• Everolimus is taken long-term.
• It should be taken every day as long as it is working unless unacceptable side effects occur.
• In clinical trials, the average duration of treatment was approximately 24.0 weeks (range one week to almost 200 weeks).

Everolimus is an oral medication that, depending on the brand, may be used to treat certain types of cancer or to suppress the immune system.

Everolimus is usually taken every day for as long as it is working or until unacceptable side effects occur. It is meant to be taken as a long-term treatment.

In clinical trials, the average duration of treatment was approximately 24.0 weeks (range one week to almost 200 weeks).

Before you start everolimus, your doctor will run some blood tests, which will be repeated periodically while you are taking everolimus. These check the levels of certain blood cells and other substances in the blood and also check how well your liver and kidneys are working.

Everolimus may be taken either with or without food. It should be taken at approximately the same time each day. If you miss a dose of everolimus, and less than six hours have passed from the time you usually take it, then take it. If more than 6 hours have passed, skip that dose and take everolimus, as usual, the next day.

What is everolimus approved to treat?

Everolimus is approved to treat:

• Advanced breast cancer in postmenopausal women who have taken letrozole or anastrozole but the cancer has returned. Usually given in combination with exemestane (Afinitor only)
• Certain advanced neuroendocrine tumors of pancreatic, gastrointestinal or lung origin (Afinitor only)
• Advanced renal cell carcinoma (RCC) that has not responded to sunitinib or sorafenib (Afinitor only)
• Tuberous sclerosis complex (TSC)-associated partial-onset seizures in adults and children aged two or older (Afinitor Disperz only). TSC is a genetic disorder
• TSC-associated renal angiomyolipoma that does not require immediate surgery (Afinitor only)
• Subependymal giant cell astrocytoma (SEGA) associated with TSC in adults and children aged one year and older that requires treatment but which can’t be removed surgically
• Organ rejection after a kidney or liver transplant (Zortress only).

Everolimus may also be used off-label for other types of cancer, such as carcinoid tumors or Hodgkin lymphoma, lung or heart transplantation, or Waldenström macroglobulinemia.

Everolimus may be referred to as a chemotherapy medicine (cancer medication), a targeted treatment, or an immunosuppressant agent.

How does everolimus work?

Everolimus works by slowing or stopping the growth of cancer or tumor cells, or other growths. It belongs to the class of medicines called mechanistic target of rapamycin (mTOR) inhibitors. It may also be called a macrolide immunosuppressant because its structure includes a macrolide ring.

mTOR is a type of enzyme called a kinase that assists with the transfer of a phosphate group from ATP (adenosine triphosphate), the energy-carrying molecule found in the cells of all living things to other molecules. mTOR plays a vital role in regulating cell growth and proliferation.

This means that mTOR is a good target for conditions, such as cancer, that are characterized by extensive cell proliferation. mTOR inhibitors, such as everolimus, inhibit mTOR which is more active in certain cancers. This reduces cell proliferation, reducing the growth of cancer cells or other overly prolific cells and also prevents tumors from growing their own blood vessels.

mTOR inhibitors are also effective at reducing the volume of lipomas – these are lumps under the skin that occur due to an overgrowth of fat cells. Angiomyolipomas (AML) occur in people with TSC and are lipomas that occur within the kidneys. Everolimus can treat these.

When used for organ transplants, the Zortress brand of everolimus reduces the activity of the body’s immune system to stop the immune system from fighting the transplanted organ. This is because our immune system can reject a transplanted organ such as a liver or a kidney as it perceives the new organ as an invader. Zortress is used together with cyclosporine, steroids, and other medications.

The benefits of mTOR inhibitors are enhanced when they are combined with other chemotherapy agents.