Tolerability and steady-state pharmacokinetics of everolimus in maintenance renal transplant patients

Abstract

These results indicate that up to 5 mg/day everolimus results in a dose-proportional exposure, and is adequately well tolerated in renal transplant recipients receiving cyclosporin and steroids.

Everolimus treatment for patients with autoimmune hepatitis and poor response to standard therapy and drug alternatives in use

“…It blocks the transduction signals of the T-cell response to alloantigen and this leads to mediation of the downstream inflammatory signaling. The adverse effects reported in the literature from the treatment of cancer patients and organ transplant patients include hypertriglyceridemia, hypercholesterolemia, leuco-, thrombo-and erythrocytopenia, infections including opportunistic infections, edema and gastrointestinal symptoms [41][42][43]. Less common is the development of toxic pneumonitis in 18% that may be severe, and the metabolic disturbances mentioned above that occur in 5% [44,45].…”

Sirolimus and everolimus in kidney transplantation

“…For everolimus, dose dependency has been shown for thrombocytopenia, but not for leukopenia. Hypertriglyceridemia and hypercholesterolemia were not dose dependent [47]. Aphthous stomatitis and diarrhea are also more frequently reported than in CNI and mycophenolic acid (MPA) regimens [48].…”

Pharmacokinetic analysis after implantation of everolimus-eluting self-expanding stents in the peripheral vasculature

“…12,18 Pharmacologically, everolimus has been shown to be safe and well-tolerated at systemic therapeutic concentrations between 3 and 15 ng/mL. [18][19][20] Approximately 98% of the drug is metabolized in the liver, so everolimus should be dosed cautiously in patients with hepatic dysfunction. 21 Pharmacodynamically, everolimus inhibits vascular smooth muscle cell proliferation, enhances vascular remodeling, 13,22,23 and has been shown to be safe and effective as the drug component of coronary DES.…”

“…Data points represent mean Ϯ standard error.were well-tolerated. In a longer-term study, Budde et al treated a similar patient population with oral everolimus in doses of 0.75 to 10 mg per day for 4 weeks and documented similar C max ranges of 22 to 169 ng/mL 19. Lastly, Kovarik et al followed 101 patients receiving daily everolimus in divided doses of 1 to 4 mg for a full year and documented steady state C max levels ranging from 5 to 22 ng/mL 20.…”