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Everolimus Dosage

Applies to the following strength(s): 0.5 mg ; 0.75 mg ; 0.25 mg ; 5 mg ; 10 mg ; 2.5 mg ; 7.5 mg ; 2 mg ; 3 mg

The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.

Usual Adult Dose for Breast 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.

Usual Adult Dose for Renal Cell Carcinoma

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.

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.

Usual Adult Dose for Renal Angiomyolipoma

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.

Usual Adult Dose for Neuroendocrine Carcinoma

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.

Usual Adult Dose for Brain/Intracranial Tumor

4.5 mg/m2 orally once a day

Duration of therapy: Continue until disease progression or unacceptable toxicity occurs. The optimal duration of therapy is unknown.

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.
-Do not combine AFINITOR (R) tablets and AFINITOR DISPERZ (R) to achieve the desired total dose.
-Use therapeutic drug monitoring to guide subsequent dosing.
-Adjust dose at 2 week intervals as needed to achieve and maintain trough concentrations of 5 to 15 ng/mL.

Use:
Afinitor(R) and Afinitor Disperz (R):
The treatment of adult and pediatric patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected

Usual Adult Dose for Organ Transplant - Rejection Prophylaxis

Kidney transplant: 0.75 mg orally twice a day

Comments:
-This drug should be administered in combination with reduced dose cyclosporine as soon as possible after transplantation.
-Oral prednisone should be initiated once oral medication is tolerated. Doses may be further individualized based on the clinical status of the patient and function of the graft.

Liver transplant: 1 mg orally twice a day

Comments:
-Start therapy at least 30 days after transplant.
-Use this drug in combination with reduced dose tacrolimus.
-Steroid doses may be individualized based on the clinical status of the patient and function of the graft.

Uses:
Zortress(R):
-Prophylaxis of organ rejection in adult patients at low-moderate immunologic risk receiving a kidney transplant and in combination with basiliximab induction and concurrently with reduced doses of cyclosporine and with corticosteroids.
-Prophylaxis of allograft rejection in adult patients receiving a liver transplant to be administered no earlier than 30 days post-transplant concurrently with reduced doses of tacrolimus and with corticosteroids.

Usual Pediatric Dose for Brain/Intracranial Tumor

4.5 mg/m2 orally once a day

Duration of therapy: Continue until disease progression or unacceptable toxicity occurs.

Use:
Afinitor(R) and Afinitor Disperz(R):
The treatment of adult and pediatric patients with subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC) who require therapeutic intervention but are not candidates for curative surgical resection.

Renal Dose Adjustments

No adjustment recommended

Liver Dose Adjustments

AFINITOR(R):
Breast Cancer, Renal Cell Carcinoma, Renal Angiomyolipoma, Pancreatic Cancer:
-Mild hepatic impairment (Child-Pugh class A): The recommended dose is 7.5 mg a day. The dose may be reduced to 5 mg a day if not well tolerated.
-Moderate hepatic impairment (Child-Pugh class B): The recommended dose is 5 mg a day. The dose may be decreased to 2.5 mg a day if not well tolerated.
-Severe hepatic impairment (Child-Pugh class C): If the desired benefit outweighs the risk, a dose of 2.5 mg a day may be used but must not be exceeded.

-Dose adjustments should occur if a patient's hepatic status changes during treatment.

Brain/Intracranial Tumors:
-Mild and moderate hepatic impairment (Child-Pugh class A and B): Dose adjustment may not be necessary.

-Severe hepatic impairment (Child-Pugh class C): 2.5 mg/m2 orally once a day; subsequent dosing should be based on therapeutic drug monitoring.
-Assess trough concentrations approximately 2 weeks after commencing treatment, a change in dose, or any change in hepatic function.

ZORTRESS(R):
Mild hepatic impairment (Child-Pugh class A): The initial daily dose should be reduced by one-third of the normally recommended initial dose.

Moderate hepatic impairment (Child-Pugh class B) or severe hepatic impairment (Child-Pugh class C): Initial daily dose should be reduced to one-half of the normally recommended initial dose.

Dose Adjustments

AFINITOR(R):
Breast Cancer, Renal Cell Carcinoma, Pancreatic Cancer, Renal Angiomyolipoma:
Non-infectious pneumonitis:
-Grade 1: No dose adjustment is recommended.
-Grade 2: Consider interruption of therapy, rule out infection and consider treatment with corticosteroids until symptoms improve to less than or equal to Grade 1. Re-initiate drug at 5 mg a day. Discontinue treatment if failure to recover within 4 weeks.
-Grade 3: Interrupt therapy until symptoms improve to less than or equal to Grade 1. Rule out infection and consider treatment with corticosteroids. Consider re-initiating at 5 mg a day and if Grade 3 toxicity occurs again, consider discontinuation.
-Grade 4: Discontinue therapy, rule out infection, and consider treatment with corticosteroids.

Stomatitis:
-Grade 1: No dose adjustment is recommended.
-Grade 2: Temporarily interrupt therapy until symptoms improve to less than or equal to Grade 1. Re-initiate the drug at the same dose. If stomatitis recurs at Grade 2, interrupt therapy until improvement to less than or equal to Grade 1 and re-initiate at 5 mg a day.
-Grade 3: Temporarily interrupt therapy until symptoms improve to less than or equal to Grade 1. Re-initiate the drug at 5 mg a day.
-Grade 4: Discontinue therapy and initiate appropriate medical treatment.

Other non-hematological toxicities:
-Grade 1: No dose adjustment is recommended.
-Grade 2: Only adjust dose if toxicity becomes intolerable. A temporary dose interruption is recommended until symptoms improve to less than or equal to Grade 1. Re-initiate the drug at the same dose. If toxicity recurs at Grade 2, interrupt therapy until recovery to less than or equal to Grade 1 and re-initiate at 5 mg a day.
-Grade 3: Temporarily interrupt therapy until recovery to less than or equal to Grade 1. Consider re-initiating this drug at 5 mg a day. If toxicity recurs at Grade 3, consider discontinuation.
-Grade 4: Discontinue therapy and initiate appropriate medical treatment.

Metabolic events:
-Grades 1 and 2: No dose adjustment is recommended.
-Grade 3: Temporarily interrupt therapy. Re-initiate the drug at 5 mg a day.
-Grade 4: Discontinue therapy and initiate appropriate medical treatment.

Concomitant use with moderate CYP450 3A4/P-gp inhibitors:
-If patients require concomitant use, reduce dose of this drug to 2.5 mg a day.
-The dose may be increased from 2.5 mg a day to 5 mg a day based on patient tolerance.
-If the moderate inhibitor is discontinued, a period of 2 to 3 days should pass before increasing the dose of everolimus.

Concomitant use with strong CYP450 3A4/P-gp inducers:
-If patients require concomitant use, consider doubling the daily dose of this drug using increments of 5 mg or less.
-If the strong inducer is discontinued, a period of 3 to 5 days should pass before decreasing the dose to the dose used prior to initiation of the strong inducer.

Brain/Intracranial Tumor:
Therapeutic drug monitoring:
-Monitor trough levels routinely in all patients.
-Assess trough concentrations approximately two weeks after initiation of treatment, a change in dose, a change in co-administration of CYP450 3A4/P-gp inducers and/or inhibitors, a change in hepatic function, or a change in dosage form from Afinitor(R) to Afinitor Disperz(R).
-Once a stable dose is attained, monitor trough levels every 3 to 6 months in patients with changing body surface area or every 6 to 12 months in patients with a stable body surface area.
-For trough concentrations less than 5 ng/mL, increase the daily dose by 2.5 mg (Afinitor tablets) or 2 mg (Afinitor Disperz).
-For trough concentrations greater than 15 ng/mL, reduce the daily dose by 2.5 mg (Afinitor tablets) or 2 mg (Afinitor Disperz).
-If dose reduction is required for patients taking the lowest available strength, administer every other day.

Adverse reactions:
-Temporarily interrupt or permanently discontinue therapy for severe or intolerable adverse reactions.
-If dose reduction is necessary, reduce the dose by 50% when re-initiating therapy.
-If dose reduction is necessary for patients receiving the lowest available strength, administer every other day.

CYP450 3A4/P-gp inhibitors:
-For patients receiving concomitant treatment with this drug and moderate CYP450 3A4/P-gp inhibitors: Initial dose: 2.5 mg/m2 orally once a day; maintenance dose: reduce by 50% or administer every other day for patients receiving the lowest available strength and maintain trough concentrations between 3 and 15 ng/mL.

-Assess the trough concentration approximately two weeks after dose reduction.
-After discontinuation of a moderate CYP450 3A4/P-gp inhibitor, resume the dose that was used prior to initiating the inhibitor after a period of 2 to 3 days. Assess the everolimus trough concentration approximately two weeks after.

CYP450 3A4/P-gp Inducers:
-For patients receiving concomitant treatment with this drug and strong CYP450 3A4/P-gp inducers: Initial dose: 9 mg/m2 orally once a day; maintenance dose: double the dose of this drug and assess tolerability.

-Assess the trough concentration approximately two weeks later and adjust the dose if necessary to maintain the concentration between 3 and 15 ng/mL.
-After discontinuation of a strong CYP450 450 3A4/P-gp inducer, resume the dose that was used prior to initiating the inducer and assess trough concentrations two weeks after.

Afinitor(R) therapeutic drug range: 3 to 15 ng/mL

Zortress(R) therapeutic drug range: 3 to 8 ng/mL

Precautions

US BOXED WARNINGS (Zortress(R)):
-MANAGEMENT OF IMMUNOSUPPRESSION: Only physicians experienced in immunosuppressive therapy and management of transplant patients should use Zortress(R).
-INFECTION AND MALIGNANCIES: Increased susceptibility to infection and the possible development of malignancies may result from immunosuppression.
-KIDNEY GRAFT THROMBOSIS: Increased incidence of kidney graft thrombosis.
-ZORTRESS AND CALCINEURIN INHIBITOR-INDUCED NEPHROTOXICITY: Reduced doses of cyclosporine are required for use in combination with Zortress(R) in order to reduce nephrotoxicity.
-HEART TRANSPLANTATION: Increased mortality in a heart transplant clinical trial. Use in heart transplantation is not recommended.

Safety and efficacy have not been established in patients younger than 1 year (Afinitor(R)).
Safety and efficacy have not been established in patients younger than 18 years (Zortress(R)).

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:
-Take consistently with or without food.
-Maintain consistency in time of administration.
-Afinitor(R) tablets should be taken with a full glass of water.
-Afinitor(R) tablets should not be broken or crushed.
-Do not combine the two dosage forms (Afinitor(R) tablets and Afinitor Disperz(R)) to achieve the desired total dose for patients with SEGA with TSC.
-If a dose is missed, continue normal dosing schedule. Do not take two doses to make up for missed dose.
-Zortress(R) should be taken 12 hours apart with or without food and at the same time as cyclosporine or tacrolimus.

Storage requirements:
-Store in original container away from light and moisture.

Reconstitution/preparation techniques:
Afinitor Disperz(R):
-Wear gloves to avoid possible contact with the drug when preparing suspensions for another person.
-Administer as a suspension only within 60 minutes of preparation. If not used within 60 minutes, discard suspension.
-Prepare suspension in water only.

For additional information, refer to manufacturer product information.

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