Drug information of Everolimus

Everolimus

Drug group:

Everolimus lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader. The everolimus is used to prevent organ rejection after a kidney or liver transplant Everolimus is used together with cyclosporine, steroids, and other medications.

Mechanism of effect

Inhibitor of mammalian target of rapamycin (mTOR), which is a serine-threonine kinase. Everolimus binds to an intracellular protein, resulting in an inhibitory complex formation and inhibition of mTOR kinase activity.

Pharmacodynamic

Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake

Pharmacokinetics

T max is 1 to 2 h. C max and AUC are approximately 11.1 ng/mL and 75 + 31 ng•h/mL, respectively, for a 0.75 mg twice-daily dosage in renal transplant patients Protein binding is approximately 74%. Vd is 107 to 342 L. Everolimus is a substrate for CYP3A4 and P-glycoprotein (P-gp). Elimination half-life is approximately 30 h. Recovery in the feces and urine is 80% and 5%, respectively.

Dosage

Usual Adult Dose for Organ Transplant - Rejection Prophylaxis Kidney transplant: 0.75 mg orally twice a day Usual Adult Dose for Renal Cell Carcinoma 10 mg orally once a day Duration of therapy: Continue until disease progression or unacceptable toxicity occurs.

Alerts

1- Increased susceptibility to infection and the possible development of malignancies, such as lymphoma and skin cancer, may result from immunosuppression. 2- In renal transplant patients, use reduced doses of cyclosporine in combination with everolimus in order to reduce renal dysfunction. It is important to monitor the cyclosporine and everolimus whole blood trough concentrations 3- An increased risk of kidney arterial and venous thrombosis resulting in graft loss was reported, mostly within 30 days posttransplantation.

Points of recommendation

1- Administer at the same time each day, either consistently with or without food 2- Do not chew or crush tablets. 3- In patients receiving a renal transplant, initiate oral prednisone once oral medication is tolerated

Pregnancy level

D

Related drugs

Sirolimus


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