What is Everolimus: Uses, Dosage, Side Effects and More

Everolimus is a prescription medication that helps slow down certain types of cancer cell growth and prevents organ rejection after transplants. This powerful immunosuppressive drug works by blocking specific proteins in your body that control cell division and immune responses.

You might be prescribed everolimus if you have kidney cancer, breast cancer, certain brain tumors, or if you've received a kidney transplant. Your doctor will carefully monitor you while taking this medication to ensure it's working effectively and safely for your specific condition.

What is Everolimus?

Everolimus belongs to a class of medications called mTOR inhibitors. It's a targeted therapy that interferes with a protein pathway called mTOR, which controls how cells grow, multiply, and survive.

This medication comes in tablet form and is taken by mouth daily. The drug was originally developed to prevent organ rejection in transplant patients, but researchers discovered it also has powerful anti-cancer properties. Today, doctors use everolimus to treat several different conditions where controlling cell growth is important.

Think of everolimus as a cellular traffic controller. It slows down the signals that tell cells to grow and divide rapidly, which can help stop cancer cells from spreading or prevent your immune system from attacking a transplanted organ.

What is Everolimus Used For?

Everolimus treats several serious medical conditions by controlling how your cells grow and how your immune system responds. Your doctor prescribes it when you need to slow down specific cellular processes in your body.

Here are the main conditions everolimus helps treat, each requiring careful medical supervision:

• Advanced kidney cancer (renal cell carcinoma) - when the cancer has spread or returned after other treatments
• Hormone receptor-positive breast cancer - specifically when used with exemestane in postmenopausal women
• Kidney transplant rejection prevention - helps your body accept the new organ
• Liver transplant rejection prevention - works alongside other immunosuppressive drugs
• Subependymal giant cell astrocytoma (SEGA) - a type of brain tumor associated with tuberous sclerosis complex
• Pancreatic neuroendocrine tumors - when they cannot be surgically removed
• Tuberous sclerosis complex (TSC) - helps manage kidney problems called angiomyolipomas

Each of these conditions requires different dosing and monitoring approaches. Your healthcare team will tailor your treatment plan based on your specific diagnosis and overall health status.

How Does Everolimus Work?

Everolimus works by blocking a protein pathway called mTOR, which stands for "mechanistic target of rapamycin." This pathway controls how cells grow, divide, and use energy throughout your body.

When everolimus blocks mTOR, it essentially puts the brakes on rapid cell growth. In cancer treatment, this means tumor cells can't multiply as quickly or spread as easily. For transplant patients, it means your immune system becomes less likely to attack and reject the new organ.

This medication is considered a strong, targeted therapy rather than a general chemotherapy drug. It specifically targets the mTOR pathway without affecting as many other body systems. However, because it does suppress your immune system, you'll need regular monitoring to prevent infections and other complications.

The drug typically takes several weeks to reach its full effectiveness in your system. Your doctor will likely check your blood levels regularly during the first few months to ensure you're getting the right amount.

How Should I Take Everolimus?

Take everolimus exactly as your doctor prescribes, usually once daily at the same time each day. Consistency in timing helps maintain steady levels of the medication in your bloodstream.

You should take everolimus on an empty stomach, either one hour before eating or two hours after eating. This helps your body absorb the medication properly. Swallow the tablets whole with a full glass of water - don't crush, chew, or break them.

If you're taking the tablets for suspension (used for certain conditions), follow your pharmacist's instructions carefully for mixing. The suspension should be prepared fresh each time and used immediately after mixing.

Here are important guidelines to follow while taking everolimus:

• Take it at the same time every day to maintain consistent blood levels
• Don't eat grapefruit or drink grapefruit juice, as this can increase side effects
• Avoid live vaccines while taking this medication
• Store tablets at room temperature away from moisture and heat
• Keep tablets in their original container until ready to take
• Don't share your medication with others

If you have trouble swallowing tablets, talk to your doctor about alternative formulations. Never change how you take everolimus without medical guidance, as this can affect how well it works.

How Long Should I Take Everolimus For?

The length of everolimus treatment depends entirely on your specific condition and how well you respond to the medication. Some people take it for months, while others may need it for years or even long-term.

For cancer treatment, you'll typically continue taking everolimus as long as it's helping control your disease and you're not experiencing severe side effects. Your doctor will monitor your progress through regular scans and blood tests to determine if the medication is still beneficial.

Transplant patients often take everolimus for life to prevent organ rejection. Your healthcare team will adjust your dose over time based on your blood levels and overall health, but stopping the medication could put your transplanted organ at risk.

Your doctor will regularly evaluate whether you should continue treatment by considering factors like how well the medication is working, what side effects you're experiencing, and your overall quality of life. Never stop taking everolimus suddenly without medical supervision, as this could be dangerous depending on your condition.

What Are the Side Effects of Everolimus?

Like all powerful medications, everolimus can cause side effects ranging from mild to serious. Most people experience some side effects, but many are manageable with proper care and monitoring.

Understanding what to expect can help you recognize when to contact your healthcare team and when symptoms are part of the normal adjustment process:

Common Side Effects

These side effects occur in many people taking everolimus and are usually manageable:

• Mouth sores or ulcers - often the most bothersome side effect
• Fatigue and weakness - may improve as your body adjusts
• Diarrhea - usually mild to moderate
• Nausea and decreased appetite - eating smaller, frequent meals can help
• Skin rash or acne-like eruptions - typically on face and upper body
• Cough - usually dry and persistent
• Swelling in hands, feet, or legs - due to fluid retention
• Headache - often mild and manageable

Serious Side Effects

These side effects require immediate medical attention and may need treatment adjustments:

• Severe lung problems - including pneumonia or inflammation of lung tissue
• Serious infections - your immune system is suppressed, making you more vulnerable
• Kidney problems - especially important for transplant patients
• Severe mouth ulcers - that interfere with eating or drinking
• High blood sugar or diabetes - requires monitoring and possible medication changes
• High cholesterol levels - may need dietary changes or additional medications
• Severe skin reactions - including widespread rash or blistering

Rare but Serious Side Effects

These complications are uncommon but require emergency medical care:

• Severe allergic reactions - difficulty breathing, swelling of face or throat
• Heart problems - irregular heartbeat or chest pain
• Severe liver damage - yellowing of skin or eyes, dark urine
• Blood clots - sudden leg pain, chest pain, or shortness of breath
• Severe bleeding - unusual bruising or bleeding that won't stop
• Brain swelling - severe headache, confusion, or vision changes

Your healthcare team will monitor you closely for these side effects through regular blood tests and check-ups. Many side effects can be prevented or minimized with proper precautions and early intervention.

Who Should Not Take Everolimus?

Everolimus isn't safe for everyone, and certain medical conditions or circumstances make it inappropriate or dangerous. Your doctor will carefully review your medical history before prescribing this medication.

You should not take everolimus if you have a known allergy to the medication or its ingredients. Signs of allergic reactions include hives, difficulty breathing, or swelling of your face, lips, tongue, or throat.

Several health conditions require special caution or may prevent you from taking everolimus safely:

• Active infections - your immune system needs to be strong enough to fight current infections
• Severe liver disease - your liver processes this medication, so impaired function is dangerous
• Severe kidney disease - may worsen kidney function further
• Recent surgery - everolimus can interfere with wound healing
• Lung disease - including asthma or chronic obstructive pulmonary disease
• Pregnancy or breastfeeding - can harm developing babies
• Recent live vaccines - your suppressed immune system can't handle live vaccines safely

Certain medications can interact dangerously with everolimus, especially antifungal drugs, antibiotics, and other immunosuppressants. Always tell your doctor about all medications, supplements, and herbal products you're taking.

Your doctor will also consider your age, overall health status, and ability to follow the monitoring requirements before prescribing everolimus.

Everolimus Brand Names

Everolimus is available under several brand names, each formulated for specific medical conditions. The most common brand names include Afinitor, Afinitor Disperz, and Zortress.

Afinitor is the most widely prescribed brand, available in regular tablets for cancer treatment and certain genetic conditions. Afinitor Disperz comes as tablets that dissolve in water, making it easier for people who have trouble swallowing pills or need feeding tubes.

Zortress is specifically formulated for transplant patients and comes in different strengths than the cancer treatment versions. The dosing and monitoring requirements may differ between brands, so it's important to stick with the specific brand your doctor prescribes.

Generic versions of everolimus are also available and contain the same active ingredient. However, your doctor may prefer you stay with a specific brand to ensure consistent blood levels and effectiveness.

Everolimus Alternatives

Several alternative medications are available if everolimus isn't suitable for your condition or if you experience significant side effects. The best alternative depends on your specific medical situation.

For cancer treatment, alternatives might include other targeted therapies like sunitinib (Sutent), pazopanib (Votrient), or axitinib (Inlyta) for kidney cancer. Breast cancer patients might consider other hormone therapy combinations or CDK4/6 inhibitors.

Transplant patients have several immunosuppressive alternatives, including tacrolimus (Prograf), mycophenolate (CellCept), or sirolimus (Rapamune). Each has different side effect profiles and monitoring requirements.

The choice of alternative depends on factors like your previous treatment history, current health status, other medications you're taking, and personal preferences regarding side effects and monitoring schedules.

Is Everolimus Better Than Sirolimus?

Everolimus and sirolimus are closely related medications that work through similar pathways, but they have important differences that make one more suitable than the other in certain situations.

Everolimus is newer and has been more extensively studied in cancer treatment. It's often preferred for cancer patients because it has more FDA-approved cancer indications and more predictable blood levels.

Sirolimus has been used longer in transplant medicine and may be preferred for certain transplant patients due to its longer track record and different side effect profile. Some people tolerate one better than the other.

The choice between these medications depends on your specific condition, previous treatments, other health problems, and individual response patterns. Your doctor will consider all these factors when deciding which medication offers the best balance of effectiveness and manageable side effects for your situation.