What is Afinitor (Everolimus)?
Everolimus, also known as Afinitor, is an anticancer medication. This medication is most commonly used for cancer of the brain, kidneys, and breasts. The breast cancers treated are in postmenopausal women with advanced hormone receptor cancer. In these cases, Everolimus is used with exemestane after letrozole or anastrozole therapy failed.
Everolimus also treats specific types of tumors in the stomach, intestines, and pancreas. These specific tumors are advanced, progressive cancers. Everolimus is used for advanced pancreas cancer when the neuroendocrine tumors are unresectable.
Other conditions that Everolimus can treat include seizures and tuberous sclerosis complex (TSC). TSC is a genetic condition that causes benign brain and kidney tumors. Everolimus is used when surgery is not immediately necessary or when the tumors cannot be removed completely or safely.
Everolimus has also been used, off-label, in heart, liver or kidney transplantation and for Waldenstrom macroglobulinemia.
How Afinitor Everolimus works
Everolimus binds specific proteins in human cells. Binding to these cell proteins blocks cancer from interacting with specific genes in the cells. In this way, Everolimus leads to cell death, because the cancer cells are unable to reproduce without these genes. Everolimus also stops the cancer cells that develop their own blood supply. This is important because the cancer uses the body’s blood to spread cancer. Bottom line: these changes halt cancer cells from multiplying in the body.
Storage, dosage, and how to use Afinitor Everolimus
Take the tablet by mouth at the same time every day. Swallow it whole with a glass of water. Never crush or chew the tablets. Do not touch or breathe in the powder of any broken or chipped tablets. Take this drug with or without food; however, it is recommended that the drug is thereafter taken the same way.
Important – if a dose is missed, do NOT double-dose. If you accidentally take too many Everolimus tablets, contact your Provider immediately or go to the emergency department. Take the Everolimus package, so the attending emergency Provider knows exactly what has been overdosed.
Store Everolimus out of reach from others, keeping the lid secure. Children under the age of 18 cannot take this drug without a TSC specialist’s guidance. Keep the drug in its original package to protect Everolimus from light. There are no special temperature requirements.
Dosage is decided by the Prescribing Provider and based upon the condition treated. Everolimus comes in three strengths:
- White to off-white oval 2.5mg tablets – E9VS on one side and 2.5 on the other side
- White to off-white oval 5mg tablets – E9VS 5 on one side
- White to off-white oval 10mg tablets – E9VS 10 on one side
There are 30 tablets in each package.
During Everolimus treatment, routine monitoring, assessments, and examinations will be scheduled. A number of blood labs may be routinely performed.
IMPORTANT SELF-CARE TIPS:
- Drink at least 2-3 quarts of fluid every 24 hours
- Avoid crowds or any persons with colds or signs of infections
- Wash your hands often
- Use a soft toothbrush and rinse your mouth thrice daily with baking soda water
- Avoid contact sports
- Eat small but frequent meals
- Avoid sun exposure
- Avoid alcoholic beverages or keep them to a minimum
- Get plenty of rest
- Maintain good nutrition
- Discuss any side effects with the healthcare team
- Do not hesitate to contact your assigned healthcare team with questions or concerns
The most common side effects of Everolimus are:
- mouth sores
- rash, itching, dry skin
- stomach pain or cramping
- nausea, vomiting, discomfort
- blood test abnormalities
Any or some of the above is seen in more than 30% of the patients.
Less common side effects that occur in 10-29% of patients are:
- loss of appetite
- shortness of breath
- high blood pressure
- bleeding problems
- joint pain
- muscle pain
- loss of fertility
Rarely occurring side effects, occurring in less than 10% of patients, are unlisted in this drug sheet. Contact your Provider for any unusual or new symptoms.
Some symptoms are serious and should be reported to the Provider within 24 hours:
- nausea that is preventing eating
- vomiting more than 4-5 times in 24 hours
- diarrhea 4-5 episodes within 24 hours
- unusual bleeding or bruising
- black or tarry stools
- blood in urine
- pain/burning with urination
- extreme fatigue interfering with self-care
- mouth sores that become red, painful, or create ulcers
Warnings & Precautions
WARNING: Contact the Provider IMMEDIATELY, day or night, if you experience a fever of 100.4F (38C) or higher, chills, or any other sign of infection.
WARNING: Everolimus is only administered to patients under the age of 18 by a Provider experienced in treatment of young patients with tuberous sclerosis complex (TSC). These patients must be avidly monitored as a safety precaution.
WARNING: This medication reduces the immune response. Immediately report any signs of infections, especially symptoms of respiratory infections. Non-infectious pneumonitis is a known effect of the rapamycin class of drugs. Concerning symptoms to report immediately include difficulty breathing, cough, shortness of breath, and signs of lack of oxygenation such as faintness, drowsiness, and dizziness.
During therapy the patient is at risk for infections that they would not normally experience. For example, a fungal infection may become systemic.
The patient is also at risk for new allergic type symptoms. Again, these would not necessarily occur when the immune system is functioning normally.
Let your Prescribing Provider know if you have any of the following conditions:
- kidney problems or disease
- liver disease
- diabetes, pre-diabetes, or high blood glucose problems
- high cholesterol or triglyceride levels
- any infections
- history of hepatitis B
- skin cancer or family history of skin cancer
- Lapp lactase deficiency
- glucose-galactose malabsorption
- upcoming vaccinations
- scheduled or planned surgery
- receiving radiation therapy or scheduled for radiation in future
Before beginning Everolimus therapy, report a full list of drugs being taken for any condition. This list should include over-the-counter medications, supplements, herbal products, alcohol and recreational substances.
Do not take the following medications without the Provider’s express permission:
- aspirin or any product that contains aspirin
- immunizations or vaccines
There are over 455 medications that may interact with Everolimus. Some of these drugs may cause Everolimus to be less effective. Others may exacerbate side effects. Many of the medications that interfere with Everolimus are common familiar medicines. Do NOT use medications, including over-the-counter medications, supplements, or herbal products without first asking the healthcare team overseeing your case.
KNOWN ALLERGY TO MEDICATIONS CONTAINING SIROLIMUS OR TEMSIROLIMUS
Known hypersensitive reactions to these drugs and their ingredients strongly contraindicates receiving this treatment therapy.
KNOWN HYPERSENSITIVITY TO RAPAMYCIN DERIVATIVES
Any drug hypersensitivity to rapamycin, or to a medication with rapamycin as an ingredient, strongly contraindicates the use of Everolimus therapy.
When receiving ACE Inhibitor treatment, the risk of airway and tongue swelling can increase. With or without respiratory involvement, this is considered a high risk to patient survival.
Everolimus may decrease haemoglobin, lymphocytes, neutrophils, and platelet production. Wound healing is impaired by rapamycin, and therefore, the manufacturer advises against its use in acute bleeding conditions.
WOMEN OF CHILDBEARING AGE
Women of childbearing age must use a highly effective contraception during treatment and for 8 weeks after treatment ends.
HEPATIC IMPAIRMENT IN CHILDREN
This medication is NOT recommended for patients younger than 18 years of age who have known liver disease or history. For patients older than 18, Everolimus is only used when the benefits outweigh the risks. Dosing is determined based on the degree of liver impairment.