects or miscarriage.

Talk to your healthcare provider if you are or plan to become pregnant, to weigh the benefits and risks of taking Alinia during your pregnancy.

Breastfeeding: The active part of Afinitor is present in breast milk. There is a possibility of negative reactions in a newborn, so do not breastfeed while taking Afinitor.

Adults over 65 years: In the randomized hormone receptor-positive, HER2-negative breast cancer study (BOLERO-2), deaths due to any cause within 28 days of Afinitor use was 6% in people older than 65 versus 2% in people younger than 65. Negative reactions leading to permanent treatment stoppage occurred in 33% of people older than 65 years compared to 17% in people younger than 65. Therefore, appropriate dose adjustments are encouraged in older adults.

Children: The youngest age approved for the use of Afinitor/Afinitor Disperz is 1 year old, specifically for TSC-associated SEGA that requires treatment but cannot be removed via surgery.

Missed Dose

If you miss a dose, take it as soon as you remember it. However, if it is very close to the time for your next dose, do not double up.

It likely will not make a significant difference in your cancer treatment if you skip a single dose, but try to take your medication exactly as prescribed. Doing so will help make the treatment as effective as possible.

Overdose: What Happens If I Take Too Much Afinitor?

If you accidentally take just a little more Afinitor than prescribed, it may not be a cause for concern. However, you should check in with your provider. Taking more than you have been prescribed may increase your risk of severe side effects from Afinitor.

What Happens If I Overdose on Afinitor?

If you think you or someone else may have overdosed on Afinitor, call a healthcare provider or the Poison Control Center (1-800-222-1222).

If someone collapses or isn't breathing after taking Afinitor, call 911 immediately.

Precautions

Drug Content Provided and Reviewed by IBM Micromedex®

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. It may also cause birth defects if the father is using it when his sexual partner becomes pregnant. Female patients should use an effective form of birth control during treatment with this medicine and for at least 8 weeks after the last dose. Male patients who have female partners should use effective birth control during treatment with Afinitor® or Afinitor® Disperz and for 4 weeks after the last dose. If you think you have become pregnant while using the medicine, tell your doctor right away.

If you are planning to have children, talk with your doctor before using this medicine. Some men and women using this medicine have become infertile (unable to have children).

This medicine may cause a serious lung problem called interstitial lung disease or non-infectious pneumonitis. Check with your doctor right away if you have chest pain, chills, cough, fever, or trouble breathing.

Check with your doctor right away if you have bloody urine, a decrease in frequency or amount of urine, an increase in blood pressure, increased thirst, loss of appetite, lower back or side pain, nausea, swelling of the face, fingers, or lower legs, trouble breathing, unusual tiredness or weakness, vomiting, or weight gain. These may be symptoms of a serious kidney problem.

While you are being treated with everolimus, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval. Everolimus may lower your body's resistance and the vaccine may not work as well or you might get the infection the vaccine is meant to prevent. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live virus vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.

Everolimus can temporarily lower the number of white blood cells in your blood, which increases the chance of getting an infection. 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 right away 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 right away 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 AM and 3:00 PM, if possible.
  • Wear protective clothing, including a hat and sunglasses.
  • Apply a sunblock product that has a sun 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.

This medicine may cause a serious allergic reaction called anaphylaxis, which can be life-threatening and requires immediate medical attention. Tell your doctor right away if you have a rash, itching, hoarseness, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth after using this medicine.

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 (eg, captopril [Capoten®], enalapril [Vasotec®], fosinopril [Monopril®], quinapril [Accupril®], ramipril [Altace®]). Check with 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 genitals, trouble 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 urine, fever, nausea, or vomiting.

This medicine may also prevent you from healing correctly after an injury. Do not take this medicine at least 1 week before surgery and at least 2 weeks after a surgery. Call your doctor right away if you have blood, fluid, or pus in your incision, your incision opens up, or if it is red, warm, painful, or swollen.

Make sure any doctor who treats you knows that you are using this medicine. This medicine may worsen the side effects from radiation treatment.

If you are taking this medicine after a kidney transplant, it may increase your risk for developing rare and serious virus infections, such as polyoma virus-associated nephropathy (PVAN), progressive multiple leukoencephalopathy (PML), and 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 have 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 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 (eg, dexamethasone alcohol-free oral solution) 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 have diabetes, check with your doctor if you notice a change in your blood or urine sugar tests.

Tell your doctor if you are taking a corticosteroid or another medicine that may weaken your immune system. This may increase your risk for developing a serious infection.

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 (eg, St. John's Wort) or vitamin supplements.

What Are Reasons I Shouldn't Take Afinitor?

Some data show that Afinitor may cause problems for the fetus during pregnancy. Talk to your healthcare provider about the risks and benefits of taking Afinitor in your specific situation.

If you have a history of liver disease, discuss the pros and cons of taking Afinitor with your healthcare provider. You might be able to use the drug safely at a lower dose.

You should not use Afinitor if you know you are allergic to everolimus or any of the ingredients that are in the medication.

What Other Medications Interact With Afinitor?

Using Afinitor can change how quickly your body breaks down other medications.

Also, taking some other medications can affect how long everolimus stays in your body. These are known as drug interactions.

While you are taking Afinitor, you may need to completely avoid certain drugs that have particularly strong interactions. Some examples include:

In other cases, you might be able to take the drugs at the same time if your dose is adjusted.

Talk to your healthcare provider about all of your medications, including herbal preparations and any over-the-counter (OTC) products.

What Medications Are Similar?

Cancer treatment is complex. It’s highly dependent on the specific subtype of cancer and how much it has spread in the body. Treatment options will depend on these and other factors, like medical conditions and previous treatments.

For people with advanced RCC, it’s recommended that Afinitor only be used if they have not had a good response to Sutent (sunitinib) or Nexavar (sorafenib). These drugs, known as tyrosine kinase inhibitors, work similarly to help fight cancer. If these drugs have not worked, experts are not quite which drugs are the next best options.

If you’ve already tried different cancer treatments, some other potential drug options that work similarly to Afinitor include:

Evidence suggests that Cometriq might be more effective than Afinitor in terms of prolonging survival. Morevoer, Opdivo may also be more effective than Afinitor. Regardless, your healthcare provider might suggest one of these other options first.

Your healthcare provider might also prescribe Afinitor along with another drug, such as Lenvima (lapatinib). While it might be more effective than using Afinitor by itself, you might also have an increased risk of side effects.

You and your healthcare provider will decide on the best medication or medication combination for you.

Frequently Asked Questions

  • What is Afinitor used for?

    Afinitor is used to treat several types of cancer. This includes some types of breast cancers, kidney cancers, and neuroendocrine cancers. It can also be used to treat some people who have growths from TSC.

  • How do I stop taking Afinitor?

    Do not stop taking Afinitor without talking to your provider first. Taking the medication as prescribed gives you the best chance of effectively treating your cancer. Afinitor is meant to be taken over the long term.

    If it seems like it is not working for you, you can discuss other options with your healthcare team. Your provider can also tell you about other choices if the side effects of Afinitor are a problem.

  • Can Afinitor give me an infection?

    Like a lot of drugs that treat cancer, Afinitor can make you more prone to certain kinds of infections. Some are minor, but others can be more serious. Let your healthcare provider know right away if you have signs of infection, like fever.

  • Can I get vaccinated for COVID-19 while taking Afinitor?

    Talk to your provider first. Some vaccines are fine, but if you are taking Afinitor you need to avoid vaccines that are made with live viruses, such as the one for chicken pox. Other vaccines, like the vaccines approved for COVID-19 in the United States, do not use live viruses.

  • Do I have other treatment options?

    Cancer treatment is very complex. You might be able to use another treatment instead of or in addition to Afinitor. Depending on your circumstances, you might talk to your provider about focusing on the quality of your life instead of treating your cancer. Discuss all your options with your healthcare provider to decide what's right for you.

How Can I Stay Healthy While Taking Afinitor?

If you are considering using Afinitor, you are likely dealing with a very serious health condition. Drugs like Afinitor can be one way to help you manage your health and spend more time doing the things you love. Your healthcare provider will help come up with a treatment plan that makes sense for you.

Like other cancer drugs, Afinitor can cause some serious side effects, like increasing your risk of infections.

Tell your healthcare provider right away about any new health symptoms—even if it's just something simple like a cough. Your provider can let you know whether it's a reason for concern.

15 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. DailyMed. Label: Afinitor- everolimus tablet. Afinitor Disperz- everolimus tablet, for suspension.

  2. Zheng Y, Jiang Y. mTOR inhibitors at a glanceMol Cell Pharmacol. 2015;7(2):15-20.

  3. Li J, Kim SG, Blenis J. Rapamycin: one drug, many effectsCell Metab. 2014;19(3):373-379. doi:10.1016/j.cmet.2014.01.001

  4. BreastCancer.org. Afinitor.

  5. Waldner M, Fantus D, Solari M, Thomson AW. New perspectives on mTOR inhibitors (rapamycin, rapalogs and TORKinibs) in transplantationBr J Clin Pharmacol. 2016;82(5):1158-1170. doi:10.1111/bcp.12893

  6. National Library of Medicine. Label: Afinitor- everolimus tablet. Afinitor Disperz- everolimus tablet, for suspension.

  7. Novartis Pharmaceuticals. Medication guide: Zortress (everolimus) tablets.

  8. National Library of Medicine, MedlinePlus. Everolimus.

  9. Papadimitrakopoulou VA, Soria JC, Jappe A, et al. Everolimus and erlotinib as second- or third-line therapy in patients with advanced non-small-cell lung cancer. J Thorac Oncol. 2012;7(10):1594-601. doi:10.1097/JTO.0b013e3182614835

  10. American Cancer Society. Off-label drug use.

  11. Dhakal A, Antony Thomas R, Levine EG, et al. Outcome of everolimus-based therapy in hormone-receptor-positive metastatic breast cancer patients after progression on palbociclib. Breast Cancer (Auckl). 2020;14:1178223420944864. doi:10.1177/1178223420944864

  12. Prescribers' Digital Reference. Everolimus - drug summary.

  13. Motzer RJ, Jonasch E, Boyle S, et al. NCCN guidelines insights: kidney cancer, version 1.2021. J Natl Compr Canc Netw. 2020;18(9):1160-1170. doi:10.6004/jnccn.2020.0043

  14. Amzal B, Fu S, Meng J, Lister J, Karcher H. Cabozantinib versus everolimus, nivolumab, axitinib, sorafenib and best supportive care: A network meta-analysis of progression-free survival and overall survival in second line treatment of advanced renal cell carcinoma. PLoS One. 2017;12(9):e0184423. doi:10.1371/journal.pone.0184423

  15. Motzer RJ, Escudier B, McDermott DF, et al. Nivolumab versus everolimus in advanced renal-cell carcinoma. N Engl J Med. 2015;373(19):1803-13. doi:10.1056/NEJMoa1510665

By Ruth Jessen Hickman, MD
Ruth Jessen Hickman, MD, is a freelance medical and health writer and published book author.