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Pharmacology · mTOR inhibitors

Everolimus !

An oral mTOR inhibitor related to rapamycin, used for some breast, kidney and neuroendocrine cancers. Mouth sores, high sugar and pneumonitis are key risks.

Updated 2026-11-01

  • Class: mTOR inhibitors
  • Enzyme: mTOR (mechanistic target of rapamycin), through FKBP12
  • ATC code: L04AH02
  • WHO Model List of Essential Medicines

No human structure with everolimus is available. The figure shows rapamycin (sirolimus), from which everolimus is derived, bridging human FKBP12 and the FRB domain of mTOR in the same site.

Target in 3D: mTOR (mechanistic target of rapamycin), through FKBP12. PDB structure 1FAP (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Everolimus is a derivative of sirolimus. It binds FKBP12, and the complex inhibits mTORC1, the kinase complex that drives protein synthesis, cell growth and proliferation and helps tumour blood vessel growth. Cancer cell growth slows; in transplant recipients, T-cell proliferation is blocked.

  1. Binds FKBP12 inside the cell
  2. The complex inhibits mTORC1
  3. Protein synthesis and cell growth fall
  4. Tumour growth slows

Pharmacokinetics

Absorption
Taken by mouth
Metabolism
By CYP3A4; also a P-glycoprotein substrate
Half-life
About 30 hours

Indications

  • Advanced hormone receptor-positive, HER2-negative breast cancer in postmenopausal women, with exemestane, after letrozole or anastrozole Breast cancer →
  • Progressive neuroendocrine tumours of the pancreas, gut or lung
  • Advanced renal cell carcinoma after other targeted therapy
  • Renal angiomyolipoma and other tumours in tuberous sclerosis complex

Adverse effects

Common

  • Mouth sores (stomatitis)
  • Infections
  • Rash
  • Fatigue
  • Diarrhoea and oedema
  • High glucose, cholesterol and triglycerides

Contraindications

  • Hypersensitivity to everolimus or other rapamycin derivatives

Key interactions

P-glycoprotein and strong CYP3A4 inhibitors (ketoconazole, clarithromycin, ritonavir) and grapefruit
Large rise in everolimus levels; avoided.
Strong CYP3A4 inducers (rifampicin, carbamazepine, phenytoin)
Lower everolimus levels.
ACE inhibitors
Higher risk of angioedema.
Live vaccines
Avoided during treatment.

What is monitored

  • Glucose and lipids
  • Kidney function and urine protein
  • Blood counts
  • Respiratory symptoms
  • Mouth for stomatitis

Administration and safety

  • Oral tablets or tablets for oral suspension, at the same time each day, consistently with or without food; the two forms are not combined to make one dose.
  • Tablets are swallowed whole with water, not broken or crushed; gloves are worn when preparing the suspension.

Nursing care

  • Teach the use of an alcohol-free dexamethasone mouthwash from the start, as prescribed, to prevent mouth sores.
  • Ask about cough, breathlessness or chest pain.
  • Check glucose and lipids, especially in people with diabetes.
  • Treatment is paused around surgery because it delays wound healing.
  • Teach to avoid grapefruit and to report new medicines.

Pregnancy and breastfeeding

Can harm a fetus; effective contraception is used during treatment and for 8 weeks after the last dose.

Test yourself

Think of the answer, then tap the question to see it.

How is everolimus related to sirolimus?

It is a derivative of sirolimus (rapamycin) and works the same way: it binds FKBP12 and the complex inhibits mTOR.

Which simple measure reduces stomatitis with everolimus?

An alcohol-free dexamethasone mouthwash started with treatment.

A patient on everolimus develops a new dry cough and breathlessness. What should be suspected?

Non-infectious pneumonitis, a recognised serious effect of mTOR inhibitors; it needs prompt assessment.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Everolimus: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2018); DailyMed - EVEROLIMUS tablet EVEROLIMUS tablet, for suspension (DailyMed (U.S. National Library of Medicine), 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.