II. Indications
-
Solid Organ Transplant
Immunosuppression (maintenance prevention of rejection)
- Not approved for Heart Transplant (increased mortality)
- Renal Transplant
- Liver Transplant
- Malignancy
- Breast Cancer (postmenopausal, advanced, Hormone receptor-positive, HER2-negative)
- Neuroendocrine tumors of pancreatic origin (PNET, adults, progressive)
- Renal Cell Carcinoma (RCC, advanced, refractory)
- Renal angiomyolipoma (adults not requiring immediate surgery)
- Tuberous sclerosis complex (TSC, adults not requiring immediate surgery)
- Also indicated in age >1 year with subependymal giant cell astrocytoma (SEGA, non-resectable needing treatment)
III. Mechanism
IV. Medications
- Everolimus (Afinitor, Zortress) tablets: 0.25 mg, 0.5 mg, 0.75 mg
V. Dosing
- See other references for specific dosing regimens per indication
- Prescribers are typically specialists knowledgeable about the risks and monitoring
- Decrease dose in renal dysfunction, and adjust doses based on serum levels
VI. Adverse Effects
- Nephrotoxicity including Proteinuria
- Myelosuppression
- Rash
- Delayed Wound Healing
- Secondary Malignancy (including Lymphoma)
- Male Infertility
- Cardiopulmonary
- Interstitial Lung Disease or Pulmonary fibrosis
- Hyperlipidemia
- Edema
- Thrombosis
- Hepatic artery thrombosis
- Kidney graft thrombosis
-
Thrombotic Thrombocytopenic Purpura (TTP) or Hemolytic Uremic Syndrome (HUS)
- More common in combination with Cyclosporine
-
Angioedema
- More common in combination with ACE Inhibitors
- Serious Infections (including Polyoma Virus Infections)
- Latent Viral Infection activation
- BK virus associated nephropathy
VII. Drug Interactions
- See Cytochrome P-450 3A4
- Many Drug Interactions
- Agents that increase Purine Synthesis Inhibitor concentrations
- Linezolid potentiates myelosuppression
- Erythromycin (and Clarithromycin to a lesser extent)
- Agents that decrease Purine Synthesis Inhibitor concentrations
-
Cyclosporine
- Decrease Cyclosporine dosing to decrease nephrotoxic effects
- Live Virus Vaccines
- Avoid while using Everolimus
VIII. Safety
- Avoid in Lactation
- Avoid in Pregnancy (despite original Pregnancy Category C designation)
- Use reliable Contraception during treatment and for at least 8 weeks after completion
IX. Resources
- Everolimus Oncology Indications (DailyMed)
- Everolimus Transplant Indications (DailyMed)
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Related Studies
| everolimus (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| EVEROLIMUS 0.5 MG TABLET | Generic | $12.55 each |