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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Mammalian target of rapamycin (mTOR) kinase inhibitors
everolimus
L01EG02
Forms & Strengths
- 2.5mg, 5mg, 7.5mg, and 10mg tablets
- 0.25mg, 0.5mg, and 0.75mg tablets for pediatric patients
- 2mg/mL oral solution
Adult Dosing
- Advanced renal cell carcinoma: 10mg once daily
- Advanced pancreatic neuroendocrine tumors: 10mg once daily
- Breast cancer: 10mg once daily in combination with exemestane
- SEGA: 4.5mg/m^2 once daily, rounded to the nearest 0.5mg or 2.5mg strength
Pediatric Dosing
- SEGA: 4.5mg/m^2 once daily, rounded to the nearest 0.5mg or 2.5mg strength
- Tuberous sclerosis complex: 4.5mg/m^2 once daily for patients with SEGA, rounded to the nearest 0.5mg or 2.5mg strength
- Renal impairment: reduce dose by 1/3 to 1/2
Indications
- Treatment of advanced renal cell carcinoma
- Treatment of advanced pancreatic neuroendocrine tumors
- Treatment of hormone receptor-positive, HER2-negative advanced breast cancer
- Treatment of subependymal giant cell astrocytoma (SEGA) in patients with tuberous sclerosis complex
Mechanism of Action
- Inhibits mammalian target of rapamycin (mTOR)
- Blocks proliferation of tumor cells and formation of new blood vessels
- Inhibits angiogenesis by reducing expression of vascular endothelial growth factor
Contraindications
- Hypersensitivity to everolimus, other rapamycin derivatives, or to any component of the formulation
- Pregnancy and lactation
Adverse Reactions
- Non-infectious pneumonitis
- Infections
- Angioedema
- Stomatitis
- Renal failure
- Hyperlipidemia
- Hyperglycemia
Drug Interactions
- Strong CYP3A4 inhibitors: increase everolimus levels, reduce dose
- Strong CYP3A4 inducers: decrease everolimus levels, increase dose
- Cyclosporine: increases everolimus levels, monitor and adjust dose
Curated Content: Needs Vetting Before Put to Clinical Use