Everolimus

What is Everolimus?

Everolimus is a prescription medicine. It belongs to a drug class called mTOR inhibitors (mammalian target of rapamycin inhibitors). Depending on the product, it works as a targeted cancer therapy or as an immunosuppressant (a medicine that lowers the immune system’s activity). Everolimus was first sold under the brand names Afinitor and Afinitor Disperz (for cancer and related conditions) and Zortress (for transplant). Generic versions are available.

Everolimus products are not interchangeable. They have different approved uses and different dosing. Always take only the product your doctor prescribed.

Approved uses of Afinitor and Afinitor Disperz (United States): In adults, everolimus is approved for:

• Breast cancer: Hormone receptor-positive, HER2-negative advanced breast cancer in postmenopausal women, used with exemestane after treatment with letrozole or anastrozole has not worked
• Neuroendocrine tumors (NET): Progressive, well-differentiated neuroendocrine tumors of the pancreas, or non-functional tumors of the stomach, intestine, or lung, that are advanced or have spread
• Kidney cancer (RCC): Advanced renal cell carcinoma after treatment with sunitinib or sorafenib
• Renal angiomyolipoma: A noncancerous kidney tumor in people with tuberous sclerosis complex (TSC) who do not need immediate surgery

In adults and children with tuberous sclerosis complex (TSC), it is also approved for subependymal giant cell astrocytoma (SEGA) that cannot be cured by surgery, and, in the tablets for oral suspension, as add-on treatment of TSC-related partial-onset seizures.

Approved use of Zortress (United States): Prevention of organ rejection in adults who have received a kidney or liver transplant, used together with other medicines.

Formulations and strengths:

• Afinitor tablets: 2.5 mg, 5 mg, 7.5 mg, and 10 mg
• Afinitor Disperz (tablets for oral suspension): 2 mg, 3 mg, and 5 mg
• Zortress tablets: 0.25 mg, 0.5 mg, 0.75 mg, and 1 mg

Other uses should be discussed only with your doctor.

What is the Recommended Dosage of Everolimus?

Your dose is set by your doctor and should always follow their instructions and your pharmacy label. Everolimus is taken by mouth, usually once a day (Afinitor) or twice a day (Zortress), at about the same time each day. Take it the same way each time, either always with food or always without food.

Your care team may adjust the dose or schedule based on:

• The condition being treated: Dosing differs for cancer, TSC, and transplant.
• Body size (for children and TSC uses): Doses may be based on body surface area.
• Blood levels: For some uses, such as TSC and transplant, blood tests measure how much everolimus is in your body, and doses are adjusted to reach a target range.
• Liver function: People with liver impairment may need a lower dose.
• Tolerance: Treatment may be paused or the dose lowered if side effects occur.
• Other medicines: Some drugs change how much everolimus is in your body.

Swallow tablets whole with a glass of water. Do not chew or crush them. Afinitor Disperz is mixed with water only, in a small glass or oral syringe, and taken right away. Do not change, skip, or stop doses on your own.

How Everolimus Works

mTOR is a protein that helps cells grow, divide, and make new blood vessels. In some cancers and tumors, this signal is too active.

In cancer and TSC, everolimus blocks mTOR, which can slow tumor growth. In transplant, mTOR also helps immune cells multiply, so blocking it lowers the chance that the immune system attacks the new organ. Everolimus is used to manage these conditions and is not a cure for cancer. Regular scans, blood tests, and visits help your care team see how treatment is working.

Is a Prescription Required to Buy Everolimus Online?

Yes. Everolimus is prescription-only. It should be prescribed and monitored by a licensed medical specialist, such as a medical oncologist (for cancer), a neurologist, nephrologist, or TSC specialist (for TSC), or a transplant physician (for transplant).

• Buy only from a licensed pharmacy that requires a valid prescription.
• Counterfeit or substandard medicines exist. Be cautious of websites that sell without a prescription or ship from unclear sources.
• Check that the tablets match what your pharmacist describes, and ask your pharmacist if packaging or appearance looks different.

Side Effects of Everolimus

Not everyone gets every side effect. Many can be managed with help from your care team.

Common Side Effects

• Mouth sores or ulcers (stomatitis), often the most common
• Infections, such as colds, sinus, or urinary infections
• Rash or dry skin
• Tiredness or weakness
• Diarrhea, nausea, or decreased appetite
• Swelling in the hands, feet, or legs
• Cough
• Fever
• Headache
• Higher blood sugar and cholesterol or fat levels on blood tests
• Low red blood cell counts (anemia) or low white blood cell counts

Serious Side Effects

These are less common but need prompt attention:

• Lung problems (non-infectious pneumonitis): new or worsening cough, shortness of breath, or chest pain
• Serious infections: fever, chills, flu-like symptoms, or signs of a wound infection. Hepatitis B can become active again in people who carry the virus.
• Severe allergic reactions and swelling (angioedema): swelling of the face, lips, tongue, or throat, or trouble breathing. Risk may be higher if you also take an ACE inhibitor.
• Kidney problems: less urine, swelling, or changes in kidney blood tests
• High blood sugar or diabetes: increased thirst, frequent urination, or blurred vision
• Slow wound healing
• Low blood counts: easy bruising, bleeding, or ongoing infections
• Blood clots (especially with transplant use): leg swelling or pain, or sudden shortness of breath

Seek immediate medical care if you have trouble breathing, swelling of the face or throat, or signs of a serious infection. Contact your care team promptly for mouth sores that make eating hard, a new cough, a fever, or a wound that is not healing. Your team may recommend a special alcohol-free mouth rinse or other mouth care, so follow their instructions.

Drug Interactions

Tell your doctor and pharmacist about everything you take, including prescription drugs, over-the-counter (OTC) products, vitamins, supplements, and herbal products. Major categories include:

• Strong CYP3A4 and P-gp inhibitors (such as ketoconazole, itraconazole, clarithromycin, ritonavir) can raise everolimus levels and are generally avoided.
• Moderate CYP3A4 and P-gp inhibitors (such as erythromycin, verapamil, diltiazem, fluconazole) may raise levels, and your doctor may lower the dose or monitor you more closely.
• Strong CYP3A4 inducers (such as rifampin, carbamazepine, phenytoin) can lower everolimus levels and may make it less effective. These are generally avoided, or the dose may be increased.
• ACE inhibitors (blood pressure medicines such as lisinopril): These may raise the risk of swelling (angioedema).
• Other immune-lowering medicines: In transplant, everolimus is taken with other medicines such as cyclosporine or tacrolimus, and doses are carefully managed.
• Live vaccines: These should be avoided during treatment. Ask your care team about vaccines, and try to complete needed vaccinations before starting.
• Grapefruit and grapefruit juice can raise everolimus levels and should be avoided.
• Herbal products, especially St. John’s wort, can lower everolimus levels. Ask your pharmacist before using any herbal or dietary supplement.

Bring a complete, updated medication list to every appointment.

Safety & Important Considerations

• Infections: Everolimus can lower the body’s ability to fight infection. Report fever or symptoms early.
• Mouth care: Mouth sores are common. Keep your mouth clean, and ask your team about recommended rinses. Avoid products with alcohol or peroxide unless your team says they are safe.
• Lung symptoms: Report any new cough or breathing changes. Your team may order scans to check.
• Blood tests: Blood counts, kidney function, blood sugar, and cholesterol are checked before treatment and regularly during treatment. Everolimus blood levels are also checked for some uses.
• Liver disease: A lower dose may be used. Discuss any liver problems, including hepatitis B, with your specialist.
• Kidney disease: Kidney function is monitored, and urine protein may be checked.
• Wound healing: Tell any surgeon or dentist you take everolimus. Treatment may be paused around surgery.
• Radiation therapy: Everolimus may make side effects of radiation worse, including after radiation has ended.
• Pregnancy: Everolimus can harm an unborn baby. Women who could become pregnant should use effective contraception during treatment and for 8 weeks after the last dose, and male partners should use contraception during treatment and for 4 weeks after, according to U.S. labeling. Tell your doctor right away if you are or may become pregnant.
• Fertility: Everolimus may affect fertility in women and men. Talk with your specialist if this is a concern.
• Breastfeeding: Breastfeeding is not recommended during treatment and for 2 weeks after the last dose.
• Older adults and children: Older adults are monitored closely for infection and kidney function. Children may be treated for TSC-related conditions, with doses based on body size and blood levels.
• Transplant boxed warnings: Zortress carries warnings about a higher risk of cancer and serious infections, kidney graft blood clots, and kidney problems when used with standard doses of cyclosporine. Your transplant team will review these with you.
• Handling: Caregivers should avoid direct contact with crushed or broken tablets or with the suspension, and should wash their hands afterward. Pregnant caregivers should ask the care team about handling precautions.

Who This Medication Is For

Everolimus is intended for adults with certain advanced cancers (breast, neuroendocrine, and kidney), for adults and children with certain tumors or seizures related to tuberous sclerosis complex, and for adults who have received a kidney or liver transplant, as decided by their care team. Treatment plans differ from person to person.

Who Should Not Take Everolimus

Everolimus should not be used by people who have had a severe allergic reaction to everolimus, sirolimus, other rapamycin-related medicines, or any ingredient in the tablet.

Discuss with your doctor before starting if you:

• Have an active infection or a history of repeated infections
• Have hepatitis B or have been exposed to it
• Have lung disease or breathing problems
• Have liver disease or kidney disease
• Have diabetes, high cholesterol, or high triglycerides
• Have had a recent surgery or have planned surgery
• Are pregnant, planning pregnancy, or breastfeeding
• Take an ACE inhibitor or any medicine that interacts with everolimus
• Need a vaccine

What to Do If You Miss a Dose

• Afinitor and Afinitor Disperz: If you remember within about 6 hours of your usual time, you may take the missed dose. If more than 6 hours have passed, skip it and take your next dose at the usual time.
• Zortress and other uses: Because timing is important for transplant, contact your transplant team or pharmacist for specific instructions.
• Never take two doses at once to make up for a missed one.
• If you are unsure what to do, or you miss several doses, contact your care team or pharmacist.

Related medications to Everolimus

Other medicines are used for the same conditions, depending on the condition and your health:

• Breast cancer: other hormone therapies, CDK4/6 inhibitors, alpelisib, capivasertib, and chemotherapy
• Neuroendocrine tumors: somatostatin analogs, sunitinib (for pancreatic tumors), radioligand therapy, and chemotherapy
• Kidney cancer: axitinib, cabozantinib, sunitinib, pazopanib, lenvatinib (used with everolimus in some cases), and immunotherapy-based options
• Tuberous sclerosis complex: surgery, seizure medicines, and other TSC-directed care
• Transplant: tacrolimus, cyclosporine, mycophenolate, azathioprine, and other anti-rejection medicines

These medicines differ in side effects, interactions, and approved uses. Switching or combining treatments must be decided together with your doctor.

Storage Instructions

• Store at room temperature, about 68°F to 77°F (20°C to 25°C), with brief trips between 59°F and 86°F (15°C to 30°C) allowed.
• Keep tablets in the original blister pack until you are ready to take them, protected from light and moisture. Do not store in the bathroom.
• Keep out of reach of children and pets.
• Do not use tablets past the expiration date. Ask your pharmacist about safe disposal of unused medicine.
• Do not open the blister pack until the dose is needed, and wash your hands after handling.

Disclaimer

This page is for educational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Patients must consult a licensed medical oncologist, transplant physician, or other relevant medical specialist before starting, changing, or stopping treatment. Treatment decisions must be based on a full clinical evaluation by a qualified specialist.