Everolimus

Everolimus, sold under the brand name Afinitor among others, is a medication used as an immunosuppressant to prevent rejection of organ transplants[10] and as a targeted therapy in the treatment of renal cell cancer and other tumours.[28] A phase IIa randomized, placebo-controlled clinical trial published in 2018 showed that everolimus in combination with dactolisib decreased the rate of reported infections in an elderly population.mTORC1 inhibition by everolimus has been shown to normalize tumor blood vessels, to increase tumor-infiltrating lymphocytes, and to improve adoptive cell transfer therapy.As a consequence, mRNAs that code for proteins implicated in the cell cycle and in the glycolysis process are impaired or altered, and tumor growth is inhibited.The most common adverse reactions (incidence greater than or equal to 30%) were stomatitis, infections, diarrhea, peripheral edema, fatigue and rash.The most common blood abnormalities found (incidence greater than or equal to 50%) were anemia, hypercholesterolemia, lymphopenia, elevated aspartate transaminase (AST) and fasting hyperglycemia.".[35] A positive impact on hepatocellular carcinoma (HCC) was observed when everolimus was used as primary immunosuppression starting as early as first week after living donor liver transplantation (LDLT) surgery.Everolimus was used in a clinical trial by Novartis, and short-term treatment was shown to enhance the response to the influenza vaccine in the elderly, possible by reversing immunosenescence.
Drugs.comMedlinePlusLicense dataDailyMedPregnancycategoryRoutes ofadministrationBy mouthATC codeL01EG02L04AH02Legal statusWARNINGPharmacokineticElimination half-lifeIUPAC nameCAS NumberDrugBankChemSpiderChEMBLCompTox DashboardECHA InfoCardFormulaMolar massSMILESmedicationimmunosuppressantrejectionorgan transplantstargeted therapydrug-eluting stentrestenosissirolimusmammalian target of rapamycinNovartisTuberous Sclerosis ComplexWorld Health Organization's List of Essential Medicinesgeneric medicationSubependymal giant cell astrocytoma (SEGA)tuberous sclerosis (TS)pancreatic neuroendocrine tumorsexemestaneneuroendocrine tumorsNHS EnglandTuberous Sclerosisgastric cancerhepatocellular carcinomalymphomachronic graft-versus-host diseaseprogression-free survivalinfluenza vaccinedactolisibrapamycinmTORC1mTORC2negative feedbacktumor-infiltrating lymphocytesadoptive cell transfer therapyglucose intoleranceimmunosuppressionFKBP12chronic allograft vasculopathydrug-eluting coronary 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