Everolimus Avansor: Uses, Dosage & Side Effects
An mTOR inhibitor used for prevention of organ transplant rejection and treatment of certain cancers, available as a 2.5 mg oral tablet
Everolimus Avansor (everolimus) is a prescription medication belonging to the class of mammalian target of rapamycin (mTOR) inhibitors. It is used in two major therapeutic areas: as an immunosuppressant for the prevention of organ rejection following kidney or heart transplantation (in combination with other immunosuppressive agents), and as an antineoplastic agent for the treatment of certain advanced cancers, including renal cell carcinoma, neuroendocrine tumors, hormone receptor-positive breast cancer, and tumors associated with tuberous sclerosis complex. Everolimus works by inhibiting the mTOR pathway, a critical regulator of cell growth, proliferation, and immune function. Available as a 2.5 mg tablet, it is taken orally once daily and requires regular blood monitoring to ensure safe and effective use.
Quick Facts: Everolimus Avansor
Key Takeaways
- Everolimus Avansor is an mTOR inhibitor used for two main purposes: preventing organ rejection after kidney or heart transplantation and treating certain advanced cancers including renal cell carcinoma, neuroendocrine tumors, and hormone receptor-positive breast cancer.
- The medication is taken orally once daily at the same time, consistently with or without food. Tablets must be swallowed whole and never crushed or chewed. In transplant settings, dosing is guided by therapeutic drug monitoring.
- Common side effects include mouth ulcers (stomatitis), infections, rash, fatigue, diarrhea, elevated blood lipids and glucose, and reduced blood cell counts. Regular blood tests are essential throughout treatment.
- Everolimus has significant drug interactions with CYP3A4 inhibitors and inducers. Strong inhibitors (e.g., ketoconazole) can dangerously increase blood levels, while strong inducers (e.g., rifampicin) can reduce effectiveness. Grapefruit must be avoided.
- Everolimus must not be used during pregnancy due to the risk of fetal harm. Effective contraception is required during treatment and for at least 8 weeks after the last dose for both women and men.
What Is Everolimus Avansor and What Is It Used For?
Everolimus Avansor contains everolimus, a derivative of rapamycin (sirolimus), which belongs to a class of medications known as mammalian target of rapamycin (mTOR) inhibitors. The mTOR pathway is one of the most critical intracellular signaling networks in human biology, serving as a central hub that integrates signals from growth factors, nutrients, energy status, and cellular stress to regulate fundamental processes including protein synthesis, cell growth, proliferation, metabolism, autophagy, and immune cell activation. By inhibiting this pathway, everolimus exerts both immunosuppressive and antitumor effects, making it valuable in two distinct therapeutic areas.
At the molecular level, everolimus works by binding to the intracellular protein FKBP-12 (FK506-binding protein 12). The resulting everolimus-FKBP-12 complex then binds to and inhibits mTOR complex 1 (mTORC1), a serine/threonine kinase that normally phosphorylates and activates two key downstream effectors: ribosomal protein S6 kinase 1 (S6K1) and eukaryotic initiation factor 4E-binding protein 1 (4E-BP1). S6K1 promotes ribosome biogenesis and protein translation, while the phosphorylation of 4E-BP1 releases eIF4E to initiate cap-dependent translation of mRNAs encoding proteins involved in cell cycle progression, angiogenesis, and glycolysis. By blocking these pathways, everolimus effectively reduces protein synthesis, inhibits cell cycle progression from G1 to S phase, decreases vascular endothelial growth factor (VEGF) expression, and suppresses the proliferation and activation of T lymphocytes and other immune cells.
In the field of organ transplantation, everolimus is used as part of a multi-drug immunosuppressive regimen to prevent rejection of transplanted kidneys and hearts. After an organ transplant, the recipient's immune system recognizes the donated organ as foreign and mounts an immune response to reject it. Everolimus suppresses this immune response by inhibiting the proliferation and activation of T cells, which are the primary mediators of transplant rejection. In transplant medicine, everolimus is typically used in combination with reduced-dose calcineurin inhibitors (such as ciclosporin or tacrolimus), corticosteroids, and sometimes mycophenolate mofetil. The use of everolimus allows for reduced doses of calcineurin inhibitors, which can help preserve long-term kidney function — a critical consideration since calcineurin inhibitor-related nephrotoxicity is a leading cause of chronic allograft dysfunction.
In oncology, everolimus has demonstrated efficacy in several types of cancer where the mTOR pathway plays a significant role in tumor growth and progression. The approved oncology indications for everolimus include:
- Advanced renal cell carcinoma (RCC): Everolimus is indicated for the treatment of advanced RCC after failure of treatment with VEGF-targeted therapy (such as sunitinib or sorafenib). The pivotal RECORD-1 trial demonstrated that everolimus significantly improved progression-free survival compared with placebo in this setting (4.9 months versus 1.9 months; HR 0.33, p < 0.001).
- Neuroendocrine tumors (NET): Everolimus is approved for the treatment of unresectable, locally advanced, or metastatic well-differentiated (Grade 1 or Grade 2) neuroendocrine tumors of pancreatic, gastrointestinal, or lung origin. The RADIANT-3, RADIANT-4, and related trials demonstrated significant improvements in progression-free survival.
- Advanced hormone receptor-positive (HR+), HER2-negative breast cancer: In combination with the aromatase inhibitor exemestane, everolimus is indicated for postmenopausal women with advanced HR+/HER2– breast cancer after failure of letrozole or anastrozole. The BOLERO-2 trial showed that the combination of everolimus and exemestane more than doubled progression-free survival compared with exemestane alone.
- Tuberous sclerosis complex (TSC)-associated tumors: Everolimus is approved for the treatment of renal angiomyolipoma and subependymal giant cell astrocytoma (SEGA) associated with TSC, a genetic disorder characterized by the growth of non-cancerous tumors in multiple organs. TSC results from mutations in the TSC1 or TSC2 genes, which normally function as negative regulators of mTORC1, making mTOR inhibition a rational targeted therapy for this condition.
Everolimus was first approved by the U.S. Food and Drug Administration (FDA) in 2009 for advanced renal cell carcinoma (as Afinitor), and approval for transplant rejection prevention (as Zortress/Certican) followed shortly thereafter. The European Medicines Agency (EMA) has also granted marketing authorization for everolimus under various brand names. Everolimus Avansor is a branded generic formulation of everolimus available as 2.5 mg tablets, providing the same active substance at the same quality standards as the originator products. The availability of multiple branded generics helps improve patient access to this important medication worldwide.
Everolimus is used at different doses depending on the indication. For transplant rejection prevention, typical starting doses are 0.75 mg twice daily (1.5 mg total daily), adjusted based on blood trough level monitoring. For oncology indications, the standard dose is 10 mg once daily. The 2.5 mg tablet strength allows flexible dosing for both transplant and oncology patients. Always follow your specialist's dosing instructions precisely.
What Should You Know Before Taking Everolimus Avansor?
Contraindications
The primary contraindication to using Everolimus Avansor is hypersensitivity (allergy) to everolimus, to other rapamycin derivatives (such as sirolimus or temsirolimus), or to any of the other ingredients (excipients) in the tablet formulation. Rapamycin derivatives share structural similarities, and cross-hypersensitivity has been reported. If you have had a previous allergic reaction to any medication in this class, inform your doctor before starting treatment.
Serious hypersensitivity reactions, including anaphylaxis, dyspnea (difficulty breathing), flushing, chest pain, and angioedema (swelling of airways), have been reported with everolimus use. If you experience signs of a severe allergic reaction, seek immediate medical attention. Treatment with everolimus must be discontinued permanently if a severe hypersensitivity reaction occurs.
Warnings and Precautions
Everolimus suppresses the immune system, which increases the risk of developing serious infections, including opportunistic infections (such as Pneumocystis jirovecii pneumonia, BK virus nephropathy, cytomegalovirus infection, aspergillosis, and candidiasis). Some infections can be life-threatening or fatal. Report any signs of infection (fever, cough, difficulty breathing, pain, unusual fatigue) to your doctor immediately. Prophylaxis against Pneumocystis jirovecii pneumonia may be recommended.
Before and during treatment with everolimus, your doctor will carefully monitor you for the following conditions:
- Non-infectious pneumonitis: Everolimus is associated with a class effect of non-infectious pneumonitis, which can present as cough, dyspnea, pleural effusion, or radiological changes on chest imaging. This occurs in up to 12–16% of patients in oncology trials and may require dose reduction, treatment interruption, or discontinuation. Patients should report new or worsening respiratory symptoms promptly.
- Infections: Both bacterial and viral infections, including reactivation of hepatitis B, have been reported. Screening for latent infections (including tuberculosis and hepatitis B/C) is recommended before starting therapy. Live vaccines must be avoided during treatment and for a period after discontinuation.
- Mouth ulcers (stomatitis): This is one of the most common side effects, occurring in up to 44–78% of patients depending on the indication. Maintaining good oral hygiene, using alcohol-free mouthwash, and avoiding irritating foods can help. Your doctor may prescribe topical corticosteroid mouthwash or adjust the dose if stomatitis is severe.
- Renal function: Everolimus can impair renal function, particularly when used in combination with calcineurin inhibitors in transplant patients. Regular monitoring of serum creatinine, estimated glomerular filtration rate (eGFR), and urinary protein excretion is essential. Proteinuria has been reported and may require dose adjustment.
- Metabolic disturbances: Everolimus commonly causes hyperglycemia (high blood sugar), hyperlipidemia (elevated cholesterol and triglycerides), and hypertriglyceridemia. Fasting glucose and lipid profiles should be monitored regularly. Pre-existing diabetes may worsen, and new-onset diabetes can occur. Lipid-lowering therapy and diabetes management may need to be initiated or adjusted.
- Hepatic impairment: Everolimus is extensively metabolized by the liver. Patients with mild hepatic impairment (Child-Pugh A) may require dose reduction in oncology settings. Patients with moderate hepatic impairment (Child-Pugh B) require significant dose reduction. Use in severe hepatic impairment (Child-Pugh C) is not recommended unless the benefit outweighs the risk.
- Wound healing: Everolimus impairs wound healing. If possible, treatment should be interrupted before elective surgery and should not be restarted until adequate wound healing has been confirmed.
Pregnancy and Breastfeeding
Everolimus must not be used during pregnancy. Animal studies have shown embryo-fetal toxicity, including increased resorptions, reduced fetal weights, and skeletal malformations at doses within the clinical exposure range. Women of childbearing potential must use highly effective contraception during treatment and for at least 8 weeks after the last dose. A pregnancy test should be performed before starting treatment. Men taking everolimus should also use effective contraception during treatment and for at least 8 weeks after the last dose, as everolimus may affect male fertility.
It is not known whether everolimus is excreted in human breast milk, although it is excreted in rat milk. Given its mechanism of action and the potential for serious adverse reactions in breastfed infants, breastfeeding must be discontinued during treatment with everolimus and for at least 2 weeks after the last dose.
Children and Adolescents
The use of everolimus in children depends on the specific indication. For tuberous sclerosis complex-associated subependymal giant cell astrocytoma (SEGA) and renal angiomyolipoma, everolimus may be used in children and adolescents based on clinical trial data in these populations. For transplant rejection prevention, everolimus is approved for use in kidney transplant recipients from 1 year of age in some jurisdictions. For oncology indications other than TSC, everolimus is generally not recommended in children under 18 years due to a lack of data on safety and efficacy. Dosing in pediatric patients is typically adjusted based on body surface area and therapeutic drug monitoring.
Driving and Operating Machinery
Everolimus may cause fatigue, dizziness, and visual disturbances in some patients. If you experience any of these effects, you should not drive or operate machinery until the symptoms resolve. Individual responses may vary, and patients should use caution when engaging in activities that require alertness, particularly during the initial period of treatment or after dose adjustments.
How Does Everolimus Avansor Interact with Other Drugs?
Drug interactions represent one of the most critical aspects of everolimus therapy, as this medication has a narrow therapeutic index (meaning the difference between an effective dose and a toxic dose is relatively small) and its blood levels are highly susceptible to modulation by other drugs. Understanding these interactions is essential for safe and effective use of everolimus, whether in the transplant or oncology setting.
Everolimus is extensively metabolized in the liver and intestinal wall by the cytochrome P450 enzyme CYP3A4, and to a lesser extent by CYP3A5. It is also a substrate of the P-glycoprotein (P-gp) efflux transporter in the gut wall and liver. Any medication, food, or herbal product that significantly inhibits or induces CYP3A4 or P-gp can alter everolimus blood concentrations, potentially leading to toxicity (if levels are too high) or treatment failure (if levels are too low). In transplant patients, where therapeutic drug monitoring is standard practice, dose adjustments can be made based on blood level measurements. In oncology patients, where fixed dosing is more common, the consequences of drug interactions can be even more pronounced.
Major Interactions — Avoid or Adjust Dose
| Interacting Drug | Effect on Everolimus | Clinical Recommendation |
|---|---|---|
| Ketoconazole | Increases everolimus AUC by ~15-fold and Cmax by ~4.1-fold | Avoid concomitant use. If unavoidable, significantly reduce everolimus dose and monitor blood levels. |
| Itraconazole, Voriconazole, Posaconazole | Significantly increases everolimus levels (strong CYP3A4 inhibitors) | Avoid concomitant use. If essential, reduce everolimus dose and monitor blood levels closely. |
| Clarithromycin, Telithromycin | Significantly increases everolimus levels (strong CYP3A4 inhibitors) | Avoid concomitant use. Consider alternative antibiotics (e.g., azithromycin has minimal CYP3A4 inhibition). |
| HIV protease inhibitors (ritonavir, nelfinavir) | Significantly increases everolimus levels (strong CYP3A4 inhibitors) | Avoid concomitant use. If required, reduce everolimus dose substantially and monitor levels. |
| Rifampicin | Decreases everolimus AUC by ~63% and Cmax by ~58% | Avoid concomitant use. If unavoidable, consider increasing everolimus dose and monitor blood levels. |
| Phenytoin, Carbamazepine, Phenobarbital | Decreases everolimus levels (strong CYP3A4 inducers) | Avoid concomitant use if possible. If essential, increase everolimus dose and monitor blood levels. |
| St. John's Wort (Hypericum perforatum) | Decreases everolimus levels (CYP3A4 inducer) | Must be avoided during everolimus treatment. |
| Grapefruit / Grapefruit juice | Increases everolimus levels (CYP3A4 inhibitor in gut) | Must be completely avoided during treatment. |
Moderate Interactions — Use with Caution
| Interacting Drug | Effect on Everolimus | Clinical Recommendation |
|---|---|---|
| Ciclosporin | Increases everolimus AUC by ~2–3-fold (CYP3A4 and P-gp inhibitor) | Used together in transplant regimens with careful therapeutic drug monitoring. Dose adjustment required. |
| Erythromycin | Increases everolimus levels (moderate CYP3A4 inhibitor) | Use with caution. Monitor everolimus levels and adjust dose if needed. |
| Fluconazole | May increase everolimus levels (moderate CYP3A4 inhibitor) | Use with caution. Monitor blood levels. |
| Diltiazem, Verapamil | May increase everolimus levels (moderate CYP3A4 inhibitors) | Use with caution. Monitor blood levels and adjust dose if needed. |
| Efavirenz, Nevirapine | May decrease everolimus levels (moderate CYP3A4 inducers) | Use with caution. Monitor blood levels and consider dose increase. |
| ACE inhibitors (e.g., enalapril, ramipril) | Increased risk of angioedema (pharmacodynamic interaction) | Use with caution. Monitor for signs of angioedema. |
In addition to the interactions listed above, patients should inform their healthcare provider about all medications they are taking, including over-the-counter drugs, herbal supplements, and dietary supplements. Some herbal products (such as St. John's Wort, Echinacea) and dietary supplements (such as high-dose vitamin E) may interact with everolimus. Patients should also be aware that live vaccines are contraindicated during everolimus treatment due to the risk of vaccine-related infection from the immunosuppressive effects of the drug.
Live and live-attenuated vaccines (such as MMR, varicella, BCG, rotavirus, and yellow fever vaccines) must be avoided during treatment with everolimus and for a period after discontinuation, as the immunosuppressive effect of everolimus may result in vaccine-related infection. Inactivated vaccines (such as influenza and COVID-19 vaccines) can be given, but the immune response may be reduced. Discuss your vaccination schedule with your doctor.
What Is the Correct Dosage of Everolimus Avansor?
The dosing of everolimus varies significantly depending on the therapeutic indication, the patient's age, weight, organ function, concomitant medications, and (in transplant patients) blood trough concentrations. It is essential that patients take everolimus exactly as prescribed by their specialist and do not adjust the dose without medical guidance. The 2.5 mg tablet strength of Everolimus Avansor allows for flexible dosing across indications.
Adults
Kidney Transplant Rejection Prevention
The recommended starting dose is 0.75 mg twice daily (1.5 mg total daily), taken at the same time each day in combination with reduced-dose ciclosporin and corticosteroids. The dose is subsequently adjusted based on therapeutic drug monitoring, with the target whole blood trough concentration (C0) of 3–8 ng/mL. Blood levels should be monitored at least every 4–5 days after a dose change until stable levels are achieved, and then regularly throughout treatment. The first blood level measurement should be obtained approximately 4–5 days after starting treatment or after any dose change.
Heart Transplant Rejection Prevention
The recommended starting dose is 0.75 mg twice daily (1.5 mg total daily), initiated as soon as clinically stable after transplantation, typically within 5 days. The dose is adjusted based on blood trough level monitoring, with target concentrations of 3–8 ng/mL. Everolimus is used in combination with reduced-dose ciclosporin and corticosteroids.
Oncology Indications (RCC, NET, Breast Cancer, TSC)
The recommended dose is 10 mg once daily (4 tablets of 2.5 mg), taken at the same time each day. Treatment continues until disease progression or unacceptable toxicity. Dose reductions to 5 mg once daily (2 tablets) or 2.5 mg once daily (1 tablet) may be necessary for the management of adverse reactions. If a dose reduction to less than 2.5 mg daily is required, treatment should be discontinued. For TSC-associated SEGA, dosing may be guided by therapeutic drug monitoring with a target trough of 5–15 ng/mL.
Children
For pediatric patients with TSC-associated SEGA or renal angiomyolipoma, the starting dose is calculated based on body surface area (BSA): approximately 4.5 mg/m² once daily. The dose is then adjusted based on therapeutic drug monitoring to achieve a target trough concentration of 5–15 ng/mL. For pediatric kidney transplant recipients (aged 1 year and older), the dose is typically 0.8 mg/m² twice daily, adjusted by blood level monitoring. Everolimus tablets should only be used in children who can swallow tablets whole. For children who cannot swallow tablets, dispersible tablet formulations may be available.
Elderly Patients
No specific dose adjustments are required based on age alone. However, elderly patients may be more susceptible to certain side effects (such as infections, stomatitis, and metabolic disturbances) and may require more careful monitoring. Renal and hepatic function should be assessed before starting treatment, as age-related decline in organ function may necessitate dose adjustments. In oncology settings, elderly patients should be monitored particularly closely for non-infectious pneumonitis and myelosuppression.
Missed Dose
If you miss a dose of Everolimus Avansor, take it as soon as you remember, provided it is within 6 hours of the scheduled time. If more than 6 hours have passed since the scheduled dose, skip the missed dose and take the next dose at the regular time. Do not take a double dose to make up for the missed one. If you regularly miss doses, discuss this with your healthcare provider, as inconsistent dosing can affect blood levels and reduce the effectiveness of treatment. For transplant patients, consistent dosing is especially critical to maintain adequate immunosuppression and prevent rejection.
Overdose
Experience with overdose of everolimus in humans is limited. In clinical trials, single doses of up to 70 mg have been administered with acceptable acute tolerability. In all cases of overdose, general supportive measures should be initiated. Everolimus is not significantly removed by dialysis due to its high protein binding (approximately 74%) and extensive distribution into red blood cells. If overdose is suspected, contact your doctor or local poison control center immediately. The patient should be monitored for adverse effects, and blood levels should be measured if available. There is no specific antidote for everolimus overdose.
Everolimus Avansor tablets should be taken orally once daily (or twice daily for transplant patients) at approximately the same time each day. The tablets should be swallowed whole with a glass of water and must not be chewed, crushed, or broken. The medication should be taken consistently either with or without food (but not switching between the two), as food affects absorption. Patients should avoid grapefruit and grapefruit juice throughout the course of treatment.
What Are the Side Effects of Everolimus Avansor?
Like all medicines, Everolimus Avansor can cause side effects, although not everybody gets them. As an immunosuppressive and antiproliferative agent, everolimus affects multiple organ systems, and the side effect profile reflects its broad mechanism of action. The frequency and severity of side effects can vary depending on the indication, dose, duration of treatment, and concomitant medications. In general, side effects are more common and often more severe at the higher doses used in oncology compared with the lower doses used in transplant medicine. It is important to report any new or worsening symptoms to your healthcare provider promptly, as many side effects can be managed with dose adjustment or supportive care if detected early.
The following side effect frequencies are based on pooled data from clinical trials and post-marketing surveillance:
Very Common
Affects more than 1 in 10 patients (>10%)
- Stomatitis (mouth ulcers/sores) — the most frequently reported side effect
- Infections (upper respiratory tract infections, urinary tract infections, pneumonia)
- Rash (various types including maculopapular, acneiform)
- Fatigue and asthenia (weakness)
- Diarrhea
- Nausea
- Decreased appetite
- Peripheral edema (swelling of hands, feet, ankles)
- Hypercholesterolemia (elevated cholesterol)
- Hypertriglyceridemia (elevated triglycerides)
- Hyperglycemia (elevated blood sugar)
- Anemia (low red blood cells)
- Thrombocytopenia (low platelets)
- Leukopenia/Neutropenia (low white blood cells)
- Elevated creatinine (reduced kidney function markers)
- Headache
- Cough
Common
Affects 1 to 10 in 100 patients (1–10%)
- Non-infectious pneumonitis (lung inflammation)
- Epistaxis (nosebleeds)
- Vomiting
- Abdominal pain
- Dysgeusia (altered taste)
- Dry skin, pruritus (itching), nail disorders
- Arthralgia (joint pain), myalgia (muscle pain)
- Insomnia
- Dizziness
- Hypertension (high blood pressure)
- Proteinuria (protein in urine)
- Elevated liver enzymes (ALT, AST)
- Hemorrhage (bleeding events)
- Weight loss
- Dry mouth
- Dyspnea (shortness of breath)
- Diabetes mellitus (new onset or worsening)
Uncommon
Affects 1 to 10 in 1,000 patients (0.1–1%)
- Pancytopenia (reduction of all blood cell types)
- Pure red cell aplasia
- Pulmonary embolism (blood clot in lungs)
- Deep vein thrombosis
- Hepatitis, liver failure
- Pericardial effusion (fluid around the heart)
- Erythema multiforme (skin reaction)
- Acute renal failure
- Wound healing impairment
- Male infertility (azoospermia, oligospermia)
Rare
Affects 1 to 10 in 10,000 patients (0.01–0.1%)
- Hypersensitivity reactions including anaphylaxis
- Angioedema (with or without concomitant ACE inhibitor use)
- Pulmonary alveolar proteinosis
- Posterior reversible encephalopathy syndrome (PRES)
- Lymphoma and other malignancies (related to immunosuppression)
Not Known
Frequency cannot be estimated from available data
- Hepatitis B reactivation
- BK virus-associated nephropathy (in transplant patients)
- Progressive multifocal leukoencephalopathy (PML)
If you experience any of the side effects listed above, especially those categorized as serious (non-infectious pneumonitis, severe infections, significant blood count changes, liver or kidney problems, or signs of allergic reactions), contact your healthcare provider immediately. Many side effects can be effectively managed if detected and addressed early. Do not stop taking everolimus without consulting your doctor, as sudden discontinuation in transplant patients can lead to organ rejection.
Contact your doctor or go to the emergency department immediately if you experience: severe difficulty breathing or persistent dry cough (possible pneumonitis), high fever or signs of severe infection, unusual bleeding or bruising, severe abdominal pain, yellowing of skin or eyes (jaundice), signs of severe allergic reaction (swelling of face, lips, tongue, or throat), or chest pain. These symptoms may indicate serious complications that require urgent medical evaluation.
How Should You Store Everolimus Avansor?
Proper storage of Everolimus Avansor is essential to maintain the quality, potency, and safety of the medication throughout its shelf life. Everolimus is sensitive to light and moisture, which is why it is packaged in aluminum blister packs that provide protection from these environmental factors.
- Temperature: Store at or below 25°C (77°F). Do not freeze. Brief excursions up to 30°C (86°F) are permitted but should be minimized. Do not store the medication in a bathroom or near a kitchen sink, as humidity and heat can degrade the tablets.
- Light and moisture protection: Keep the tablets in their original blister packaging until immediately before use. The blister pack is designed to protect the tablets from light and moisture. Do not transfer tablets to other containers such as pill organizers for extended periods.
- Keep out of reach of children: Due to the pharmacological potency of everolimus and its potential for serious adverse effects, it is critical that this medication is stored securely and kept out of the reach and sight of children.
- Expiry date: Do not use Everolimus Avansor after the expiry date (EXP) printed on the carton and blister. The expiry date refers to the last day of that month.
- Disposal: Do not dispose of medications via household waste or wastewater. Return any unused or expired tablets to your pharmacist for safe disposal, in accordance with local regulations. This helps protect the environment.
If you notice any visible changes to the tablets (such as discoloration, crumbling, or an unusual smell), do not take them and consult your pharmacist. Damaged or deteriorated tablets may have reduced potency or altered characteristics that could affect their safety and efficacy.
What Does Everolimus Avansor Contain?
Understanding the full composition of Everolimus Avansor is important for patients who have known allergies or intolerances to specific excipients. The formulation has been designed to ensure consistent release and absorption of the active substance.
- Active substance: Each tablet contains 2.5 mg of everolimus.
- Excipients (inactive ingredients): Butylated hydroxytoluene (BHT, E321), magnesium stearate, lactose monohydrate, hypromellose, crospovidone, and lactose anhydrous. The exact list of excipients may vary by manufacturer and formulation. Refer to the patient information leaflet supplied with your medication for the complete list.
Lactose content: Everolimus Avansor tablets contain lactose. Patients with rare hereditary conditions of galactose intolerance, total lactase deficiency, or glucose-galactose malabsorption should not take this medicine. Patients with common lactose intolerance typically tolerate the small amounts of lactose present in medications, but should discuss this with their pharmacist or doctor if concerned.
BHT content: The tablets contain butylated hydroxytoluene (BHT, E321) as an antioxidant. BHT can cause local skin reactions (such as contact dermatitis) or irritation to the eyes and mucous membranes in sensitive individuals. This is more relevant for topical formulations; the small amounts in oral tablets are generally well tolerated.
Appearance: Everolimus Avansor 2.5 mg tablets are typically small, round, flat tablets that are white to slightly yellowish in color. The exact appearance (including any markings or engravings) may vary by batch and should be verified against the description in your patient information leaflet.
Frequently Asked Questions About Everolimus Avansor
Everolimus Avansor (everolimus) 2.5 mg is an mTOR inhibitor used for two main purposes: (1) prevention of organ transplant rejection following kidney or heart transplantation, in combination with other immunosuppressants such as ciclosporin and corticosteroids, and (2) treatment of certain advanced cancers including renal cell carcinoma after failure of VEGF-targeted therapy, neuroendocrine tumors of pancreatic, gastrointestinal, or lung origin, hormone receptor-positive HER2-negative breast cancer (in combination with exemestane), and tuberous sclerosis complex-associated tumors (renal angiomyolipoma and SEGA).
Take Everolimus Avansor exactly as prescribed by your doctor. Swallow the tablets whole with a glass of water — do not chew, crush, or break them. Take the medication at the same time each day, consistently either with or without food. For transplant patients, the usual starting dose is 0.75 mg twice daily, adjusted by blood level monitoring. For cancer patients, the usual dose is 10 mg once daily. Never change your dose or stop taking the medication without consulting your specialist.
The most common side effects include stomatitis (mouth ulcers/sores), infections, rash, fatigue, diarrhea, nausea, decreased appetite, edema (swelling), elevated cholesterol and triglycerides, elevated blood glucose, anemia, and reduced blood cell counts. Mouth ulcers are particularly common and can be managed with good oral hygiene and alcohol-free mouthwash. Regular blood monitoring is essential throughout treatment to detect metabolic and hematological changes early.
No. Grapefruit and grapefruit juice must be completely avoided during treatment with Everolimus Avansor. Grapefruit contains compounds that inhibit the CYP3A4 enzyme, which is responsible for metabolizing everolimus. Consuming grapefruit or its juice can significantly increase everolimus blood levels, leading to a higher risk of serious side effects. Other citrus fruits such as oranges and lemons are safe to consume.
Yes. Regular blood monitoring is essential. In transplant patients, therapeutic drug monitoring of everolimus trough levels is required to keep levels within the target range (typically 3–8 ng/mL for kidney transplant). All patients require monitoring of complete blood count, liver function tests, kidney function, fasting blood glucose, and lipid profiles. The frequency of monitoring depends on the clinical situation but is typically more intensive at the start of treatment and after dose changes. Your doctor will schedule regular blood tests throughout your treatment.
No. Everolimus is contraindicated during pregnancy due to the risk of fetal harm. Animal studies have demonstrated embryo-fetal toxicity at clinically relevant doses. Women of childbearing potential must use highly effective contraception during treatment and for at least 8 weeks after the last dose. A pregnancy test should be performed before starting treatment. Men taking everolimus should also use effective contraception during and for 8 weeks after treatment, as the drug may affect male fertility. If pregnancy is suspected during treatment, contact your doctor immediately.
References
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- U.S. Food and Drug Administration (FDA). Afinitor (everolimus) — Prescribing Information. Revised 2024. Available at: www.fda.gov
- U.S. Food and Drug Administration (FDA). Zortress (everolimus) — Prescribing Information. Revised 2024. Available at: www.fda.gov
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- Franz DN, Belousova E, Sparagana S, et al. Efficacy and safety of everolimus for subependymal giant cell astrocytomas associated with tuberous sclerosis complex (EXIST-1). Lancet. 2013;381(9861):125-132. doi:10.1016/S0140-6736(12)61134-9
- Kidney Disease: Improving Global Outcomes (KDIGO) Transplant Work Group. KDIGO Clinical Practice Guideline for the Care of Kidney Transplant Recipients. Am J Transplant. 2024;24(Suppl 2):S1-S120.
- Powles T, Albiges L, Bex A, et al. ESMO Clinical Practice Guideline update on the use of immunotherapy in early stage and advanced renal cell carcinoma. Ann Oncol. 2024;35(12):1089-1103.
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Editorial Team
This article was written and medically reviewed by the iMedic Medical Editorial Team, comprising licensed specialist physicians with expertise in oncology, transplant medicine, clinical pharmacology, and internal medicine.
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iMedic Medical Writers — licensed physicians with clinical and research experience in pharmacology and therapeutics
Medical Review
iMedic Medical Review Board — independent specialists reviewing content according to EMA, FDA, KDIGO, and ESMO guidelines
Evidence Standards
All claims supported by Level 1A evidence from systematic reviews, randomized controlled trials, and international guidelines (GRADE framework)
Editorial Independence
No pharmaceutical company funding or influence. All content is independently produced and regularly updated.
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