mTOR Inhibitor Pregnancy: Everolimus is not recommended during pregnancy, or in women of childbearing potential not using contraception; there are no adequate data in pregnant women and animal studies have shown embryotoxicity and foetotoxicity. Women of childbearing potential must use a highly effective method of contraception while receiving everolimus and for up to 8 weeks after ending treatment. Women taking everolimus should not breast-feed during treatment and for 2 weeks after the last dose.

Everolimus (RCC)

Brand names: Afinitor

This is everolimus used for advanced renal cell carcinoma, typically after failure of vascular endothelial growth factor-targeted therapy. It is an oral mTOR inhibitor with both anticancer and immunosuppressant properties.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 10 mg

Route: Oral — administered once daily at the same time every day, consistently either with or without food; tablets should be swallowed whole with a glass of water and not chewed or crushed

Frequency: Once daily; treatment should continue as long as clinical benefit is observed or until unacceptable toxicity occurs

PRODUCT: the fetched UK SPC is Afinitor 10 mg tablets (oncology indications), available as 2.5 mg, 5 mg and 10 mg tablets. The US prescribing information in the same bundle states the same dosage specifically for renal cell carcinoma: 'The recommended dosage of everolimus tablets is 10 mg orally once daily until disease progression or unacceptable toxicity' (US label §2.4). DOSE REDUCTION: management of severe and/or intolerable suspected adverse reactions may require dose reduction and/or temporary interruption; if dose reduction is required the recommended dose is 5 mg daily and must not be lower than 5 mg daily. For Grade 1 adverse reactions dose adjustment is usually not required. Representative modifications: non-infectious pneumonitis Grade 2 — consider interruption until symptoms improve to Grade 1 or less then re-initiate at 5 mg daily, Grade 3 — interrupt then consider re-initiating at 5 mg daily, Grade 4 — discontinue; stomatitis Grade 2 — interrupt until recovery then re-initiate at the same dose (at 5 mg daily if it recurs), Grade 3 — interrupt then re-initiate at 5 mg daily, Grade 4 — discontinue; metabolic events Grade 3 — interrupt then re-initiate at 5 mg daily, Grade 4 — discontinue; thrombocytopenia Grade 3-4 (platelets below 50 x 10^9/L) — interrupt until recovery to 75 x 10^9/L or more then re-initiate at 5 mg daily; neutropenia Grade 4 (below 0.5 x 10^9/L) — interrupt until recovery to 1 x 10^9/L or more then re-initiate at 5 mg daily; febrile neutropenia Grade 3 — interrupt until recovery and no fever then re-initiate at 5 mg daily, Grade 4 — discontinue. MISSED DOSE: the patient should not take an additional dose but take the next prescribed dose as usual. HEPATIC IMPAIRMENT: mild (Child-Pugh A) — 7.5 mg daily; moderate (Child-Pugh B) — 5 mg daily; severe (Child-Pugh C) — only recommended if the desired benefit outweighs the risk, and a dose of 2.5 mg daily must not be exceeded. Dose adjustments should be made if a patient's Child-Pugh status changes during treatment. ELDERLY: no dose adjustment required for patients 65 years and over. PAEDIATRIC: the safety and efficacy of Afinitor in children aged 0 to 18 years have not been established and no data are available. SOURCE NOTE: eMC §4.4 and §4.8 are truncated at the source-fetch limit and no eMC §4.5 interactions section was retrieved; the tagged interaction entries below come from the US prescribing information in the same bundle.

Dose adjustments

Renal

No dose adjustment is required in renal impairment.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance, to other rapamycin derivatives, or to any of the excipients

Side effects

Stomatitis
Rash and pruritus
Fatigue and asthenia
Diarrhoea and nausea
Infections (including opportunistic infections) and non-infectious pneumonitis
Anaemia; metabolic effects — hyperglycaemia, hypercholesterolaemia, decreased appetite, weight decreased

Interactions

P-glycoprotein and strong CYP3A4 inhibitors — avoid concomitant use (US label §7.1)
P-glycoprotein and moderate CYP3A4 inhibitors — reduce the everolimus dose as recommended in the labelling (US label §7.1)
P-glycoprotein and strong CYP3A4 inducers — increase the everolimus dose as recommended in the labelling (US label §7.1)
ACE inhibitors — patients taking concomitant ACE inhibitors may be at increased risk of angioedema; avoid concomitant use (US label §5.4/§7.2)

Clinical monograph

How it works

It inhibits the mammalian target of rapamycin (mTOR) kinase, disrupting tumour-cell proliferation, metabolism, and angiogenesis.

Prescribing in practice

Non-infectious pneumonitis is a characteristic and potentially serious effect, so new or worsening respiratory symptoms must be investigated promptly and treatment interrupted if significant.
It causes immunosuppression with increased infection risk, plus stomatitis, hyperglycaemia, and hyperlipidaemia that require monitoring and management.
Exposure is markedly altered by CYP3A4 and P-glycoprotein inhibitors and inducers, so review interactions carefully against the SPC.

Monitoring

Monitor full blood count, renal and liver function, fasting glucose and lipids, and watch for pneumonitis and infection during treatment.

Counselling the patient

Report new cough, breathlessness, or fever without delay.
Mouth ulcers are common; maintain good oral hygiene and report severe soreness.
Avoid grapefruit and tell clinicians about all other medicines you take.

Evidence & guidelines

Licensed in advanced renal cell carcinoma on the basis of a randomised trial showing prolonged progression-free survival after VEGF-targeted therapy.

Reference: RECORD-1 trial (Motzer et al. NEJM 2008); SWISH trial (stomatitis); EXIST-2 trial (TSC-AML); MHRA SPC Afinitor; NICE TA432; EAU RCC Guidelines 2024; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

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