Is everolimus a chemotherapy?

No. It is a targeted mTOR inhibitor (a rapamycin analogue) that blocks a growth-signalling pathway rather than a cytotoxic chemotherapy, though it is used in oncology alongside other cancer treatments.

Why do doctors monitor for lung and mouth problems?

Non-infectious pneumonitis and stomatitis (mouth ulcers) are recognised class effects of mTOR inhibitors, so clinicians watch for new cough, breathlessness, or oral soreness and adjust dosing accordingly.

Does everolimus affect blood sugar and cholesterol?

Yes; hyperglycaemia and hyperlipidaemia are common, so fasting glucose and lipids are typically checked before and during treatment.

Can everolimus be used without a prescription?

No. It is a specialist-prescribed immunosuppressant and anticancer agent that requires medical supervision and, in transplant settings, blood-level monitoring; it is not a self-administered or research-use compound.

EMA-approved

Everolimus — Complete Research Guide (2026)

Last updated 2026-06-30

TL;DR

Everolimus is a peptide catalogued under Cyclic & Antimicrobial. Neutral reference entry; EU status: EU-approved prescription medicine.

What is Everolimus?

Everolimus is an orally administered mTOR inhibitor (a rapamycin analogue, or rapalog) marketed as Afinitor in oncology and as Zortress/Certican in transplant medicine.

It is FDA- and EMA-approved across several indications: advanced renal cell carcinoma, advanced pancreatic and GI/lung neuroendocrine tumours, HR-positive/HER2-negative advanced breast cancer, tuberous sclerosis complex (TSC)-associated SEGA, renal angiomyolipoma and refractory seizures, and rejection prophylaxis after kidney or liver transplant; it also coats everolimus-eluting coronary stents.

The evidence base is strong, resting on multiple randomised placebo-controlled phase 3 trials (RECORD-1, RADIANT-3/4, BOLERO-2, EXIST-1).

How does Everolimus work?

Everolimus binds the intracellular protein FKBP-12, and the resulting complex inhibits mTOR complex 1 (mTORC1), suppressing downstream signalling that drives cell growth, proliferation and angiogenesis.

In immune cells the same mTOR blockade curbs IL-2-driven T-lymphocyte proliferation, which underlies its use as an immunosuppressant.

What does the research say about Everolimus?

In advanced renal cell carcinoma progressing after VEGF-targeted therapy, everolimus roughly doubled progression-free survival versus placebo (RECORD-1). ^[1]
In advanced pancreatic neuroendocrine tumours, everolimus significantly prolonged progression-free survival versus placebo (RADIANT-3). ^[2]
Added to exemestane in HR-positive/HER2-negative advanced breast cancer, everolimus more than doubled progression-free survival (BOLERO-2). ^[4]

Clinical research & studies

The references below are the primary sources cited throughout this guide. Each links directly to PubMed or the regulator. Where evidence is preclinical (animal or in-vitro), that is stated rather than implied.

[1] Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial — Motzer RJ et al., Lancet 2008. (Randomised placebo-controlled phase 3 trial (RECORD-1))
[2] Everolimus for advanced pancreatic neuroendocrine tumors — Yao JC et al., The New England Journal of Medicine 2011. (Randomised placebo-controlled phase 3 trial (RADIANT-3))
[3] Everolimus for the treatment of advanced, non-functional neuroendocrine tumours of the lung or gastrointestinal tract (RADIANT-4): a randomised, placebo-controlled, phase 3 study — Yao JC et al., Lancet 2016. (Randomised placebo-controlled phase 3 trial (RADIANT-4))
[4] Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer — Baselga J et al., The New England Journal of Medicine 2012. (Randomised placebo-controlled phase 3 trial (BOLERO-2))
[5] Efficacy and safety of everolimus for subependymal giant cell astrocytomas associated with tuberous sclerosis complex (EXIST-1): a multicentre, randomised, placebo-controlled phase 3 trial — Franz DN et al., Lancet 2013. (Randomised placebo-controlled phase 3 trial (EXIST-1))
[6] Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis — Krueger DA et al., The New England Journal of Medicine 2010. (Open-label phase 1/2 trial)

Dosing context

This is not medical advice or a usage recommendation. Dosing figures are reported research context only, cited from the published literature.

Dosing is entirely context-dependent: oncology regimens differ from transplant regimens, and the formulations (Afinitor tablets, Afinitor Disperz, Zortress) are not interchangeable.

It is a prescription medicine titrated by specialists - with blood-level monitoring in transplant - and is not a self-administered or research-use compound.

Side effects & safety profile

As an mTOR-inhibitor immunosuppressant, everolimus raises the class risk of serious and opportunistic infections and of malignancy.

Common drug-specific toxicities include stomatitis/mouth ulcers, non-infectious pneumonitis, rash, fatigue, cytopenias, and metabolic disturbance (hyperglycaemia and hyperlipidaemia).

It also impairs wound healing, so it requires specialist prescribing and, in transplant, therapeutic drug-level monitoring.

Stacking & combinations

Everolimus is a prescription drug used within defined medical regimens (for example with exemestane, or with a reduced-dose calcineurin inhibitor after transplant), not a discretionary stack component.

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Frequently asked questions

It is approved for advanced renal cell carcinoma, pancreatic and lung/GI neuroendocrine tumours, HR-positive/HER2-negative advanced breast cancer, several tuberous sclerosis complex manifestations (SEGA, renal angiomyolipoma, refractory seizures), and transplant rejection prophylaxis; it also coats some coronary stents.

References

[1] Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial — Motzer RJ et al., Lancet 2008. PMID: 18653228. View sourceStudy: Randomised placebo-controlled phase 3 trial (RECORD-1)Everolimus roughly doubled progression-free survival versus placebo in metastatic RCC after VEGFR-TKI failure.
[2] Everolimus for advanced pancreatic neuroendocrine tumors — Yao JC et al., The New England Journal of Medicine 2011. PMID: 21306238. View sourceStudy: Randomised placebo-controlled phase 3 trial (RADIANT-3)Everolimus significantly prolonged progression-free survival versus placebo in advanced pancreatic NET.
[3] Everolimus for the treatment of advanced, non-functional neuroendocrine tumours of the lung or gastrointestinal tract (RADIANT-4): a randomised, placebo-controlled, phase 3 study — Yao JC et al., Lancet 2016. PMID: 26703889. View sourceStudy: Randomised placebo-controlled phase 3 trial (RADIANT-4)Everolimus improved progression-free survival in advanced non-functional lung/GI neuroendocrine tumours.
[4] Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer — Baselga J et al., The New England Journal of Medicine 2012. PMID: 22149876. View sourceStudy: Randomised placebo-controlled phase 3 trial (BOLERO-2)Adding everolimus to exemestane more than doubled progression-free survival in HR+/HER2- advanced breast cancer.
[5] Efficacy and safety of everolimus for subependymal giant cell astrocytomas associated with tuberous sclerosis complex (EXIST-1): a multicentre, randomised, placebo-controlled phase 3 trial — Franz DN et al., Lancet 2013. PMID: 23158522. View sourceStudy: Randomised placebo-controlled phase 3 trial (EXIST-1)Everolimus produced meaningful SEGA volume reduction versus placebo in tuberous sclerosis complex.
[6] Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis — Krueger DA et al., The New England Journal of Medicine 2010. PMID: 21047224. View sourceStudy: Open-label phase 1/2 trialEverolimus reduced subependymal giant-cell astrocytoma volume in patients with tuberous sclerosis complex.

This article is for educational and research purposes only. Peptides discussed here are not approved for human consumption by the FDA, EMA, or equivalent regulators outside of specific clinical contexts. Always consult a licensed medical professional before any therapeutic use.