Afinitor Disperz

Name: Afinitor Disperz

Afinitor Disperz and Lactation

It is not known if Afinitor Disperz crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. You should not do both. 

Afinitor Disperz Dosage

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your liver function
  • your weight
  • your height
  • your age

The recommended dose of Afinitor Disperz is 4.5 mg/m2 once daily. Your doctor will adjust your dose based on how much of the medication is in your blood.

In addition, your doctor will reduce your dose if you have poor liver function and if you are taking certain medications. 

What happens if I miss a dose?

Take the missed dose as soon as you remember. If you are more than 6 hours late, skip the missed dose. Do not take extra medicine to make up the missed dose.

Before Using Afinitor Disperz

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of everolimus when used for SEGA brain tumors in children. However, use is not recommended in children younger than 1 year.

Appropriate studies have not been performed on the relationship of age to the effects of everolimus when used for kidney cancer, neuroendocrine tumors, and kidney or liver transplants in children. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of everolimus in the elderly. However, elderly patients are more likely to have unwanted side effects, which may require caution and an adjustment in the dose for patients receiving everolimus.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Ritonavir

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Adenovirus Vaccine Type 4, Live
  • Adenovirus Vaccine Type 7, Live
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Benazepril
  • Boceprevir
  • Captopril
  • Carbamazepine
  • Ceritinib
  • Cholera Vaccine, Live
  • Clarithromycin
  • Cobicistat
  • Conivaptan
  • Dronedarone
  • Eliglustat
  • Enalapril
  • Enalaprilat
  • Enzalutamide
  • Fosinopril
  • Fosphenytoin
  • Idelalisib
  • Indinavir
  • Influenza Virus Vaccine, Live
  • Itraconazole
  • Ketoconazole
  • Lisinopril
  • Lopinavir
  • Lumacaftor
  • Measles Virus Vaccine, Live
  • Mitotane
  • Moexipril
  • Mumps Virus Vaccine, Live
  • Nefazodone
  • Nelfinavir
  • Perindopril
  • Phenytoin
  • Poliovirus Vaccine, Live
  • Posaconazole
  • Quinapril
  • Ramipril
  • Ribociclib
  • Rifampin
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Saquinavir
  • Smallpox Vaccine
  • St John's Wort
  • Telaprevir
  • Telithromycin
  • Trandolapril
  • Typhoid Vaccine
  • Varicella Virus Vaccine
  • Venetoclax
  • Verapamil
  • Voriconazole
  • Yellow Fever Vaccine
  • Zofenopril

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Grapefruit Juice

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Blood clotting problems or
  • Diabetes or
  • Hepatitis B infection, history of or
  • Hyperglycemia (high sugar in the blood) or
  • Hyperlipidemia (high cholesterol in the blood) or
  • Hypertriglyceridemia (high fat in the blood) or
  • Hypoxia (low oxygen in the blood) or
  • Infection (eg, bacteria, fungus, virus) or
  • Lung or breathing problems or
  • Lymphoma (cancer of the lymph glands) or
  • Proteinuria (protein in the urine) or
  • Skin cancer—Use with caution. May make these conditions worse.
  • Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Uses of Afinitor Disperz

  • It is used to treat cancer.
  • It is used to treat certain kinds of kidney cysts.
  • It may be given to you for other reasons. Talk with the doctor.

What do I need to tell my doctor BEFORE I take Afinitor Disperz?

  • If you have an allergy to everolimus, temsirolimus, sirolimus, or any other part of Afinitor Disperz (everolimus tablets for oral suspension).
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have an infection.
  • If you take any drugs (prescription or OTC, natural products, vitamins) that must not be taken with this medicine, like certain drugs that are used for HIV, infections, or depression. There are many drugs that must not be taken with Afinitor Disperz. Your doctor or pharmacist can tell you if you are taking a drug that must not be taken with this medicine.
  • If you are taking another drug that has the same drug in it.
  • If you are taking St. John's wort. Do not take St. John's wort with Afinitor Disperz. This medicine may not work as well.
  • If you are breast-feeding. Do not breast-feed while you take this medicine and for 2 weeks after your last dose.

This is not a list of all drugs or health problems that interact with Afinitor Disperz.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about Afinitor Disperz, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about Afinitor Disperz. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using Afinitor Disperz.

Review Date: October 4, 2017

Dosing & Uses

Dosage Forms & Strengths

tablet (Afinitor)

  • 2.5mg
  • 5mg
  • 7.5mg
  • 10mg

tablet for oral suspension (Afintior Disperz)

  • 2mg
  • 3mg
  • 5mg

tablet (Zortress)

  • 0.25mg
  • 0.5mg
  • 0.75mg

Breast Cancer

Afinitor: Indicated in postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole

10 mg PO qDay consistently with or without food (also see dosage modifications)

Renal Cell Carcinoma

Afinitor: Indicated for advanced renal cell carcinoma (RCC) after failure with sunitinib or sorafenib

10 mg PO qDay consistently with or without food (also see dosage modifications)

Renal Angiomyolipomas with TSC

Afinitor: Indicated for the treatment of noncancerous kidney tumors (renal angiomyolipomas) with tuberous sclerosis complex (TSC) in patients not requiring immediate surgery

10 mg PO qDay consistently with or without food (also see dosage modifications)

Advanced Neuroendocrine Tumors

Indicated for progressive neuroendocrine tumors (PNET) located in the pancreas that are not surgically resectable or are metastatic; also indicated for well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung

10 mg PO qDay consistently with or without food (also see dosage modifications)

Dosage Modifications (Breast Cancer, PNET, RCC, Renal Angiomyolipoma)

Concomitant strong CYP3A4 inducers: May increase dose by 5-mg increments; not to exceed 20 mg/day

Avoid strong CYP3A4 inhibitors

If moderate CYP3A4 and/or PgP inhibitors required: Decrease dose to 2.5 mg/day; if tolerated, may increase up to 5 mg/day

Treatment interruption, discontinuation, and/or dose reduction to 5 mg/day may be required to manage adverse drug effects (see manufacturer’s prescribing information)

Hepatic impairment

  • Mild (Child Pugh class A): Decrease dose to 7.5 mg qDay; dose may be decreased further to 5 mg qDay if not well tolerated
  • Moderate (Child Pugh class B): Decrease dose to 5 mg qDay; dose may be decreased further to 2.5 mg qDay if not well tolerated
  • Severe (Child Pugh class C): Decrease dose to 2.5 mg qDay; administer only if desired benefit outweighs risk; not to exceed 2.5 mg qDay
  • Adjust dose if status changes during treatment

Noninfectious pneumonitis

  • Grade 1: No dose adjustment required; initiate appropriate monitoring
  • Grade 2: Consider interrupting treatment until symptoms resolve to Grade ≤1 (rule out infection and consider treatment with corticosteroids); reinitiate at ~50% lower than the dose previously administered; discontinue treatment if failure to recover within 4 weeks
  • Grade 3: Interrupt treatment until symptoms resolve to Grade ≤1; consider reinitiating at ~50% lower than the dose previously administered; if toxicity recurs at Grade 4, consider discontinuation
  • Grade 4: Discontinue treatment

Stomatitis

  • Grade 1: No dosage adjustment required; manage with nonalcoholic or salt water (0.9%) mouthwash several times a day
  • Grade 2
    • Manage with topical analgesic mouth treatments (eg, benzocaine, butyl aminobenzoate, tetracaine hydrochloride, menthol or phenol) with or without topical corticosteroids (eg, triamcinolone oral paste)
    • Avoid using agents containing alcohol, hydrogen peroxide, iodine, and thyme derivatives in management of stomatitis which may worsen mouth ulcers
    • Interrupt dose until recovery to Grade ≤1; re-initiate treatment at the same dose
  • Grade 2 stomatitis recurs or Grade 3: Reinitiate at ~50% lower than the dose previously administered
  • Grade 4: Discontinue treatment and treat appropriately

Other nonhematologic toxicities

  • Treat appropriately and monitor
  • No dosage adjustment
    • Grade 1 or Grade 2 (if toxicity is tolerable)
  • Interrupt treatment until recovery at Grade ≤1
    • Grade 2 (if toxicity is intolerable): Reinitiate at same dose
    • Grade 2 toxicity recurs: Reinitiate at ~50% lower than the dose previously administered
    • Grade 3: Reinitiate at a lower dose
  • Discontinue treatment
    • Grade 3 recurs: Consider discontinuation
    • Grade 4

Metabolic events (eg, hyperglycemia, dyslipidemia)

  • Treat appropriately and monitor
  • Grade 1 or 2: No dosage adjustment required
  • Grade 3: Interrupt dose temporarily; reinitiate treatment ~50% lower than the dose previously administered
  • Grade 4: Discontinue treatment

Thrombocytopenia

  • Grade 1 (<75,000/mm³): No dosage adjustment required
  • Grade 2 (50,000 – 75,000/mm³): Interrupt dose until recovery at Grade ≤1; reinitiate treatment at same dose
  • Grade 3 or 4 (<50,000/mm³): Interrupt dose until recovery at Grade ≤1; reinitiate at ~50% lower than the dose previously administered

Neutropenia

  • Grade 1 or 2 (1,000 - 1,500/mm³): No dosage adjustment required
  • Grade 3 (500 – 1,000/mm³): Interrupt dose until recovery at Grade ≤2; reinitiate treatment at same dose
  • Grade 4 (<500/mm³): Interrupt dose until recovery at Grade ≤2; reinitiate at ~50% lower than the dose previously administered

Febrile neutropenia

  • Grade 3 (ANC <1,000/mm³ single temperature > 38.3ºC (101ºF) or a sustained temperature of ≥38ºC (100.4ºF) for >1hr): Interrupt dose until recovery at Grade ≤2 and no fever; reinitiate at ~50% lower than the dose previously administered
  • Grade 4 (Life-threatening consequences): Discontinue treatment

Subependymal Giant Cell Astrocytoma with TSC

Afinitor and Afinitor Disperz: Indicated for subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex that cannot be treated with surgery

Do not combine Afinitor tablets with Afinitor Disperz to achieve desired total dose

Initial: 4.5 mg/m² PO qDay

Adjust dose at 2 week intervals as needed to achieve and maintain trough concentrations of 5-15 ng/mL

Dosage modifications (SEGA)

  • Avoid strong CYP3A4 inducers if other therapy is available
  • If coadministration with strong CYP3A4 inducer required, double initial dose; base subsequent doses on serum concentration; readjust dose if strong CYP3A4 inducer is discontinued
  • Avoid strong CYP3A4 inhibitors
  • Coadministration with moderate CYP3A4 and/or PgP inhibitors: Reduce dose by 50%; administer every other day if dose reduction is required for patients receiving the lowest available strength and maintain trough concentrations of 5-15 ng/mL
  • Reduce dose or withhold for severe or intolerable adverse reactions; reduce dose by ~50%; if dose reduction required while receiving lowest available strength, administer every other day
  • Hepatic impairment
    • Mild-to-moderate (Child Pugh class A or B): Adjustment to the recommended starting dose may not be needed; however, subsequent dosing should be based on therapeutic drug monitoring
    • Severe (Child Pugh class C): Reduce dose by 50%; base subsequent doses on serum concentrations

Therapeutic drug monitoring (SEGA)

  • Monitor whole blood trough concentrations
  • Assess trough concentrations approximately 2 weeks after commencing treatment, a change in dose, a change in coadministration of CYP3A4 and/or PGP inducers or inhibitors, changes in hepatic function, or a change in dosage form between tablets and tablets for oral suspension
  • Once a stable dose is attained, monitor trough concentrations every 3-6 months in patients with changing body surface area or every 6-12 months in patients with stable body surface area for the duration of treatment
  • Titrate dose to attain trough concentration between 5-15 ng/mL
    • Trough concentrations <5 ng/mL: Increase daily dose by 2.5 mg (Afinitor) or 2 mg (Afinitor Disperz)
    • Trough Concentrations >15 ng/mL: Reduce daily dose by 2.5 mg (Afinitor) or 2 mg (Afinitor Disperz)
    • If dose reduction required for patients receiving the lowest available strength, administer every other day

Dosage considerations (SEGA)

  • Do not combine the 2 dosage forms (Afinitor and Afinitor Disperz) to achieve the desired dose; use 1 dosage form or the other

Kidney Transplant Rejection (Zortress)

Zortress: Indicated for prophylaxis of organ rejection in patients with low-moderate immunologic risk

Use in combination with reduced doses of cyclosporine, as well as basiliximab and corticosteroids

Starting dose: 0.75 mg PO q12hr initially; adjust maintenance dose to achieve trough whole blood concentrations of 3-8 ng/mL target range

Moderate hepatic impairment: Reduce daily dose by 50% and monitor blood concentrations

Administer as soon as possible after kidney transplantation

Liver Transplant Rejection (Zortress)

Zortress: Indicated for prophylaxis of allograft rejection in adult liver transplant recipients in combination with reduced doses of tacrolimus and with corticosteroids

Starting dose (30 days posttransplant): 1 mg PO q12hr initially; adjust maintenance dose to achieve trough whole blood concentrations of 3-5 ng/mL by 3 weeks after first dose of everolimus and through 12 months

Do not administer until at least 30 days post liver transplant (earlier administration associated with hepatic artery thrombosis, graft loss, and death)

Therapeutic Drug Monitoring (Zortress)

Optimally, dose adjustments should be based on trough concentrations obtained 4 or 5 days after a previous dosing change

Trough concentration <3 ng/mL: Double total dialy dose using the available tablet strenghts (ie, 0.25 mg, 0.5 mg, 0.75 mg)

Trough concentration >8 ng/mL on 2 consecutive measurement: Decrease dose by 0.25 mg BID

Orphan Indications (Orphan)

Diffuse large B-cell lymphoma

Gastric cancer

Waldenstrom macroglobulinemia (also known as lymphoplasmacytic lymphoma)

Orphan indication sponsor

  • Novartis Pharmaceuticals Corporation; One Health Plaza; East Hanover, NJ 07936-1080

Tuberous Sclerosis Topical Treatment (Orphan)

Everolimus ointment

Orphan designation for topical treatment of tuberous sclerosis

Sponsor

  • Aucta Pharmaceuticals, LLC; 675 US Highway One; North Brunswick, New Jersey 08902

Renal Impairment

No clinical studies were conducted in patients with decreased renal function

Renal impairment is not expected to result in dosage adjustment

Dosage Forms & Strengths

tablet (Afinitor)

  • 2.5mg
  • 5mg
  • 7.5mg
  • 10mg

tablet for oral suspension (Afintior Disperz)

  • 2mg
  • 3mg
  • 5mg

Subependymal Giant Cell Astrocytoma

Afinitor and Afinitor Disperz: Indicated for SEGA associated with tuberous sclerosis that cannot be treated with surgery

Initial dose based on body surface area with subsequent titration to attain trough concentrations of 5-15 ng/mL

4.5 mg/m² PO qDay

Dosage modifications (SEGA)

  • Avoid strong CYP3A4 inducers if other therapy is available
  • If coadministration with strong CYP3A4 inducer required, double initial dose to 9 mg/m² initially; base subsequent doses on serum concentration; adjust dose if strong CYP3A4 inducer is discontinued
  • Avoid strong CYP3A4 inhibitors
  • Coadministration with moderate CYP3A4 and/or PgP inhibitors: 2.5 mg/m² initially; base subsequent doses on serum concentration
  • Severe hepatic impairment (Child-Pugh class C): 2.5 mg/m² initially; base subsequent doses on serum concentration
  • Mild-to-moderate hepatic impairment: Adjustment to the recommended starting dose may not be needed; however, subsequent dosing should be based on therapeutic drug monitoring
  • Reduce dose or withhold for severe or intolerable adverse reactions; reduce dose by ~50%; if dose reduction required while receiving lowest available strength, administer every other day

Therapeutic drug monitoring (SEGA)

  • Monitor whole blood trough concentrations
  • Assess trough concentrations approximately 2 weeks after commencing treatment, a change in dose, a change in coadministration of CYP3A4 and/or PGP inducers or inhibitors, changes in hepatic function, or a change in dosage form between tablets and tablets for oral suspension
  • Once a stable dose is attained, monitor trough concentrations every 3-6 months in patients with changing body surface area or every 6-12 months in patients with stable body surface area for the duration of treatment
  • Titrate dose to attain trough concentration between 5-15 ng/mL
  • -Trough concentrations <5 ng/mL: Increase daily dose by 2.5 mg (Afinitor) or 2 mg (Afinitor Disperz)
  • -Trough Concentrations >15 ng/mL: Reduce daily dose by 2.5 mg (Afinitor) or 2 mg (Afinitor Disperz)
  • -If dose reduction required for patients receiving the lowest available strength, administer every other day

Dosage considerations (SEGA)

  • Do not combine the 2 dosage forms (Afinitor and Afinitor Disperz) to achieve the desired dose; use 1 dosage form or the other

In a randomized advanced hormone receptor positive, HER2-negative breast cancer study, no overall differences in safety or effectiveness were observed between these elderly patients and younger patients during clinical trials

Pregnancy & Lactation

Pregnancy

Based on animal studies and mechanism of action therapy can cause fetal harm when administered to pregnant woman; there are limited case reports of use in pregnant women; however, these reports are not sufficient to inform about risks of birth defects or miscarriage; advise pregnant women of potential risk to fetus

Contraception

  • Females
    • Advise female patients of reproductive potential to use effective contraception during treatment and for 8 weeks after last dose
  • Males
    • Based on findings in animal reproduction studies, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 4 weeks after last dose

Infertility

  • Females
    • Menstrual irregularities, secondary amenorrhea, and increases in luteinizing hormone (LH) and follicle stimulating hormone (FSH) occurred in female patients receiving therapy; based on these clinical findings and findings in animals, female fertility may be compromised by treatment with drug
  • Males
    • Based on clinical findings and findings in animals, treatment may impair fertility in male patients; cases of reversible azoospermia reported in male patients receiving therapy; in male rats, sperm motility, sperm count, plasma testosterone levels and fertility were diminished at exposures (AUC) similar to those in patients receiving a dose of 10 mg daily; the fertility index in rats increased when everolimus administration was stopped for a 10-13 week recovery

Lactation

There are no data on presence of everolimus in human milk, effects on breastfed infant or on milk production; drug and/or its metabolites passed into milk of lactating rats at a concentration 3.5 times higher than in maternal serum; because of potential for serious adverse reactions in breastfed infants from everolimus, advise lactating women not to breastfeed during treatment and for 2 weeks after last dose

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Usual Adult Dose for Pancreatic Cancer

10 mg orally once a day

Comments:
-Dose should be taken at the same time each day.
-Dose should be taken consistently with or without food.
-Afinitor (R) tablets should be swallowed whole with a glass of water and not chewed, broken, or crushed.

Uses:
AFINITOR(R):
1) Advanced Hormone Receptor-Positive, HER2-Negative Breast Cancer (Advanced HR+ BC):
-Treatment of postmenopausal women with advanced hormone receptor positive, HER2 negative breast cancer in combination with exemestane, after treatment with letrozole or anastrozole has failed.
2) Advanced Neuroendocrine Tumors (NET):
-Treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease.
-Treatment of adult patients with progressive, well-differentiated, nonfunctional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin with unresectable, locally advanced or metastatic disease.
3) Advanced Renal Cell Carcinoma (RCC):
-Treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib.
-Treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery.
4) Renal Angiomyolipoma with Tuberous Sclerosis Complex (TSC):
-Treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery.

Renal Dose Adjustments

No adjustment recommended

Description

AFINITOR (everolimus) and AFINITOR DISPERZ (everolimus tablets for oral suspension) are kinase inhibitors.

The chemical name of everolimus is (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18- dihydroxy-12-{(1R)-2-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]-1-methylethyl}-19,30-dimethoxy15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-aza-tricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20pentaone. The molecular formula is C53H83NO14 and the molecular weight is 958.2. The structural formula is:

AFINITOR for oral administration contains 2.5 mg, 5 mg, 7.5 mg, or 10 mg of everolimus and the following inactive ingredients: anhydrous lactose, butylated hydroxytoluene, crospovidone, hypromellose, lactose monohydrate, and magnesium stearate.

AFINITOR DISPERZ for oral administration contains 2 mg, 3 mg, or 5 mg of everolimus and the following inactive ingredients: butylated hydroxytoluene, colloidal silicon dioxide, crospovidone, hypromellose, lactose monohydrate, magnesium stearate, mannitol, and microcrystalline cellulose.

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