everolimus at a glance
Medicine class
mTOR inhibitor with immunosuppressive and cell-growth-inhibiting effects
Selected licensed roles
Preventing rejection after adult kidney, heart or liver transplantation; treating selected TSC-associated seizures or subependymal giant cell astrocytoma
Food
Take consistently in relation to food and avoid grapefruit or grapefruit juice
Monitoring
Blood concentrations and laboratory safety tests are important because exposure and toxicity vary between people and with interacting medicines
What is everolimus used for?
Selected products are licensed for distinct specialist uses:
Certican tablets: preventing organ rejection in adults receiving a kidney or heart transplant, alongside ciclosporin and corticosteroids.
Certican tablets: preventing organ rejection in adults receiving a liver transplant, alongside tacrolimus and corticosteroids.
Votubia dispersible tablets: additional treatment for refractory partial-onset seizures associated with TSC in people aged 2 years and over.
Votubia dispersible tablets: treating TSC-associated subependymal giant cell astrocytoma requiring intervention when surgery is unsuitable.
How does everolimus work?
Everolimus binds FKBP-12 and inhibits mTOR complex 1, a pathway controlling cell growth, metabolism and proliferation. This limits activated T-cell expansion after transplantation and counteracts excessive mTOR signalling caused by TSC1 or TSC2 dysfunction. Its precise antiseizure mechanism in TSC is not fully established.
everolimus preparations and strengths
Dispersible tablet
Route: Oral
Strengths: 1 mg, 2 mg, 3 mg, 5 mg
Tablet
Route: Oral
Strengths: 2.5 mg, 5 mg, 10 mg
How to take everolimus
Follow the specialist team's instructions and use only the prescribed product and formulation.
Take consistently either with food or without food.
Swallow Certican tablets whole with water; do not crush them.
Prepare Votubia dispersible tablets as a suspension using water only. Do not swallow them whole, chew them or crush them.
Use a prepared Votubia suspension promptly and discard it if it has exceeded the product's preparation limit.
Do not switch or combine tablets and dispersible tablets without specialist direction.
Caregivers preparing a suspension should avoid skin contact and wash their hands before and afterwards.
Avoid grapefruit and grapefruit juice.
everolimus side effects
Common or expected effects
- Mouth ulcers or soreness
- Infections, fever, cough or upper-respiratory symptoms
- Diarrhoea, nausea, vomiting or constipation
- Rash, acne or itching
- Headache, tiredness or sleep disturbance
- Raised cholesterol, triglycerides or blood glucose
- Reduced blood-cell counts
- High blood pressure or swelling
- Impaired wound healing
Get urgent medical advice
- Severe or opportunistic infection, including pneumonia or sepsis
- Non-infectious pneumonitis, causing new or worsening cough, breathlessness or low oxygen
- Severe allergy or angioedema with facial, tongue or airway swelling
- Kidney failure or markedly reduced urine
- Thrombotic microangiopathy, which may cause fever, bruising, confusion, jaundice or reduced urine
- Rare progressive multifocal leukoencephalopathy in immunosuppressed transplant recipients
everolimus in pregnancy
Human evidence is limited. Product information generally advises avoiding everolimus unless a specialist judges that the expected benefit outweighs the potential fetal risk. Specialist-recommended use may sometimes be necessary. Discuss pregnancy planning or a positive test promptly, but do not stop treatment without speaking to the specialist team.
everolimus while breastfeeding
Breastfeeding is not recommended during treatment because transfer into human milk and risk to the infant are uncertain. Obtain specialist advice when planning infant feeding.
everolimus interactions
Interactions affecting CYP3A4 or P-glycoprotein are particularly important. Check prescription, non-prescription and herbal products with the specialist team.
Strong CYP3A4/P-glycoprotein inhibitors, including clarithromycin, azole antifungals and some HIV antivirals
Can substantially increase everolimus exposure and toxicity; combinations are generally avoided or require specialist management.
Moderate inhibitors, including erythromycin, fluconazole, verapamil, diltiazem and cannabidiol
Can increase everolimus concentrations, prompting closer adverse-effect and blood-level monitoring.
Common questions about everolimus
Answers are fully visible for fast scanning and source review.
Why is everolimus prescribed after an organ transplant?
It suppresses growth signals used by activated immune cells, helping other immunosuppressants prevent rejection of a transplanted kidney, heart or liver.
How does everolimus help tuberous sclerosis complex?
TSC can cause excessive mTOR signalling. Everolimus inhibits this pathway and can reduce SEGA growth and help control associated refractory partial-onset seizures.
Why are blood tests needed?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.