Adult Dosing
Advanced renal cell carcinoma, advanced PNET, and renal angiomyolipoma with TSC (Afinitor)
- 10 mg PO qd at the same time every day
Note:
- Administer either consistently with food or without food. Should be swallowed wholly with a glass of water. Do not break or crush tablets
Advanced hormone receptor-positive, HER2-Negative Breast Cancer(Afinitor)
- 10 mg PO qd at the same time every day
Note:
- Used after failure of treatment with letrozole or anastrozole
- Administer either consistently with food or without food. Should be swallowed whole with a glass of water. Do not break or crush tablets
Subependymal giant cell astrocytoma (SEGA)
- BSA: 0.5-1.2m2: 2.5 mg PO qd
- BSA: 1.3-2.1m2: 5 mg PO qd
- BSA:
2.2m2: 7.5 mg PO qd - Evaluate SEGA volume approximately 3 months after starting therapy and periodically thereafter; dose adjustments may be made at 2 week intervals. Trough concentrations should be assessed every 2 weeks, dosing should be titrated to attain a concentration of 5-10 ng/mL
Note:
- Patient with SEGA < 3 years of age or with BSA < 0.58m2: Not recommended
Kidney transplant rejection prophylaxis (Zortress)
- Initial 0.75 mg bid (1.5 mg/day) in combination with reduced dose cyclosporine as soon as possible after transplantation
- May adjust dose at 4-5 day intervals to achieve everolimus trough concentration target range 3-8 ng/mL (using an LC/MS/MS assay method)
Prophylaxis of allograft rejection in liver transplant (Zortress)
- Initial dose: 1 mg PO bid
Notes:- Administer the therapy at least 30 days post transplant, in combination with reduced doses of tacrolimus and corticosteroids
- Dose adjustments should be based on trough whole blood concentrations. Recommended dose - 3-5 ng/mL by 3 weeks after first dose of everolimus and through 12 months post transplant
- Corticosteriod should be tapered on an individualized basis, depending on clinical status and function of graft
Pediatric Dosing
- Notes:
- Safety and efficacy in pediatric patients (< 18 years) has not been established [Zortress]
- Patient with SEGA < 3 years of age or with BSA < 0.58m2: Not recommended
Subependymal giant cell astrocytoma (SEGA) 3 years and older
- BSA: 0.5-1.2m2: 2.5 mg PO qd
- BSA: 1.3-2.1m2: 5 mg PO qd
- BSA: 2.2m2: 7.5 mg PO qd
- Evaluate SEGA volume approximately 3 months after starting therapy and periodically thereafter; dose adjustments may be made at 2 week intervals. Trough concentrations should be assessed every 2 weeks, dosing should be titrated to attain a concentration of 5-10 ng/mL
[Outline]
See Supplemental Patient Information
- Physicians experienced in management of systemic immunosuppressant therapy in transplantation should prescribe this drug [US Black Box Warning]
- It has immunosuppressive properties and can cause increased risk of infections. Observe for signs and symptoms and institute appropriate treatment [US Black Box Warning]
- Manage patients in facilities equipped and staffed with adequate laboratory and supportive medical resources [US Black Box Warning]
- Increased mortality is often associated with serious infections, reported within the first 3 months post-transplantation, hence the therapy is not recommended for use in heart transplantation [US Black Box Warning]
- Avoid prolonged exposure to UV light and sunlight
- Malignancy risk may be increased
- Concomitant use of everolimus with other drugs known to cause angioedema
- May increase risk of new onset diabetes mellitus after transplant; closely monitor blood glucose concentrations in patients using everolimus
- Increased risk of kidney arterial and venous thrombosis resulting in graft loss was reported [US Black Box Warning]
- Avoid contact with live vaccines and close contact with those who have received live vaccines
- Adverse reactions include:
- Non-infectious pneumonitis
- Opportunistic infections
- Oral ulceration, stomatitis, and oral mucositis
- It can cause elevations of serum creatinine, blood glucose and lipids and decrease in levels of hemoglobin, lymphocytes, neutrophils and platelets
- Grapefruit and grapefruit juice inhibit cytochrome P450 3A4 and P-gp activity and hence avoid concomitant use of everolimus and cyclosporine
- Monitor renal function, including measurement of blood urea nitrogen (BUN) or serum creatinine, complete blood count, fasting serum glucose and lipid profile prior to and periodically during therapy
- Hypersensitivity reactions including angioedema and anaphylaxis have been reported
- Impaired wound healing and wound complications may occur
- Male infertility may occur
- Polyoma virus associated nerophropathy may require dosage adjustments
- Thrombotic microangiopathy, thrombotic thromocytopenic purpura hemolytic uremic syndrome has been reported with concomitant use of cyclosporine
- Increased risk of proteinuria has been associated with the therapy, monitor the levels protein in urine during the treatment
- Avoid therapy in rare hereditary problems of galactose intolerance (Lapp lactase deficiency, glucose-galactose malabsorption) as diarrhea and malabsorption may occur
- Coadministration of CYP3A4 inducers (increase everolimus dose) and live vaccines should be avoided
Cautions: Use cautiously in
- Mild to moderate hepatic impairment (refer to dose adjustment section)
- Hyperlipidemia
- Lactation
Supplemental Patient Information
- Advise patient to report worsening respiratory symptoms or signs of infection promptly to health care professional
- Emphasize the importance of repeated laboratory tests to determine effectiveness and side effects
- Instruct patients to avoid use of live vaccines and close contact with those who have received live vaccines
Pregnancy Category:D (Afinitor) and C (Zortress)
Breastfeeding: Safety unknown, is excreted in breast milk of rats at a concentration of 3.5 times higher than serum levels. Manufacturer recommends discontinuation of breastfeeding, or postponing of treatment (taking into account the importance of the drug to the mother).
Pricing data from www.DrugStore.com in U.S.A.
- Zortress 0.25 MG TABS [Box] (NOVARTIS)
30 mg = $195.99
90 mg = $555.97
Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.
