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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; continue 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 moderate CYP3A4/PgP inhibitors: reduce to 2.5mg once daily; may consider increasing to 5mg if tolerated. If moderate inhibitor is discontinued, allow 2–3 days washout period before increasing everolimus dose; return to dose used prior to initiating the moderate inhibitor. Concomitant strong CYP3A4/PgP inducers: avoid; if required, consider doubling the daily dose by increments of 5mg or less. If strong inducer is discontinued, consider washout period of 3–5 days before returning to the dose used prior to initiating the strong inducer. Dose modifications for adverse reactions, or others: see full labeling.

Children:

Not recommended.

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. 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 dose). Monitor CBCs, renal function, lipids, and blood glucose prior to starting and periodically thereafter. 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.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, amprenavir, fosamprenavir, aprepitant, erythromycin, fluconazole, verapamil, diltiazem); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital), St. John's Wort; avoid or increase dose (see Adult). Increased risk of angioedema with concomitant ACE inhibitor.

Pharmacological Class:

mTOR kinase inhibitor.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; decreased hemoglobin, WBC, platelets, lymphocytes, neutrophils, serum phosphate, potassium, albumin; increased cholesterol, blood glucose, AST, ALT, triglycerides, serum creatinine, proteinuria, renal failure.

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 (advanced HR+ BC) 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; continue 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 moderate CYP3A4/PgP inhibitors: reduce to 2.5mg once daily; may consider increasing to 5mg if tolerated. If moderate inhibitor is discontinued, allow 2–3 days washout period before increasing everolimus dose; return to dose used prior to initiating the moderate inhibitor. Concomitant strong CYP3A4/PgP inducers: avoid; if required, consider doubling the daily dose by increments of 5mg or less. If strong inducer is discontinued, consider washout period of 3–5 days before returning to the dose used prior to initiating the strong inducer. Dose modifications for adverse reactions, or others: see full labeling.

Children:

Not recommended.

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. 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 dose). Monitor CBCs, renal function, lipids, and blood glucose prior to starting and periodically thereafter. 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.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, amprenavir, fosamprenavir, aprepitant, erythromycin, fluconazole, verapamil, diltiazem); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital), St. John's Wort; avoid or increase dose (see Adult). Increased risk of angioedema with concomitant ACE inhibitor.

Pharmacological Class:

mTOR kinase inhibitor.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; decreased hemoglobin, WBC, platelets, lymphocytes, neutrophils, serum phosphate, potassium, albumin; increased cholesterol, blood glucose, AST, ALT, triglycerides, serum creatinine, proteinuria, renal failure.

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:

In adults and children with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected.

Adults and Children:

<1yr: not recommended. 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. ≥1yrs: initially 4.5mg/m2 once daily. Do not combine the 2 dosage forms 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 5–15ng/mL (see full labeling). Continue therapy until disease progression or unacceptable toxicity. Severe hepatic impairment: initiate at 2.5mg/m2 once daily. Concomitant strong CYP3A4/PgP inhibitors: avoid; moderate CYP3A4/PgP inhibitors: initiate at 2.5mg/m2 once daily, if CYP3A4/PgP inhibitor discontinued, after 2–3 days, return to dose used prior to initiating moderate inhibitor. Concomitant strong CYP3A4 inducers: avoid; if required, then initiate at 9mg/m2 once daily; if discontinued, then return to dose used prior to initiating strong inducer. Dose modifications for adverse reactions, or others: 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. 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 dose). Monitor CBCs, renal function, lipids, and blood glucose prior to starting and periodically thereafter. 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.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, amprenavir, fosamprenavir, aprepitant, erythromycin, fluconazole, verapamil, diltiazem); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital), St. John's Wort; avoid or increase dose (see Adult). Increased risk of angioedema with concomitant ACE inhibitor.

See Also:

AFINITOR DISPERZ

Pharmacological Class:

mTOR kinase inhibitor.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; decreased hemoglobin, WBC, platelets, lymphocytes, neutrophils, serum phosphate, potassium, albumin; increased cholesterol, blood glucose, AST, ALT, triglycerides, serum creatinine, proteinuria, renal failure.

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; continue 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 moderate CYP3A4/PgP inhibitors: reduce to 2.5mg once daily; may consider increasing to 5mg if tolerated. If moderate inhibitor is discontinued, allow 2–3 days washout period before increasing everolimus dose; return to dose used prior to initiating the moderate inhibitor. Concomitant strong CYP3A4/PgP inducers: avoid; if required, consider doubling the daily dose by increments of 5mg or less. If strong inducer is discontinued, consider washout period of 3–5 days before returning to the dose used prior to initiating the strong inducer. Dose modifications for adverse reactions, or others: see full labeling.

Children:

Not recommended.

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. 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 dose). Monitor CBCs, renal function, lipids, and blood glucose prior to starting and periodically thereafter. 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.

Interactions:

Avoid live vaccines. Potentiated by strong CYP3A4/PgP inhibitors (eg, ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole), grapefruit or grapefruit juice; avoid. Caution with moderate CYP3A4/PgP inhibitors (eg, amprenavir, fosamprenavir, aprepitant, erythromycin, fluconazole, verapamil, diltiazem); see Adult. Antagonized by strong CYP3A4/PgP inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital), St. John's Wort; avoid or increase dose (see Adult). Increased risk of angioedema with concomitant ACE inhibitor.

Pharmacological Class:

mTOR kinase inhibitor.

Adverse Reactions:

Stomatitis, infections, rash, fatigue, diarrhea, edema, abdominal pain, nausea, fever, asthenia, cough, headache, decreased appetite, RTI; decreased hemoglobin, WBC, platelets, lymphocytes, neutrophils, serum phosphate, potassium, albumin; increased cholesterol, blood glucose, AST, ALT, triglycerides, serum creatinine, proteinuria, renal failure.

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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