Everolimus
AFINITOR
What it ismTOR inhibitor; transplant, renal and breast cancer, and tuberous sclerosis.
Why this oneIt is both an immunosuppressant and an antiproliferative, and it treats the tumors of tuberous sclerosis.
What limits itStomatitis is common and often dose-limiting. Non-infectious pneumonitis; hyperglycemia and hyperlipidemia.
FDA-approved for
- cancer/transplant (2009)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Renal cell carcinoma (RCC) | adult | 10 mg QD | 10 mg QD until progression/toxicity | 10 mg QD |
| TSC-associated renal angiomyolipoma | adult | 10 mg QD | 10 mg QD until progression/toxicity | 10 mg QD |
Renal Undefined (monitor renal function before and periodically)
Hepatic Mild (Child-Pugh A) 7.5 mg QD (reduce to 5 mg if not tolerated); Moderate (B) 5 mg QD (reduce to 2.5 mg); Severe (C) 2.5 mg QD if benefit outweighs risk
Instructions
- Swallow tablets whole; take consistently with or without food
- Do not combine tablets and tablets for oral suspension to reach the dose
- Start dexamethasone alcohol-free mouthwash for stomatitis prophylaxis
- Withhold >=1 week before elective surgery
Cautions
- Non-infectious pneumonitis
- Infections (may be serious/fatal)
- Severe hypersensitivity reactions
- Angioedema (increased risk with concomitant ACE inhibitors)
- Stomatitis / oral ulceration
- Renal failure
- Impaired wound healing
- Metabolic disorders (hyperglycemia, hyperlipidemia)
- Myelosuppression
- Radiation sensitization / recall
- Embryo-fetal toxicity
Adverse reactions
- Stomatitis
- Infections
- Rash
- Fatigue / asthenia
- Diarrhea
- Edema
- Abdominal pain, nausea
- Fever, cough, headache, decreased appetite
Pregnancy Can cause fetal harm (animal data, mechanism); advise pregnant women of risk and use effective contraception.
Lactation Do not breastfeed during treatment and for 2 weeks after the last dose.
⚠ BOXED WARNINGS
- Immunosuppression, infection and lymphoma
- Kidney graft thrombosis; nephrotoxicity with cyclosporine
No boxed warning for Afinitor, the oncology product, but Zortress, the transplant product carries a boxed warning for immunosuppression, infection and lymphoma, graft thrombosis and nephrotoxicity with cyclosporine.
Cost, est. cash$50–$10,000/month or cycle
Generic entry2018
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Everolimus ballicule
Open Everolimus in the interactive console ↗
Memory aids: mascots and interaction avatars
