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.[11]
This compound also has a use in cardiovascular drug-eluting stent technologies to inhibit restenosis.[medical citation needed]
It is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an inhibitor of mammalian target of rapamycin (mTOR).[12]
It is marketed by Novartis under the trade names Zortress (US) and Certican (European Union and other countries) in transplantation medicine, and as Afinitor (general tumours) and Votubia (tumours as a result of Tuberous Sclerosis Complex (TSC)) in oncology.[citation needed]
It is on the World Health Organization's List of Essential Medicines.[13] It is available as a generic medication.[14]
^Use During Pregnancy and Breastfeeding
^"FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
^"Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 30 March 2024.
^"Summary of Product Characteristics (SmPC) - (emc)". Certican Tablets. 15 January 2021. Retrieved 30 December 2021.
^"Afinitor- everolimus tablet Afinitor Disperz- everolimus tablet, for suspension". DailyMed. Retrieved 30 December 2021.
^"Zortress- everolimus tablet". DailyMed. Retrieved 30 December 2021.
^"Afinitor EPAR". European Medicines Agency. 17 September 2018. Retrieved 30 December 2021.
^"Votubia EPAR". European Medicines Agency. 17 September 2018. Retrieved 30 December 2021.
^Formica RN, Lorber KM, Friedman AL, Bia MJ, Lakkis F, Smith JD, Lorber MI (March 2004). "The evolving experience using everolimus in clinical transplantation". Transplantation Proceedings. 36 (2 Suppl): 495S–499S. doi:10.1016/j.transproceed.2004.01.015. PMID 15041395.
^Tedesco-Silva H, Saliba F, Barten MJ, De Simone P, Potena L, Gottlieb J, et al. (January 2022). "An overview of the efficacy and safety of everolimus in adult solid organ transplant recipients". Transplantation Reviews. 36 (1): 100655. doi:10.1016/j.trre.2021.100655. hdl:10230/53730. PMID 34696930. S2CID 239887236.
^Hasskarl J (2018). "Everolimus". Small Molecules in Oncology. Recent Results in Cancer Research. Vol. 211. pp. 101–123. doi:10.1007/978-3-319-91442-8_8. ISBN 978-3-319-91441-1. PMID 30069763. {{cite book}}: |journal= ignored (help)
^Hasskarl J (2018). "Everolimus". In Martens UM (ed.). Small Molecules in Oncology (Third ed.). Heidelberg: Springer. p. 101-124. ISBN 978-3-319-91442-8.
^World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
^"First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 15 November 2021. Retrieved 30 December 2021.
with everolimus.[medical citation needed] A phase IIa randomized, placebo-controlled everolimus clinical trial published in 2014 showed that everolimus improved...
responses were noted. Everolimus is the second novel Rapamycin analog. Compared with the parent compound rapamycin, everolimus is more selective for the...
immunoassay and latex agglutination turbidimetric immunoassay for evaluation of everolimus blood concentrations in renal transplant patients". Journal of Clinical...
carcinoma over everolimus in 2015 and was approved by the FDA. Cabozantinib also demonstrated an overall survival benefit over everolimus and was approved...
US Food and Drug Administration (FDA) approved it (in combination with everolimus) for the treatment of advanced renal cell carcinoma following one prior...
"Temporal trends in adverse events after everolimus-eluting bioresorbable vascular scaffold versus everolimus-eluting metallic stent implantation: A meta-analysis...
Everolimus also showed evidence of effectiveness at treating epilepsy in some people with TSC. In 2017, the European Commission approved everolimus for...
antibodies. It is also active against tumors that are PI3K/AKT/mTOR-dependent. Everolimus is an analog of sirolimus and also is an mTOR inhibitor. Zotarolimus is...
amenable to surgical removal and is causing symptoms, targeted therapy with everolimus or sunitinib can reduce symptoms and slow progression of the disease....
effective. In patients who continue to be refractory, mTOR inhibitors such as everolimus. The TPH inhibitor telotristat ethyl may be useful in controlling diarrhea...
PanNETs by the FDA based on improved progression-free survival (PFS): everolimus (Afinitor) is labeled for treatment of progressive neuroendocrine tumors...
transplantation and on detection of CAV. Medications including sirolimus and everolimus can slow disease progression. A repeat heart transplantation may be required...
to shrink or stabilize subependymal giant cell tumors: rapamycin and everolimus. These both belong to the mTOR inhibitor class of immunosuppressants,...
avoided through the use of alternate dosing regimens or analogs such as everolimus or temsirolimus. Lung toxicity is a serious complication associated with...
FDA-approved drug-eluting stents use sirolimus (also known as rapamycin), everolimus and zotarolimus. Biolimus A9-eluting stents, which utilize biodegradable...
mTOR inhibitors used in the treatment of human cancers, temsirolimus and everolimus. mTOR inhibitors have found use in the treatment of a variety of malignancies...
These other inhibitors include everolimus and temsirolimus. Compared with the parent compound rapamycin, everolimus is more selective for the mTORC1...
10% in strongly positive SRSS carcinoid tumors. Targeted therapy with everolimus (Afinitor) and sunitinib (Sutent) is approved by the FDA in unresectable...
was criticism of delays in deciding on a policy for the prescription of Everolimus in the treatment of tuberous sclerosis. Twenty doctors addressed a letter...
respond to a third sequential therapy as well. Adding an mTOR inhibitor, everolimus, can further slow the tumors' progression. Those with HER2-positive metastatic...
PN, Rini BI, Donskov F, et al. (November 2015). "Cabozantinib versus Everolimus in Advanced Renal-Cell Carcinoma". The New England Journal of Medicine...
high-resolution CT of the lung and pulmonary function testing.[citation needed] Everolimus is US Food and Drug Administration-approved for the treatment of angiomyolipomas...
trial of SGN-75 (INN: vorsetuzumab mafodotin) for use in combination with everolimus in patients with renal cell carcinoma 9 October: milestone achievement...
BEZ235/Dactolisib was administered in combination with the mTOR inhibitor Everolimus. The authors concluded that the combination of both drugs demonstrated...
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