FDA approved Zortress (everolimus) for Organ Rejection Prophylaxis in Kidney and Liver TransplantFDA approved Zortress to help prevent organ rejection after kidney or liver transplant

Zortress is an mTOR inhibitor immunosuppressant. The exact mechanism is not fully described in the label, but it is classified as an mTOR inhibitor.

Zortress is indicated for the prophylaxis of organ rejection in adult patients: 1) Kidney transplant: at low to moderate immunologic risk, in combination with basiliximab, cyclosporine (reduced doses), and corticosteroids. 2) Liver transplant: administer no earlier than 30 days posttransplant, in combination with tacrolimus (reduced doses) and corticosteroids. Limitations of Use: Safety and efficacy have not been established in kidney transplant patients at high immunologic risk, recipients of transplanted organs other than kidney or liver, or pediatric patients (less than 18 years).

Kidney transplantation: starting oral dose of 0.75 mg twice daily as soon as possible after transplantation. Liver transplantation: starting oral dose of 1 mg twice daily starting 30 days after transplantation. Monitor everolimus concentrations: adjust maintenance dose to achieve trough concentrations within the 3 to 8 ng/mL target range using LC/MS/MS assay method. Administer consistently with or without food at the same time as cyclosporine or tacrolimus. Mild hepatic impairment: reduce initial daily dose by one-third. Moderate or severe hepatic impairment: reduce initial daily dose by one-half. Dose adjustment is required if trough concentration is below 3 ng/mL: double the total daily dose using available tablet strengths (0.25 mg, 0.5 mg, 0.75 mg, or 1 mg). Dose adjustment is also required if trough concentration is greater than 8 ng/mL on 2 consecutive measures: decrease dose by 0.25 mg twice daily. Optimally, dose adjustments should be based on trough concentrations obtained 4 or 5 days after a previous dosing change.

Trial data not available in label.

Contraindications are not specified in the provided label text. Warnings and Precautions include: safety and efficacy not established in recipients of transplanted organs other than kidney or liver (5.7); liver transplant: administer no earlier than 30 days posttransplant (5.5). The label also notes the importance of monitoring everolimus blood concentrations in patients with hepatic impairment, during concomitant administration of CYP3A4 inducers or inhibitors or cannabidiol, when switching cyclosporine formulations and/or when cyclosporine dosing is reduced. There is an interaction of cyclosporine on everolimus; everolimus concentrations may decrease if cyclosporine exposure is reduced. There is little to no pharmacokinetic interaction of tacrolimus on everolimus.

Zortress is an mTOR inhibitor immunosuppressant approved for prophylaxis of organ rejection in adult kidney transplant patients at low to moderate immunologic risk and in adult liver transplant patients. It is used in combination with other immunosuppressants: basiliximab, reduced-dose cyclosporine, and corticosteroids for kidney transplant; reduced-dose tacrolimus and corticosteroids for liver transplant. Therapeutic drug monitoring of everolimus and the concomitant calcineurin inhibitor is recommended for all patients. Safety and efficacy have not been established in high immunologic risk kidney transplant patients, recipients of other organs, or pediatric patients.