| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/description
| - Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein. (en)
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| http://linked.open...y/drugbank/dosage
| |
| http://linked.open...generalReferences
| - # Kuhn B, Jacobsen W, Christians U, Benet LZ, Kollman PA: Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem. 2001 Jun 7;44(12):2027-34. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11384247 # "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21047224 # "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22899246 # "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23455452 (en)
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| http://linked.open...gy/drugbank/group
| |
| http://linked.open...drugbank/halfLife
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| http://linked.open...ugbank/indication
| - Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole. Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease. Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Indicated in pediatric and adult patients with tuberous sclerosis complex (TSC) for the treatment of subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected. (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - 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. (en)
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| http://linked.open...drugbank/packager
| |
| http://linked.open...y/drugbank/patent
| |
| http://linked.open...outeOfElimination
| - After a single dose of radiolabeled everolimus was given to transplant patients receiving cyclosporine, the majority (80%) of radioactivity was recovered from the feces and only a minor amount (5%) was excreted in urine. (en)
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| http://linked.open.../drugbank/synonym
| - Certican (en)
- Afinitor (en)
- RAD001 (en)
- SDZ-RAD (en)
- VOTUBIA (en)
- Zortress (en)
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| http://linked.open...drugbank/toxicity
| |
| http://linked.open...umeOfDistribution
| - The blood-to-plasma ratio of everolimus is 17% to 73%. (en)
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| http://linked.open...nk/proteinBinding
| - ~ 74% in both healthy patients and those with moderate hepatic impairment. (en)
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| http://linked.open...ynthesisReference
| - # http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/001038/WC500022817.pdf (en)
|
| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - In patients with advanced solid tumors, peak everolimus concentrations are reached 1 to 2 hours after administration of oral doses ranging from 5 mg to 70 mg. Following single doses, Cmax is dose-proportional between 5 mg and 10 mg. At doses of 20 mg and higher, the increase in Cmax is less than dose-proportional, however AUC shows dose-proportionality over the 5 mg to 70 mg dose range. Steady-state was achieved within 2 weeks following once-daily dosing. Dose Proportionality in Patients with SEGA (subependymal giant-cell astrocytomas) and TSC (tuberous sclerosis complex): In patients with SEGA and TSC, everolimus Cmin was approximately dose-proportional within the dose range from 1.35 mg/m2 to 14.4 mg/m2. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...rugbank/clearance
| - Following a 3 mg radiolabeled dose of everolimus, 80% of the radioactivity was recovered from the feces, while 5% was excreted in the urine. (en)
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| http://linked.open...gbank/containedIn
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
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| http://linked.open...bank/Rule-of-Five
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| http://linked.open...tional-IUPAC-Name
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| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
| |
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