Afinitor (everolimus): What It Is and What to Expect

This page is for people who have been prescribed everolimus (Afinitor), and their families. It covers what the drug is approved for, the side effects that most often change the dose, interactions, and when to get help.

Afinitor is the brand name. Everolimus is the generic name. It blocks mTOR, a switch inside the cell that decides whether to grow, divide and build blood vessels. Turn the switch down and growth slows.

The approved uses are unusually mixed.

• Advanced breast cancer that is hormone receptor positive and HER2 negative, after menopause, given with exemestane, once letrozole or anastrozole has stopped working.
• Neuroendocrine tumors of the pancreas that are progressing and cannot be removed or have spread. Also progressing, well-differentiated, non-functional neuroendocrine tumors of the gut or lung that cannot be removed or have spread. The label states it is not for functional carcinoid tumors.
• Advanced kidney cancer, after sunitinib or sorafenib have been tried.
• Kidney angiomyolipoma in tuberous sclerosis complex, where surgery is not needed straight away.
• A brain tumor called SEGA in tuberous sclerosis complex, from age 1, when it needs treating but cannot be fully removed.
• Seizures in tuberous sclerosis complex, from age 2, as an add-on. That use is for Afinitor Disperz, a version that dissolves in water.

For breast cancer, neuroendocrine tumors and kidney cancer, the dose printed on the label is 10 mg once a day. Your own team writes your prescription, and they lower it when mouth ulcers, lung inflammation or other medicines make that sensible.

Stomatitis, meaning mouth ulcers and sore inflamed lining, occurred in 44% to 78% of people across the trials in the label. It was severe in 4% to 9%. It usually starts within the first 8 weeks.

Ask your team on day one about mouthwash. The label says starting an alcohol-free steroid (dexamethasone) mouthwash with the first dose lowers how often mouth sores happen and how bad they get. Products with alcohol, hydrogen peroxide, iodine or thyme can make sores worse. Tell the team as soon as eating or drinking gets difficult, because a short pause or a lower dose often fixes it.

Everolimus dampens the immune system, so infections happen more easily. They include pneumonia, fungal infections, tuberculosis-type (mycobacterial) infections, and hepatitis B flaring up again in people who had it before. Some have been fatal. Fever, chills or a productive cough need assessing rather than waiting out.

Non-infectious pneumonitis is a separate problem: inflammation in the lungs caused by the drug itself, not by a germ. A scan can show changes with few or no symptoms, and the label says that alone does not always need a dose change. New breathlessness or a new or worse cough should be reported promptly, not put down to being tired.

Avoid live vaccines during treatment, and avoid close contact with people who have just had one. The response to other vaccines may be weaker.

Everolimus raises blood sugar, cholesterol and triglycerides in many people. Kidney function and blood counts can also shift. Expect blood tests before starting and at intervals afterward. If you have diabetes, monitoring is likely to be tightened.

Grapefruit and grapefruit juice raise everolimus levels and are best avoided completely. Several antibiotics, antifungals and heart drugs also raise it. Others lower the level and make it less effective. St. John's wort is a common example of the second kind. Show a full list to your pharmacist.

Two more things worth flagging. Wound healing can be slower, so tell surgeons and dentists before any procedure. The label says to stop the drug at least 1 week before planned surgery, and your team tells you when to restart. And taken with an ACE inhibitor for blood pressure, the risk of angioedema, a sudden swelling of the face, lips or tongue, rises. In pooled trials it was 6.8% with everolimus against 1.3% without it. That swelling is an emergency.

• Call 911 or go to an emergency department if your face, lips or tongue swell up, or your voice changes and breathing tightens. This risk is higher if you also take an ACE inhibitor. Do not drive yourself.
• Get medical care right away — do not wait for the next clinic slot — if your temperature reaches 100.4°F (38°C) or higher, or you get shaking chills. Everolimus damps the immune system, and the CDC treats a fever during cancer treatment as an emergency, because infection can turn serious in hours. Ring your team's urgent number on the way, or go straight to an emergency department.
• Call your care team right away if you have a new or worse cough, with or without phlegm, chest pain, wheezing, or you are newly short of breath. The patient leaflet says to tell your provider right away.
• Call your care team the same day if mouth ulcers stop you eating or drinking properly, or you are suddenly very thirsty, passing lots of urine and losing weight.

https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2150f73a-179b-4afc-b8ce-67c85cc72f04

https://www.cancer.gov/about-cancer/treatment/drugs/everolimus

https://www.cdc.gov/cancer-preventing-infections/patients/fever.html