AFINITOR DISPERZ (Everolimus)

What is this medication?

Everolimus, Afinitor (US/CDN)/Zortress (US)
Antineoplastic Agent; mTOR Kinase Inhibitor; Immunosuppressant Agent

“ALERT: US Boxed Warning

Breast cancer; Neuroendocrine tumors; Renal cell carcinoma; Tuberous sclerosis complex-associated renal angiomyolipoma (Afinitor only)

Tuberous sclerosis complex-associated partial-onset seizures (Afinitor Disperz only)

Tuberous sclerosis complex-associated subependymal giant cell astrocytoma (Afinitor or Afinitor Disperz only)

Liver transplantation; Renal transplantation (Zortress only)

How does this medication work? 

Everolimus, Afinitor/Zortress Everolimus is a macrolide immunosuppressant and a mechanistic target of rapamycin (mTOR) inhibitor which has antiproliferative and antiangiogenic properties.

How should I take this medication? 

Afinitor: Oral: 10 mg once daily until disease progression or unacceptable toxicity; Initial: 4.5 mg/m2 and adjust based on serum concentrations, tolerability, and response.
Afinitor Disperz: Oral: Initial: 4.5 or 5 mg/m2 once daily until disease progression or unacceptable toxicity.

How to Take: Swallow whole with a glass of water. May be taken with or without food, but to reduce variability take consistently with regard to food. Administer at the same time(s) each day. Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and moisture. Store Afinitor and Afinitor Disperz in the original container.

You Need to Avoid:  Significant drug interactions exist, requiring dose/frequency adjustment or avoidance so avoid starting any new medications without consulting prescriber. Avoid grapefruit and grapefruit juice. Patients should not be immunized with live viral vaccines during or shortly after treatment and should avoid close contact with recently vaccinated (live vaccine) individuals.

What should I watch for while using this medication?

Before starting Everolimus, Afinitor/Zortress make sure your physician is aware of any allergies or medications you currently take, if you have had a heart transplant, if you have hepatic impairment, hereditary galactose intolerance, renal impairment, a solid organ transplant (aside from liver/kidney), are pregnant, or breastfeeding. Everolimus, Afinitor/Zortress use has been associated with rare but serious adverse events such as angioedema, bone marrow suppression, edema, graft thrombosis, hepatic artery thrombosis, hypersensitivity reactions, increased risk of infection, malignancy, metabolic effects, mucositis, stomatitis, nephrotoxicity, pulmonary toxicity, and wound healing impairment.

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible. However, if it is almost time for your next dose, take only that scheduled dose. Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times. Store at room temperature, 59 to 86° F (15 to 30° C). Protect from light. Keep the container tightly closed.  Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication? 

Transplantation: Hypertension, peripheral edema, diabetes mellitus, hypercholesterolemia, hyperglycemia, hyperkalemia, hypokalemia, hypomagnesemia, hypophosphatemia, abdominal pain, constipation, diarrhea, nausea, vomiting, dysuria, hematuria, urinary tract infection, anemia, leukopenia, bacterial infection, hepatitis C, infection, viral infection, fatigue, headache, insomnia, back pain, limb pain, increased serum creatinine, upper respiratory tract infection, fever, wound healing impairment

Antineoplastic: Edema, hypertension, peripheral edema, acne vulgaris, nail disease, pruritus, skin rash, xeroderma, amenorrhea, decreased serum bicarbonate, decreased serum fibrinogen, hypercholesterolemia, hyperglycemia, hypertriglyceridemia, hypoalbuminemia, hypocalcemia, hypokalemia, hypophosphatemia, abdominal pain, anorexia, constipation, decreased appetite, diarrhea, dysgeusia, gastroenteritis, nausea, stomatitis, vomiting, weight loss, xerostomia, irregular menses, proteinuria, urinary tract infection, anemia, leukopenia, lymphocytopenia, neutropenia, prolonged partial thromboplastin time, prolonged prothrombin time, thrombocytopenia, increased serum alanine aminotransaminase, increased serum alkaline phosphatase, increased serum aspartate aminotransferase, infection, aggressive behavior, anxiety, behavioral problems, dizziness, fatigue, headache, insomnia, malaise, migraine, arthralgia, asthenia, back pain, limb pain, myalgia, increased serum creatinine, cough, dyspnea, epistaxis, nasopharyngitis, oropharyngeal pain, pneumonia, pneumonitis, respiratory tract infection, rhinitis , upper respiratory tract infection, fever

Note this is not a complete list of side effects, only the most common