Section 01 · Monograph
Everolimus
Reviewed Nov 2026FDA label
Afinitor DisperzmTOR inhibitor
- Forms
- Tab for susp: 2, 3, 5mg
- Dose
- TSC seizures: 5mg/m² once daily, titrate to trough 5-15ng/mL
- MOA
- Inhibits mTORC1 (TSC-related seizure pathway)
Indications
- Adjunctive treatment of tuberous sclerosis complex (TSC)-associated partial-onset seizures in patients 2 years and older (Afinitor Disperz)FDA-labeled
- TSC-associated subependymal giant cell astrocytomaFDA-labeled
- Several oncology indications (renal cell carcinoma, breast cancer, neuroendocrine tumors)FDA-labeled
Mechanism of Action
- mTOR (mTORC1) inhibitor via FKBP-12 binding; counteracts the hyperactive mTOR pathway that drives seizures and tumor growth in tuberous sclerosis
Full Dosing
Adult / usual
- TSC seizures: start 5mg/m² once daily (tablets for oral suspension); titrate to a trough concentration of 5-15ng/mL
- Check trough about 2 weeks after starting or changing dose
- Tablets for oral suspension: disperse in water and give immediately; take consistently with or without food
Hepatic
- Dose reduction in hepatic impairment
Contraindications
- Hypersensitivity to everolimus, sirolimus or other rapamycin derivatives
Drug Interactions
- Strong CYP3A4/P-gp inhibitors: avoid; inducers (carbamazepine, phenytoin) may lower levels
- Avoid live vaccines
- ACE inhibitors increase angioedema risk
Adverse Effects
- Stomatitis and mouth ulcers
- Infections
- Hyperlipidemia and hyperglycemia
- Non-infectious pneumonitis
- Myelosuppression, renal dysfunction
- Impaired wound healing
Monitoring Parameters
- Trough levels 5-15ng/mL
- CBC, renal function, glucose and lipids
- Respiratory symptoms
Pregnancy & Lactation
- Embryo-fetal toxicity; contraception during and for about 8 weeks after treatment
- Breastfeeding not recommended during and for about 2 weeks after the last dose