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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Mammalian target of rapamycin (mTOR) kinase inhibitors
everolimus
L04AH02
Forms & Strengths
- Tablets: 0.25 mg, 0.5 mg, 0.75 mg, 1 mg
- Tablets (Afinitor): 2.5 mg, 5 mg, 7.5 mg, 10 mg
- Dispersible tablets for oral suspension: 2 mg, 3 mg, 5 mg
Adult Dosing
- Transplantation prophylaxis: 0.75 mg orally twice daily adjusted by trough concentrations
- Advanced renal cell carcinoma: 10 mg orally once daily
- Subependymal giant cell astrocytoma (SEGA): 4.5 mg/m² orally once daily adjusted by trough
- Neuroendocrine tumors of pancreatic, gastrointestinal, or lung origin: 10 mg orally once daily
Pediatric Dosing
- SEGA associated with Tuberous Sclerosis Complex (age ≥1 year): Initial 4.5 mg/m² orally once daily
- Tuberous Sclerosis Complex-associated partial-onset seizures (age ≥2 years): Initial 5 mg/m² orally once daily
Indications
- Prophylaxis of organ rejection in kidney and heart transplantation
- Treatment of advanced renal cell carcinoma
- SEGA associated with tuberous sclerosis complex
- Advanced hormone receptor-positive, HER2-negative breast cancer (with exemestane)
- Progressive neuroendocrine tumors of pancreatic, gastrointestinal, or lung origin
Mechanism of Action
- Inhibits mammalian target of rapamycin (mTOR), specifically mTOR complex 1 (mTORC1)
- Suppresses cytokine-driven T-cell proliferation and inhibits protein synthesis and cell growth in tumors
Contraindications
- Hypersensitivity to everolimus, other rapamycin derivatives, or excipients
- Severe hepatic impairment (for certain oncology indications)
Adverse Reactions
- Stomatitis and mucosal inflammation
- Infections (upper respiratory tract, urinary tract)
- Non-infectious pneumonitis
- Hyperglycemia, hypercholesterolemia, hypertriglyceridemia
- Peripheral edema, fatigue, diarrhea, nausea
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) significantly increase everolimus concentrations
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) significantly decrease everolimus concentrations
- P-glycoprotein (P-gp) inhibitors may increase everolimus exposure
- Increased risk of nephrotoxicity when used with cyclosporine
Curated Content: Needs Vetting Before Put to Clinical Use