Everolimus is used to treat some forms of breast cancer in postmenopausal women who have not responded as expected to other drug therapies. It is also used to treat certain progressive pancreatic neuroendocrine tumors, advanced kidney cancer resistant to treatment with sorafenib or sunitinib, and some forms of renal angiomiopolipoma, tuberous sclerosis complex, and subependymal giant cell astrocytoma. Everolimus is also used in certain patients to prevent organ rejection after a kidney or liver transplant.

 

What is Everolimus?

Everolimus blocks cell proliferation and induces apoptosis (cell death) by inhibiting the activity of the mTOR protein.  It also decreases the production of new blood vessels (angiogenesis) and glucose absorption. Everolimus acts as an immunosuppressant by blocking the action of certain blood cells in the immune system. These cells may cause the body to reject the transplanted organ.  

 

How should Everolimus be taken?

Everolimus is administered orally. For the treatment of breast cancer, certain medications are combined with exemestane. In general, however, immunosuppressive treatment involves the combination of certain medications and cyclosporine.

 

Side effects associated with Everolimus

Everolimus can slow down the healing of surgical wounds, reduce the body's ability to fight infection, reduce the amount of sperm produced and promote the onset of hyperglycemia or diabetes.  It can also be associated with the appearance of a non-infectious pneumonia and an increased risk of developing cancers (especially skin cancer).

 

Among the other possible side effects of everolimus include the following:

 

  • Pain in the back, arms or legs
  • Constipation
  • Diarrhea
  • Dizziness
  • Drowsiness
  • Headache
  • Loss of appetite
  • Nausea
  • Vomiting
  • Stomach pain or discomfort
  • Tiredness or weakness
  • Insomnia
  • Sexual problems in men

 

It is important to contact a doctor immediately if you experience:

 

  • Rash
  • Urticaria
  • Difficulty breathing
  • Tightness in the chest or chest pain
  • Swelling of the mouth, face, lips or tongue
  • Unusual hoarseness
  • bloody stool
  • pain, swelling, redness or tenderness in the legs or calves
  • Appearance changes
  • Confusion
  • Fainting
  • Fast or irregular heartbeat
  • Persistent fever, chills or sore throat
  • Hallucinations
  • Changes in mood or behavior
  • Muscle pain or weakness
  • Onset of a cough or worsening of an existing cough
  • Numbness or tingling
  • Pale stools
  • Severe or persistent constipation, diarrhea, nausea, stomach pain or vomiting
  • Severe or persistent dizziness or headaches
  • Severe or persistent tiredness or weakness
  • Shortness of breath or other breathing problems
  • Blisters in the mouth or on the tongue
  • Stomach swelling
  • Swelling of arms, hands, feet or ankles
  • Swollen lymph nodes
  • Hyperglycemia
  • Kidney or urinary problems
  • Tremors
  • Bruising or bleeding
  • Vision problems
  • White patches in the mouth
  • Jaundice

 

Contraindications and warnings associated with the use of Everolimus

Everolimus is contraindicated in case of heart transplant, some hereditary disorders or  if you are taking delavirdine.

 

During treatment with this drug it is necessary to avoid eating grapefruit or drinking its juice. In addition, women of childbearing age must use effective birth control methods while taking this drug and 8 weeks following discontinuation of therapy.

 

Everolimus can impair the ability to drive or operate hazardous machinery. This side effect can be aggravated by alcohol or other medicines.

 

Before starting treatment with everolimus, it is important to tell your doctor if:

 

  • You have any allergies to the active substance, its excipients or to any other drugs, food or various substances
  • You are taking any other medications, herbal remedies or supplements. Mentioning in particular:  other immunosuppressive agents, ACE inhibitors, fibrates, HMG-CoA reductase inhibitors, drugs that can damage the liver, aprepitant, azole antifungals, delavirdine, digoxin, diltiazem, macrolide antibiotics, nefazodone, nicardipine, protease inhibitors, telithromycin, verapamil, carbamazepine, dexamethasone, efavirenz, hydantoins, nevirapine, phenobarbital, primidone, or rifamycins hypericum
  • You are suffering (or have suffered) from diabetes or hyperglycemia, high cholesterol or high triglycerides, bone marrow or blood problems, weakened  immune system, lung or breathing problems, infections, liver disease or skin cancer
  • You have a family history of skin cancer  
  • You have recently received live vaccines
  • You have recently been in contact with individuals who have received live vaccines
  • You are pregnant or breast-feeding

 

It is important to inform physicians, surgeons and dentists of any ongoing treatment with everolimus.