Everolimus interactions

Food & lifestyle

• grapefruit juice

  Moderate

  Metabolism

  Grapefruit juice may significantly increase the plasma concentrations of orally administered everolimus. The mechanism is inhibition of CYP450 3A4 and P-glycoprotein activity in the gut wall by certain compounds present in grapefruit.

  What to do: Patients treated with everolimus should avoid consumption of grapefruit and grapefruit juice.

  1 source

  1. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

Conditions

Conditions in which Everolimus needs care, as documented in this source.

• Kidney Diseases

  Major

  Cases of renal failure, including acute renal failure and elevations of serum creatinine and proteinuria, some with a fatal outcome, have been observed in patients treated with inhibitors of mTOR (mammalian target of rapamycin). Therapy with these agents should be administered cautiously in patients with renal dysfunction, in particularly where patients have additional risk factors that may further impair renal function. Renal impairment is not expected to influence drug exposure, and no dosage adjustment is recommended in patients with renal impairment. Monitoring of renal function, including measurement of blood urea nitrogen (BUN), urinary protein, or serum creatinine, is recommended prior to the start of therapy and periodically thereafter.

  2 sources

  1. "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories (2007):
  2. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

• Liver Diseases

  Major

  Everolimus exposure was increased in patients with mild (Child-Pugh class A), moderate (Child-Pugh class B), and severe (Child-Pugh class C) hepatic impairment. In patients with mild or moderate hepatic impairment, a dose reduction is recommended. Patients with severe hepatic impairment, everolimus may be used at a reduced dose if the desired benefit outweighs the risk.

  1 source

  1. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

• Hematologic Diseases

  Moderate

  Hematologic abnormalities, including decreased levels of hemoglobin, lymphocytes, platelets, and white blood cell have been observed in patients taking everolimus. Caution is recommended when treating patients predisposed to hematologic changes. Periodic monitoring of complete blood count is recommended before starting therapy and periodically thereafter.

  1 source

  1. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

• Hypercholesterolemia

  Moderate

  Elevations in cholesterol and triglyceride levels have been reported in patients taking inhibitors of mTOR (mammalian target of rapamycin). Monitoring of fasting lipid profile is recommended prior to the start of therapy and periodically thereafter. Clinicians should achieve control of lipid levels before initiating therapy with these agents.

  2 sources

  1. "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories (2007):
  2. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

• Hyperglycemia

  Moderate

  Elevations in serum blood glucose levels have been reported in patients taking inhibitors of mTOR (mammalian target of rapamycin). Monitoring of fasting serum glucose levels is recommended prior to the start of therapy and periodically thereafter. Clinicians should achieve control of glucose levels before initiating therapy with these agents.

  2 sources

  1. "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories (2007):
  2. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

• Infections

  Moderate

  The immunosuppressant effect of inhibitors of mTOR (mammalian target of rapamycin) may decrease host resistance to infectious agents and may predispose patients to bacterial, fungal, viral, or protozoal infections, infections with opportunistic pathogens, and reactivation of viral infections. Therapy with these agents should be administered with caution in patients with an infection, particularly active infections or any untreated systemic fungal, bacterial, parasitic, or viral infection. It is recommended to complete the treatment of preexisting invasive fungal infections prior to starting treatment and if a diagnosis of invasive systemic fungal infection is made during treatment, discontinue and treat with appropriate antifungal therapy.

  2 sources

  1. "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories (2007):
  2. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):

• Wounds and Injuries

  Moderate

  Inhibition of mTOR activity results in delays of wound healing and increases the occurrence of wound-related complications, which might require surgical intervention. Patients with central nervous system tumors (primary CNS tumor or metastases) and/or receiving anticoagulation therapy may be at an increased risk of developing intracerebral bleeding (including fatal outcomes). Caution is recommended when using these agents, particularly in the perioperative period.

  2 sources

  1. "Product Information. Torisel (temsirolimus)." Wyeth-Ayerst Laboratories (2007):
  2. "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals (2009):