About Afinitor in Advanced Renal Cell Carcinoma

Once-daily Afinitor® (everolimus) tablets are the only therapy with randomized, placebo-controlled Phase III evidence after failure of either sunitinib or sorafenib or both

Please see Important Safety Information below

Afinitor is a once-daily, oral inhibitor of mTOR (mammalian target of rapamycin) indicated for the treatment of patients with advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib. The active ingredient in Afinitor, everolimus, specifically blocks the activity of mTOR, an intracellular regulator important in tumor progression.1-4 Unlike other therapies that primarily inhibit tumor angiogenesis, Afinitor targets both tumor cells and blood vessel cells.2-4 Afinitor specifically blocks mTOR in 2 places, resulting in 3 distinct effects:

  • Reduced tumor cell growth and proliferation1,3,5
  • Reduced cell metabolism1,3,5
  • Reduced tumor angiogenesis2,3

When a VEGFR-TKI, such as sunitinib or sorafenib fails, Afinitor may be an option for your patients.

Learn more about Afinitor (everolimus) tablets in an interactive video presentation with Dr. Daniel George.

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Download the annotated prescribing information for key prescribing information highlighted and explained.

Afinitor is indicated for the treatment of patients with advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib.

Important Safety Information

Afinitor is contraindicated in patients with hypersensitivity to everolimus, to other rapamycin derivatives, or to any of the excipients.

Non-infectious pneumonitis is a class effect of rapamycin derivatives, including Afinitor. Fatal outcomes have been observed. If symptoms are moderate or severe, patients should be managed with dose interruption until symptoms improve or discontinuation, respectively. Corticosteroids may be indicated. Afinitor may be reintroduced at 5 mg daily depending on the individual clinical circumstances.

Afinitor has immunosuppressive properties and may predispose patients to infections. Localized and systemic infections (bacterial and invasive fungal infections) have occurred. Some of these infections have been severe or fatal. Complete treatment of pre-existing invasive fungal infections prior to starting treatment. If a diagnosis of invasive systemic fungal infection is made, discontinue Afinitor and treat with appropriate antifungal therapy.

Oral ulcerations have occurred in patients treated with Afinitor. In such cases, topical treatments are recommended, but alcohol- or peroxide-containing mouthwashes should be avoided. Antifungal agents should not be used unless fungal infection has been diagnosed.

Elevations of serum creatinine, glucose, lipids, and triglycerides and reductions of hemoglobin, lymphocytes, neutrophils and platelets have been reported in clinical trials. Renal function, hematological parameters, blood glucose, and lipids should be evaluated prior to treatment and periodically thereafter. When possible, optimal glucose and lipid control should be achieved before starting a patient on Afinitor.

Co-administration with strong or moderate inhibitors of CYP3A4 or PgP should be avoided. Increase in the Afinitor dose is recommended when co-administered with a strong CYP3A4 inducer.

Afinitor should not be used in patients with severe hepatic impairment.

The use of live vaccines and close contact with those who have received live vaccines should be avoided during treatment with Afinitor.

Fetal harm can occur if Afinitor is administered to a pregnant woman.

The most common adverse reactions (incidence ≥30%) were stomatitis (44%), infections (37%), asthenia (33%), fatigue (31%), cough (30%), and diarrhea (30%). The most common grade 3/4 adverse reactions (incidence ≥3%) were infections (9%), dyspnea (8%), fatigue (5%), stomatitis (4%), dehydration (4%), pneumonitis (4%), abdominal pain (3%), and asthenia (3%). The most common laboratory abnormalities (incidence ≥50%) were anemia (92%), hypercholesterolemia (77%), hypertriglyceridemia (73%), hyperglycemia (57%), lymphopenia (51%), and increased creatinine (50%). The most common grade 3/4 laboratory abnormalities (incidence ≥3%) were lymphopenia (18%), hyperglycemia (16%), anemia (13%), hypophosphatemia (6%), and hypercholesterolemia (4%). Deaths due to acute respiratory failure (0.7%), infection (0.7%), and acute renal failure (0.4%) were observed on the Afinitor arm.

Full Prescribing Information about Afinitor.

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References
  • Afinitor [prescribing information]. East Hanover, NJ: Novartis Pharmaceuticals Corporation; 2009.
  • Dancey JE. Inhibitors of the mammalian target of rapamycin. Expert Opin Investig Drugs. 2005;14:313-328.
  • Hartford CM, Ratain MJ. Rapamycin: something old, something new, sometimes borrowed and now renewed.
    Clin Pharmacol Ther. 2007;82:381-388.
  • Hay N, Sonenberg N. Upstream and downstream of mTOR. Genes Dev. 2004;18:1926-1945.
  • Wullschleger S, Loewith R, Hall MN. TOR signaling in growth and metabolism. Cell. 2006;124:471-484.