Everolimus

What is Everolimus?

• Everolimus (Afinitor) is a kinase inhibitor.

Everolimus ball-and-stick

Everolimus

What are the uses of this medicine?

Afinitor is a prescription medicine used to treat:

• advanced hormone receptor-positive, HER2-negative breast cancer, along with the medicine exemestane, in postmenopausal women who have already received certain other medicines for their cancer.
• adults with a type of pancreatic cancer known as pancreatic neuroendocrine tumor (PNET), that has progressed and cannot be treated with surgery.
• adults with a type of cancer known as neuroendocrine tumor (NET) of the stomach and intestine (gastrointestinal), or lung that has progressed and cannot be treated with surgery.
• Afinitor is not for use in people with carcinoid tumors that actively produce hormones.
• adults with advanced kidney cancer (renal cell carcinoma or RCC) when certain other medicines have not worked.
• people with the following types of tumors that are seen with a genetic condition called tuberous sclerosis complex (TSC):
• adults with a kidney tumor called angiomyolipoma, when their kidney tumor does not require surgery right away.
• adults and children 1 year of age and older with a brain tumor called subependymal giant cell astrocytoma (SEGA) when the tumor cannot be removed completely by surgery.

Limitations of Use: Afinitor is not indicated for the treatment of patients with functional carcinoid tumors.

Afinitor Disperz is a prescription medicine used to treat:

• adults and children 1 year of age and older with a genetic condition called tuberous sclerosis complex (TSC) who have a brain tumor called subependymal giant cell astrocytoma (SEGA) when the tumor cannot be removed completely by surgery.
• adults and children 2 years of age and older with a genetic condition called tuberous sclerosis complex (TSC) who have certain types of seizures(epilepsy), as an added treatment to other antiepileptic medicines.

How does this medicine work?

• Everolimus (e" ver oh' li mus) binds to the same intracellular receptor as tacrolimus and cyclosporine, but does not inhibit calcineurin; rather, it blocks the "mammalian target of rapamycin" (mTOR), which interrupts signaling pathways of several cytokines and growth factors including IL2 and causes a decrease in protein synthesis and cell cycle arrest.
• Everolimus therapy has been shown to improve graft survival after solid organ transplantation and to improve time to progression in several forms of cancer.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• with clinically significant hypersensitivity to everolimus or to other rapamycin derivatives.

What drug interactions can this medicine cause?

Avoid concomitant use with P-gp and strong CYP3A4 inhibitors.

• Reduce the dose for patients taking Afinitor/Afinitor Disperz with a P-gp and moderate CYP3A4 inhibitor as recommended.
• Increase the dose for patients taking Afinitor/Afinitor Disperz with a P-gp and strong CYP3A4 inducer as recommended.
• Avoid the concomitant use of ACE inhibitors with Afinitor/Afinitor Disperz.

Is this medicine FDA approved?

• Everolimus was approved for use in the United States in 2009 initially as an agent to prevent rejection after kidney and liver transplantaiton and later, in higher doses, as therapy of advanced renal cell, breast and pancreatic neuroendocrine cancers given alone or in combination with other antineoplastic agents.
• More recently, everolimus was approved as therapy of renal angiomyolipoma and subependymal giant cell astrocytoma associated with tuberous sclerosis complex (in which mTOR signaling is dysregulated).
• Everolimus like sirolimus is also used in drug eluting arterial stents, to prevent stenosis.

How should this medicine be used?

Recommended dosage: Recommended Dosage for Hormone Receptor-Positive, HER2-Negative Breast Cancer

• The recommended dosage of Afinitor is 10 mg orally once daily until disease progression or unacceptable toxicity.

Recommended Dosage for Neuroendocrine Tumors (NET)

• The recommended dosage of Afinitor is 10 mg orally once daily until disease progression or unacceptable toxicity.

Recommended Dosage for Renal Cell Carcinoma (RCC)

• The recommended dosage of Afinitor is 10 mg orally once daily until disease progression or unacceptable toxicity.

Recommended Dosage for Tuberous Sclerosis Complex (TSC)-Associated Renal Angiomyolipoma

• The recommended dosage of Afinitor is 10 mg orally once daily until disease progression or unacceptable toxicity.

Recommended Dosage for Tuberous Sclerosis Complex (TSC)-Associated Subependymal Giant Cell Astrocytoma (SEGA)

• The recommended starting dosage of Afinitor/Afinitor Disperz is 4.5 mg/m2 orally once daily until disease progression or unacceptable toxicity.

Recommended Dosage for Tuberous Sclerosis Complex (TSC)-Associated Partial-Onset Seizures

• The recommended starting dosage of Afinitor Disperz is 5 mg/m2 orally once daily until disease progression or unacceptable toxicity.

• Modify the dose for patients with hepatic impairment or for patients taking drugs that inhibit or induce P-glycoprotein (P-gp) and CYP3A4.

Administration:

• Take Afinitor or Afinitor Disperz exactly as your healthcare provider tells you to.
• Your healthcare provider may change your dose of Afinitor or Afinitor Disperz or tell you to temporarily interrupt dosing, if needed.
• Take only Afinitor or Afinitor Disperz. Do not mix Afinitor and Afinitor Disperz together.
• Use scissors to open the blister pack.
• Take Afinitor or Afinitor Disperz 1 time each day at about the same time.
• Take Afinitor or Afinitor Disperz the same way each time, either with food or without food.
• If you take too much Afinitor or Afinitor Disperz, contact your healthcare provider or go to the nearest hospital emergency room right away. Take the pack of Afinitor or Afinitor Disperz with you.
• If you miss a dose of Afinitor or Afinitor Disperz, you may take it if it is less than 6 hours after the time you normally take it. If it is more than 6 hours after you normally take your Afinitor or Afinitor Disperz, skip the dose for that day. The next day, take Afinitor or Afinitor Disperz at your usual time. Do not take 2 doses to make up for a missed dose. If you are not sure about what to do, call your healthcare provider.
• You should have blood tests before you start Afinitor or Afinitor Disperz and as needed during your treatment. These will include tests to check your blood cell count, kidney and liver function, cholesterol, and blood sugar levels.
• If you take Afinitor or Afinitor Disperz to treat SEGA or Afinitor Disperz to treat certain types of seizures with TSC, you will also need to have blood tests regularly to measure how much medicine is in your blood. This will help your healthcare provider decide how much Afinitor or Afinitor Disperz you need to take.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Afinitor: 2.5 mg, 5 mg, 7.5 mg, and 10 mg tablets
• Afinitor Disperz: 2 mg, 3 mg, and 5 mg tablets

This medicine is available in fallowing brand namesː

• Afinitor®
• Afinitor Disperz®

What side effects can this medication cause?

The most common side effects of this medicine include: Breast cancer, NET, RCC:

• stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, and decreased appetite.

TSC-Associated Renal Angiomyolipoma:

• stomatitis

TSC-Associated SEGA

• stomatitis and respiratory tract infection

TSC-Associated Partial-Onset Seizures

• stomatitis

Afinitor and Afinitor Disperz can cause serious side effects which may include:

• You may develop lung or breathing problems
• You may be more likely to develop an infection
• Severe allergic reactions
• Possible increased risk for a type of allergic reaction called angioedema
• Mouth ulcers and sores
• kidney failure
• Risk of wound healing problems
• Increased blood sugar and fat (cholesterol and triglyceride) levels in the blood
• Decreased blood cell counts
• Worsening side effects from radiation treatment

What special precautions should I follow?

• Non-Infectious Pneumonitis may occur. Monitor for clinical symptoms or radiological changes. Withhold or permanently discontinue based on severity.
• Infections may occur .Monitor for signs and symptoms of infection. Withhold or permanently discontinue based on severity.
• Severe Hypersensitivity Reactions may occur during treatment course. Permanently discontinue for clinically significant hypersensitivity.
• Angioedema may occur. Patients taking concomitant angiotensin-converting-enzyme (ACE) inhibitors may be at increased risk for angioedema. Permanently discontinue for angioedema.
• Stomatitis may occur. Initiate dexamethasone alcohol-free mouthwash when starting treatment.
• Renal Failure risk may be increased. Monitor renal function prior to treatment and periodically thereafter.
• Risk of Impaired Wound Healing may occur. Withhold for at least 1 week prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of treatment after resolution of wound healing complications has not been established.
• Monitor and adjust dose for adverse reactions in Geriatric Patients.
• Metabolic Disorders may occur. Monitor serum glucose and lipids prior to treatment and periodically thereafter. Withhold or permanently discontinue based on severity.
• Myelosuppression may occur. Monitor hematologic parameters prior to treatment and periodically thereafter. Withhold or permanently discontinue based on severity.
• Risk of Infection or Reduced Immune Response with Vaccination may occur. Avoid live vaccines and close contact with those who have received live vaccines. Complete recommended childhood vaccinations prior to starting treatment.
• Severe radiation reactions may occur.
• Afinitor and Afinitor Disperz Can cause fetal harm. Advise patients of reproductive potential of the potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on animal studies and the mechanism of action, Afinitor/Afinitor Disperz can cause fetal harm when administered to a pregnant woman.

Can this medicine be used in children?

• The safety and effectiveness of Afinitor/Afinitor Disperz have been established in pediatric patients age 1 year and older with TSC-associated SEGA that requires therapeutic intervention but cannot be curatively resected.
• The safety and effectiveness of Afinitor Disperz has been established for the adjunctive treatment of pediatric patients aged 2 years and older with TSC-associated partial-onset seizures.

The safety and effectiveness of Afinitor/Afinitor Disperz in pediatric patients have not been established in:

• Hormone receptor-positive, HER2-negative breast cancer
• Neuroendocrine tumors (NET)
• Renal cell carcinoma (RCC)
• TSC-associated renal angiomyolipoma

What are the active and inactive ingredients in this medicine?

Afinitor

• Active ingredient:

everolimus

• Inactive ingredients:

anhydrous lactose, butylated hydroxytoluene, crospovidone, hypromellose, lactose monohydrate, and magnesium stearate

Afinitor Disperz

• Active ingredient: everolimus.
• Inactive ingredients: butylated hydroxytoluene, colloidal silicon dioxide, crospovidone, hypromellose, lactose monohydrate, magnesium stearate, mannitol, and microcrystalline cellulose

Who manufactures and distributes this medicine?

Distributed by: Novartis Pharmaceuticals Corporation East Hanover, New Jersey

What should I know about storage and disposal of this medication?

• Store Afinitor or Afinitor Disperz at room temperature, between 68°F to 77°F (20°C to 25°C).
• Keep Afinitor or Afinitor Disperz in the pack it comes in.
• Open the blister pack just before taking Afinitor or Afinitor Disperz.
• Keep Afinitor or Afinitor Disperz dry and away from light.
• Do not use Afinitor or Afinitor Disperz that is out of date or no longer needed.
• Keep Afinitor or Afinitor Disperz and all medicines out of the reach of children.

• Dailymed label info on Everolimus
• FDA Everolimus

Everolimus Resources
Need Help Finding a Doctor? WikiMD's DocFinder can help find general and specialist physicians.	Latest articles Most recent articles Ongoing trials.

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• Dailymed label info on Everolimus
• FDA Everolimus

Everolimus Resources
Need Help Finding a Doctor? WikiMD's DocFinder can help find general and specialist physicians.	Latest articles Most recent articles Ongoing trials.