mTOR kinase inhibitor – immunosuppressant and antineoplastic
ATC code: L01EG02 (Everolimus)
Brand names
Afinitor, Certican, Votubia, Zortress
A sirolimus derivative. Binds cytosolic FKBP-12; the complex inhibits mTORC1 – a key regulator of cell growth, proliferation, angiogenesis, and metabolism. Suppresses proliferation of activated T- and B-cells (immunosuppression) and tumor cells in sensitive cancers (RCC, ER+ HER2-negative breast cancer, neuroendocrine tumors). CYP3A4- and P-gp metabolized – numerous drug interactions.
Second line
Combined with exemestane in metastatic ER+ HER2-negative breast cancer after non-steroidal aromatase inhibitor progression (, ) per ESMO 2024. Dose 10 mg daily. BOLERO-2 doubled progression-free survival (4.1 to 10.6 months).
Second line
Used with reduced-dose calcineurin inhibitors (tacrolimus, cyclosporine) for rejection prevention in kidney and heart transplant recipients per ESOT 2024. Particularly useful in chronic tacrolimus nephrotoxicity – allows tacrolimus dose reduction. Dose 0.75–1.5 mg twice daily.
Second line
Second-line for metastatic clear cell RCC after VEGF inhibitor progression (sunitinib, pazopanib) per ESMO 2024. Dose 10 mg once daily. RECORD-1 extended progression-free survival from 1.9 to 4.9 months.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Everolimus is an mTOR inhibitor. It is prescribed to prevent organ transplant rejection and for certain malignancies (renal cell carcinoma, pancreatic neuroendocrine tumors, HR+ HER2- metastatic breast cancer), and for tuberous sclerosis (AEMPS Ficha Técnica). In longevity communities, everolimus is actively promoted as an mTOR inhibitor for life extension, by analogy with rapamycin. The RESILIENT 2014 study in older adults showed transient improvement in vaccination response, but no randomized clinical trials with endpoints on lifespan extension in healthy adults exist. The drug has serious risks: immunosuppression with infections (including opportunistic), stomatitis (common), interstitial lung disease (life-threatening), hyperlipidemia, hyperglycemia, impaired wound healing, and thromboembolic events. If everolimus was recommended to a healthy person for longevity, seek a second opinion immediately.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Direct links to regulator labels. Open in a new tab.
Boxed warning
FDA boxed warning (transplant): increased mortality from infections and renal artery thrombosis when used in the early post-transplant period. Not used earlier than 30 days post-kidney and 70 days post-heart transplant.
Contraindicated. Reliable contraception is required in women of reproductive age and in partners of male patients during therapy and for 8 weeks after.
Contraindicated during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Everolimus is evaluated for the following indications with varying evidence strength: Organ transplant rejection prevention (evidence tier A), Renal cell carcinoma (evidence tier A), ER-positive breast cancer (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Everolimus (≥ 1 in 100): Stomatitis and oral ulcers, Rash and pruritus, Fatigue, Diarrhea, Nausea, Reduced appetite. See the Safety section for uncommon and serious reactions.
FDA category D. Contraindicated. Reliable contraception is required in women of reproductive age and in partners of male patients during therapy and for 8 weeks after.
Contraindicated during lactation.
Everolimus is contraindicated in: Hypersensitivity to everolimus, sirolimus, or rapamycin derivatives; Active severe infections; Pregnancy and lactation. Full list in the Safety section.
FDA boxed warning (transplant): increased mortality from infections and renal artery thrombosis when used in the early post-transplant period. Not used earlier than 30 days post-kidney and 70 days post-heart transplant.