Everolimus
Generic Details
Generic Name
Everolimus
Other Names
- RAD001
Drug Class
- Kinase inhibitor
- Immunosuppressant
Chemical Formula
C53H83NO14
Molecular Weight
958.22 g/mol
Mechanism of Action
- Inhibits mTOR (mammalian target of rapamycin) pathway
Indications
- Breast cancer
- Pancreatic neuroendocrine tumors
- Renal cell carcinoma
- Subependymal giant cell astrocytoma
- Tuberous sclerosis complex
- Non-cancerous kidney tumors
Common Dosage Forms
- Tablet
- Oral solution
Typical Dosage
- 10 mg to 10 mg daily depending on the indication
Pediatric Dosage
- Dosage based on weight and indication, consult a pediatric oncologist
Geriatric Dosage
- Dosage adjustment may be needed, consult a healthcare provider
Side Effects
- Fatigue
- Stomatitis
- Rash
- Diarrhea
- Infections
- Nausea
- Decreased appetite
- Peripheral edema
Contraindications
- Hypersensitivity to everolimus or its components
Pregnancy Category
- Category D - Positive evidence of risk
Lactation Safety
- Use caution, excretion in human milk unknown
Drug Interactions
- Strong CYP3A4/P-gp inhibitors
- Strong CYP3A4 inducers
- Live vaccines
Overdose Symptoms
- Infections
- Mouth ulcers
- Gastrointestinal disorders
Antidote for Overdose
- No specific antidote, manage symptoms
Storage Conditions
- Store at room temperature (20-25°C)
Pharmacokinetics
- Absorption: Peak plasma concentration reached in 1-2 hours
- Distribution: Extensively bound to plasma proteins (approx. 74%)
- Metabolism: Metabolized in the liver via CYP3A4
- Excretion: Mainly feces (approx. 80%)
Precautions
- Monitor blood counts regularly
- Monitor renal function
- Monitor for signs of infection
Warnings
- Increased risk of infections
- Risk of interstitial lung disease and non-infectious pneumonitis
- Risk of renal failure