Generic Name and Formulations:
Everolimus 0.25mg, 0.5mg, 0.75mg; tabs.

Company:
Novartis Pharmaceuticals Corp
Indications for ZORTRESS:
Organ rejection prophylaxis in renal transplant patients with low-moderate immunologic risk, in combination with basiliximab induction and reduced doses of cyclosporine and corticosteroids. Organ rejection prophylaxis in liver transplant patients, in combination with reduced doses of tacrolimus and corticosteroids.

Adult:
Swallow whole. ≥18yrs: Renal transplant: administer as soon as possible after transplantation. Initially 0.75mg every 12 hours (1.5mg/day) in combination with reduced dose cyclosporine. Initiate oral prednisone as soon as oral medication is tolerated. Liver transplant: administer no earlier than 30 days post transplant. Initially 1mg every 12 hours (2mg/day) in combination with reduced dose tacrolimus. Both: steroid doses may be further tapered on an individualized basis. May adjust dose at 4–5 day intervals to achieve everolimus trough concentration target range 3–8ng/mL. Hepatic impairment: Mild: reduce initial daily dose by ⅓; Moderate or severe: reduce initial daily dose by ½.

Children:
<18yrs: not established.

Contraindications:
Sirolimus allergy.

Warnings/Precautions:
Increased risk of infections and possible malignancies (eg, lymphoma, skin); kidney graft thrombosis; nephrotoxicity; and mortality in heart transplantation. Use in heart transplantation: not recommended. High immunologic risk or prophylaxis in other organs: not established. Avoid sun, UV light. Severe hepatic impairment or hereditary disorders (eg, galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption): not recommended. Diabetes. Obtain everolimus, cyclosporine and tacrolimus whole blood concentrations periodically (see full labeling); and trough concentrations during dose adjustments. Monitor CBCs, renal function, urine protein, lipids, blood glucose; and for pneumonitis and serious (eg, bacterial, viral, fungal, protozoal) or opportunistic infections; polyoma virus infections (eg, BK virus-associated nephropathy, and JC virus-associated progressive multiple leukoencephalopathy). Pregnancy (Cat.C); use effective method of contraception during and up to 8 weeks after therapy. Nursing mothers: not recommended.

Interactions:
Avoid live vaccines, standard doses of cyclosporine. Increased risk of angioedema with ACE-inhibitors. Potentiated by CYP3A4 and/or P-glycoprotein inhibitors; avoid strong inhibitors (eg, ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, ritonavir, boceprevir, telaprevir, grapefruit juice, digoxin); monitor and adjust dose with moderate inhibitors (eg, erythromycin, fluconazole, nicardipine, diltiazem, nelfinavir, indinavir, amprenavir), or CYP3A4 and P-glycoprotein substrate (eg, verapamil). Antagonized by CYP3A4 inducers (eg, carbamazepine, phenobarbital, phenytoin, efavirenz, nevirapine, St. Johns Wort); avoid strong inducers (eg, rifampin, rifabutin). Avoid simvastatin, lovastatin; monitor if used with atorvastatin or pravastatin. Caution with other nephrotoxic drugs, CYP3A4 or CYP2D6 substrates with a narrow therapeutic index.

Pharmacological Class:
Immunosuppressant (macrolide).

Adverse Reactions:
Peripheral edema, nausea, diarrhea, constipation, hypertension, headache, pyrexia, abdominal pain, leukopenia, anemia, infections (eg, UTI), hyperlipidemia, angioedema, malignancies (eg, lymphomas, skin), proteinuria, nephrotoxicity, graft thrombosis, hepatic artery thrombosis, delayed wound healing/dehiscence, polyoma virus infections, non-infectious pneumonitis (reduce or interrupt dose and/or manage with corticosteroids), thrombotic microangiopathy, thrombotic thrombocytopenic purpura, hemolytic uremic syndrome, new-onset diabetes post-transplant, male infertility.

Metabolism:
Hepatic; 74% protein bound.

Elimination:
Fecal (primarily), renal.

Generic Availability:
NO

How Supplied:
Tabs—60 (10 x 6 blister strips)