Trade Name: Afinitor®
Everolimus is the generic name for the trade name drug Afinitor. In some cases, health care professionals may use the brand name Afinitor when referring to the generic drug name everolimus.
Everolimus is an antineoplastic chemotherapy drug. This medication is classified as an “mTOR kinase inhibitor.” (For more detail, see “How Everolimus Works” below).
Uses of Everolimus*
- Breast Cancer: Treatment (in combination with exemestane) of advanced breast cancer in postmenopausal women following failure of letrozole or anastrozole therapy.
- Neuroendocrine Tumors (NET): Treatment of certain advanced neuroendocrine tumors of pancreatic, gastrointestinal, or lung origin.
- Renal Cell Carcinoma (RCC): Treatment of advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib.
Note: If a drug has been approved for one use, physicians may elect to use this same drug for other problems if they believe it may be helpful. Everolimus has also been used in heart, liver or kidney transplantation, Waldenstrom macroglobulinemia, and certain carcinoid tumors.
*This list is not all-inclusive. It is important to discuss the decision to start or stop any medication, including everolimus, closely with your physician.
How Everolimus Is Given
- Everolimus is in the form of a tablet
- Take at the same time each day.
- Everolimus may be taken with or without food, however it is important to remain consistent with the choice.
- Swallow whole with a glass of water, do not chew or crush tablets.
- Avoid contact with or exposure to crushed or broken tablets.
- There are 4 tablet strengths
- 2.5mg tablet; white to slightly yellow, elongated tablet with a beveled edge and no score, engraved with “LCL” on one side and “NVR” on the other.
- 5mg tablet; white to slightly yellow, elongated tablet with a beveled edge and no score, engraved with “5” on one side and “NVR” on the other.
- 7.5 mg tablet; white to slightly yellow, elongated tablet with a beveled edge and no score, engraved with “7P5” on one side and “NVR” on the other.
- 10mg tablet; white to slightly yellow, elongated tablet with a beveled edge and no score, engraved with “UHE” on one side and “NVR” on the other.
- The amount of everolimus that you will receive will be prescribed by your doctor based on established dosing guidelines.
- Missed doses may be taken up to 6 hours after the regularly scheduled time. If it has been 6 hours or more since the missed dose, skip the missed dose and go back to your normal time. DO not take 2 doses at the same time or extra doses.
Important things to remember about the side effects of everolimus:
- You will not get all of the everolimus side effects mentioned below.
- Everolimus side effects are often predictable in terms of their onset, duration, and severity.
- The Everolimus side effects are almost always reversible and will go away after therapy is complete.
- Everolimus side effects may be quite manageable. There may be options to minimize or prevent them.
Side effects that are very rare, occurring in less than about 10 percent of patients. But you should always inform your health care provider if you experience any unusual symptoms.
When to Contact Your Doctor or Health Care Provider
Contact your health care provider immediately, day or night, if you should experience any of the following symptoms:
- Fever of 100.4° F (38° C) or higher, chills (possible signs of infection)
The following symptoms require medical attention, but are not an emergency. Contact your health care provider within 24 hours of noticing any of the following:
- Nausea (interferes with ability to eat and unrelieved with prescribed medication)
- Vomiting (vomiting more than 4-5 times in a 24 hour period)
- Diarrhea (4-6 episodes in a 24-hour period)
- Unusual bleeding or bruising
- Black or tarry stools, or blood in your stools
- Blood in the urine
- Pain or burning with urination
- Extreme fatigue (unable to carry on self-care activities)
- Mouth sores (painful redness, swelling or ulcers)
Always inform your health care provider if you experience any unusual symptoms.
- Before starting everolimus treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.).
- Do not take aspirin, or products containing aspirin unless your doctor specifically permits this.
- Do not receive any kind of immunization or vaccination without your doctor’s approval while taking everolimus.
- Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Everolimus is a pregnancy category C (use in pregnancy only when benefit to the mother outweighs the risk to the fetus).
- Due to the potential for serious adverse reactions in the nursing infant, breast-feeding is not recommended by the manufacturer during therapy and for 2 weeks following the last dose.
- Drink at least two to three quarts of fluid every 24 hours
- You may be at risk of infection so try to avoid crowds or people with colds, and report fever or any other signs of infection immediately to your health care provider.
- Wash your hands often.
- To help treat/prevent mouth sores, use a soft toothbrush, and rinse three times a day with 1 teaspoon of baking soda mixed with 8 ounces of water.
- Use an electric razor and a soft toothbrush to minimize bleeding.
- Avoid contact sports or activities that could cause injury.
- To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals.
- Avoid sun exposure. Wear SPF 30 (or higher) sunblock and protective clothing.
- In general, drinking alcoholic beverages should be kept to a minimum or avoided completely. You should discuss this with your doctor.
- Get plenty of rest.
- Maintain good nutrition.
- If you experience symptoms or side effects, be sure to discuss them with your health care team. They can prescribe medications and/or offer other suggestions that are effective in managing such problems.
Monitoring and Testing While Taking Everolimus
Regular checkups by your doctor while you are taking everolimus, to monitor side effects and check your response to therapy. Periodic blood work to monitor your complete blood count (CBC) as well as the function of other organs (such as your kidneys and liver). Other labs may also be necessary.
How Everolimus Works
Targeted therapy is a result of about 100 years of research to understand the differences between cancer cells and normal cells. To date, cancer treatment has focused primarily on killing rapidly dividing cells because one feature of cancer cells is that they divide rapidly. Unfortunately, some of our normal cells divide rapidly too, causing multiple side effects.
Targeted therapy is about identifying other features of cancer cells. Scientists look for specific differences in the cancer cells and the normal cells. This information helps to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects. Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or communicate with other cells.
There are different types of targeted therapies, defined in three broad categories. Some targeted therapies focus on the internal components and function of the cancer cell. The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die. There are several types of targeted therapy that focus on the inner parts of the cells. Other targeted therapies target receptors that are on the outside of the cell. Antiangiogenesis inhibitors target the blood vessels that supply oxygen to the cells, ultimately causing the cells to starve.
Everolimus is an inhibitor of mTOR. mTOR inhibition blocks the translation of genes that regulate cancer cell proliferation. It also results in reduced levels of certain cell growth factors involved in the development of new blood vessels, such as vascular endothelial growth factor (VEGF).
Research continues to identify which cancer may be best treated with targeted therapies and to identify additional targets for more types of cancer.