AFINITOR DISPERZ Rx
Generic Name and Formulations:
Everolimus 2mg, 3mg, 5mg; tabs for oral susp.
Novartis Pharmaceuticals Corp
Indications for AFINITOR DISPERZ:
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.
Allergy to other rapamycin derivatives.
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.
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.
mTOR kinase inhibitor.
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.
Hepatic (CYP3A4, 2D6), PgP.
Fecal, renal (minor).
Tabs, Disperz—28 (4 blister cards x 7 tabs)