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AFINITOR
Bladder, kidney, and other urologic cancers
Breast cancer
CNS cancers
Pancreatic, thyroid, and other endocrine cancers
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Drug Name:

AFINITOR Rx

Generic Name and Formulations:
Everolimus 2.5mg, 5mg, 7.5mg, 10mg; tabs.

Company:
Novartis Pharmaceuticals Corp

Therapeutic Use:

Indications for AFINITOR:

In adults with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. In adults with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery.

Adult:

Swallow tabs whole with water. Take at the same time each day either consistently with or without food. 10mg once daily until disease progression or unacceptable toxicity. Mild hepatic impairment (Child-Pugh class A): 7.5mg daily, may reduce to 5mg if not tolerated. Moderate hepatic impairment (Child-Pugh class B): 5mg daily, may be reduce to 2.5mg if not tolerated. Severe hepatic impairment (Child-Pugh class C): max 2.5mg daily if benefits outweigh risks. Concomitant CYP3A4/PgP inhibitors (strong): avoid; (moderate): reduce to 2.5mg once daily, may consider increasing to 5mg if tolerated; if moderate inhibitor is discontinued, after 3 days, resume at dose prior to initiating inhibitor. Concomitant strong CYP3A4/PgP inducers: avoid; if required, double daily dose by increments of 5mg or less; if strong inducer is discontinued, after 5 days, resume at dose prior to initiating inducer. Dose modifications for adverse reactions, or others: see full labeling.

Children:

Not established.

Contraindications:

Allergy to other rapamycin derivatives.

Warnings/Precautions:

Monitor for new or worsening respiratory symptoms; discontinue, reduce dose, and/or manage with corticosteroids if non-infectious pneumonitis occurs. Increased risk of infections (may be severe or fatal); monitor and treat promptly if occur. Pre-existing invasive fungal infections: treat before starting. Give PJP prophylaxis with concomitant corticosteroids or other immunosuppressants. Use dexamethasone mouthwash at initiation to reduce the incidence and severity of stomatitis; use alcohol-, peroxide-, iodine-, or thyme-free products if occurs. Monitor for signs of wound-related complications. Peri-surgical period. Hepatic impairment (see Adult). Diabetes. Monitor CBCs, renal function, lipids, and blood glucose prior to starting and annually thereafter (more frequently if clinically indicated). Avoid close contact with those who have received live vaccines. Pediatrics: complete childhood vaccination series according to ACIP guidelines prior to initiation. Elderly. Embryo-fetal toxicity. Must use effective contraception during and for 8 weeks (females) or 4 weeks (males) after last dose. Pregnancy, nursing mothers: not recommended.

Pharmacological Class:

mTOR kinase inhibitor.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, erythromycin, verapamil); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, rifampin); see Adult. Avoid St. John's Wort. Increased risk of angioedema with concomitant ACEI; avoid.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; non-infectious pneumonitis, impaired wound healing, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, myelosuppression, renal failure, angioedema or severe hypersensitivity reactions (discontinue if occur).

Metabolism:

Hepatic (CYP3A4, 2D6), PgP.

Elimination:

Fecal, renal (minor).

Generic Availability:

NO

How Supplied:

Tabs—28 (4 blister cards x 7 tabs)

Indications for AFINITOR:

Postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole.

Adult:

Swallow tabs whole with water. Take at the same time each day either consistently with or without food. 10mg once daily until disease progression or unacceptable toxicity. Mild hepatic impairment (Child-Pugh class A): 7.5mg daily, may reduce to 5mg if not tolerated. Moderate hepatic impairment (Child-Pugh class B): 5mg daily, may be reduce to 2.5mg if not tolerated. Severe hepatic impairment (Child-Pugh class C): max 2.5mg daily if benefits outweigh risks. Concomitant CYP3A4/PgP inhibitors (strong): avoid; (moderate): reduce to 2.5mg once daily, may consider increasing to 5mg if tolerated; if moderate inhibitor is discontinued, after 3 days, resume at dose prior to initiating inhibitor. Concomitant strong CYP3A4/PgP inducers: avoid; if required, double daily dose by increments of 5mg or less; if strong inducer is discontinued, after 5 days, resume at dose prior to initiating inducer. Dose modifications for adverse reactions, or others: see full labeling.

Children:

Not established.

Contraindications:

Allergy to other rapamycin derivatives.

Warnings/Precautions:

Monitor for new or worsening respiratory symptoms; discontinue, reduce dose, and/or manage with corticosteroids if non-infectious pneumonitis occurs. Increased risk of infections (may be severe or fatal); monitor and treat promptly if occur. Pre-existing invasive fungal infections: treat before starting. Give PJP prophylaxis with concomitant corticosteroids or other immunosuppressants. Use dexamethasone mouthwash at initiation to reduce the incidence and severity of stomatitis; use alcohol-, peroxide-, iodine-, or thyme-free products if occurs. Monitor for signs of wound-related complications. Peri-surgical period. Hepatic impairment (see Adult). Diabetes. Monitor CBCs, renal function, lipids, and blood glucose prior to starting and annually thereafter (more frequently if clinically indicated). Avoid close contact with those who have received live vaccines. Pediatrics: complete childhood vaccination series according to ACIP guidelines prior to initiation. Elderly. Embryo-fetal toxicity. Must use effective contraception during and for 8 weeks (females) or 4 weeks (males) after last dose. Pregnancy, nursing mothers: not recommended.

Pharmacological Class:

mTOR kinase inhibitor.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, erythromycin, verapamil); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, rifampin); see Adult. Avoid St. John's Wort. Increased risk of angioedema with concomitant ACEI; avoid.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; non-infectious pneumonitis, impaired wound healing, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, myelosuppression, renal failure, angioedema or severe hypersensitivity reactions (discontinue if occur).

Metabolism:

Hepatic (CYP3A4, 2D6), PgP.

Elimination:

Fecal, renal (minor).

Generic Availability:

NO

How Supplied:

Tabs—28 (4 blister cards x 7 tabs)

Indications for AFINITOR:

Patients ≥1yr with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected. Adjunct treatment of patients ≥2yrs with TSC-associated partial-onset seizures.

Adults and Children:

Do not combine the 2 dosage forms to achieve the desired total dose. Swallow tabs whole with water or use Disperz tabs administered as a suspension only. Take at the same time each day either consistently with or without food. Prepare suspension using 5mL of water in an oral syringe or 25mL of water in a drinking glass; max 10mg dose per syringe or glass. Use therapeutic drug monitoring to guide subsequent dosing. Adjust dose at 1–2 week intervals as needed to achieve and maintain trough concentrations of 5–15ng/mL; max 5mg increment per titration (see full labeling). Continue until disease progression or unacceptable toxicity. SEGA: <1yr: not established. ≥1yr: initially 4.5mg/m2 once daily. Partial-onset seizures: <2yrs: not established. ≥2yrs: initially 5mg/m2 once daily. Severe hepatic impairment: initiate at 2.5mg/m2 once daily. Concomitant CYP3A4/PgP inhibitors (strong): avoid; (moderate): reduce daily dose by 50% (or change to every other day if reduced dose unavailable in tab strength); if moderate inhibitor is discontinued, after 3 days, resume dose used prior to initiating inhibitor. Concomitant strong CYP3A4/PgP inducers: double daily dose by increments of 5mg or less; if strong inducer is discontinued, after 5 days, resume dose used prior to initiating inducer. Dose modifications for adverse reactions: see full labeling.

Contraindications:

Allergy to other rapamycin derivatives.

Warnings/Precautions:

Monitor for new or worsening respiratory symptoms; discontinue, reduce dose, and/or manage with corticosteroids if non-infectious pneumonitis occurs. Increased risk of infections (may be severe or fatal); monitor and treat promptly if occur. Pre-existing invasive fungal infections: treat before starting. Give PJP prophylaxis with concomitant corticosteroids or other immunosuppressants. Use dexamethasone mouthwash at initiation to reduce the incidence and severity of stomatitis; use alcohol-, peroxide-, iodine-, or thyme-free products if occurs. Monitor for signs of wound-related complications. Peri-surgical period. Hepatic impairment (see Adult). Diabetes. Monitor CBCs, renal function, lipids, and blood glucose prior to starting and annually thereafter (more frequently if clinically indicated). Avoid close contact with those who have received live vaccines. Pediatrics: complete childhood vaccination series according to ACIP guidelines prior to initiation. Elderly. Embryo-fetal toxicity. Must use effective contraception during and for 8 weeks (females) or 4 weeks (males) after last dose. Pregnancy, nursing mothers: not recommended.

See Also:

AFINITOR DISPERZ

Pharmacological Class:

mTOR kinase inhibitor.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, erythromycin, verapamil); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, rifampin); see Adult. Avoid St. John's Wort. Increased risk of angioedema with concomitant ACEI; avoid.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; non-infectious pneumonitis, impaired wound healing, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, myelosuppression, renal failure, angioedema or severe hypersensitivity reactions (discontinue if occur).

Metabolism:

Hepatic (CYP3A4, 2D6), PgP.

Elimination:

Fecal, renal (minor).

Generic Availability:

NO

How Supplied:

Tabs, Disperz—28 (4 blister cards x 7 tabs)

Indications for AFINITOR:

In adults with progressive neuroendocrine tumors of pancreatic origin (PNET) or progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal or lung origin with unresectable, locally advanced or metastatic disease. Not for treating functional carcinoid tumors.

Adult:

Swallow tabs whole with water. Take at the same time each day either consistently with or without food. 10mg once daily until disease progression or unacceptable toxicity. Mild hepatic impairment (Child-Pugh class A): 7.5mg daily, may reduce to 5mg if not tolerated. Moderate hepatic impairment (Child-Pugh class B): 5mg daily, may be reduce to 2.5mg if not tolerated. Severe hepatic impairment (Child-Pugh class C): max 2.5mg daily if benefits outweigh risks. Concomitant CYP3A4/PgP inhibitors (strong): avoid; (moderate): reduce to 2.5mg once daily, may consider increasing to 5mg if tolerated; if moderate inhibitor is discontinued, after 3 days, resume at dose prior to initiating inhibitor. Concomitant strong CYP3A4/PgP inducers: avoid; if required, double daily dose by increments of 5mg or less; if strong inducer is discontinued, after 5 days, resume at dose prior to initiating inducer. Dose modifications for adverse reactions, or others: see full labeling.

Children:

Not established.

Contraindications:

Allergy to other rapamycin derivatives.

Warnings/Precautions:

Monitor for new or worsening respiratory symptoms; discontinue, reduce dose, and/or manage with corticosteroids if non-infectious pneumonitis occurs. Increased risk of infections (may be severe or fatal); monitor and treat promptly if occur. Pre-existing invasive fungal infections: treat before starting. Give PJP prophylaxis with concomitant corticosteroids or other immunosuppressants. Use dexamethasone mouthwash at initiation to reduce the incidence and severity of stomatitis; use alcohol-, peroxide-, iodine-, or thyme-free products if occurs. Monitor for signs of wound-related complications. Peri-surgical period. Hepatic impairment (see Adult). Diabetes. Monitor CBCs, renal function, lipids, and blood glucose prior to starting and annually thereafter (more frequently if clinically indicated). Avoid close contact with those who have received live vaccines. Pediatrics: complete childhood vaccination series according to ACIP guidelines prior to initiation. Elderly. Embryo-fetal toxicity. Must use effective contraception during and for 8 weeks (females) or 4 weeks (males) after last dose. Pregnancy, nursing mothers: not recommended.

Pharmacological Class:

mTOR kinase inhibitor.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, erythromycin, verapamil); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, rifampin); see Adult. Avoid St. John's Wort. Increased risk of angioedema with concomitant ACEI; avoid.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; non-infectious pneumonitis, impaired wound healing, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, myelosuppression, renal failure, angioedema or severe hypersensitivity reactions (discontinue if occur).

Metabolism:

Hepatic (CYP3A4, 2D6), PgP.

Elimination:

Fecal, renal (minor).

Generic Availability:

NO

How Supplied:

Tabs—28 (4 blister cards x 7 tabs)

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