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QuickView for Everolimus (compound)

Name: everolimus
PubChem Compound ID: 6442177
Molecular formula: C53H83NO14
Molecular weight: 958.224 g/mol
RAD-001; SDZ-RAD; Certican; 42-O-(2-Hydroxy)ethyl rapamycin; 159351-69-6; RAD 001; Rapamycin, 42-O-(2-hydroxyethyl)-; RAD; (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-Dihydroxy-12-((1R)-2-((1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl)-1-methylethyl)-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo(,9)hexatriaconta-16,2; Everolimus [USAN].
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Name: everolimus
Name (isomeric): DB01590
Drug Type: small molecule
Brand: Certican
Category: Immunosuppressive Agents
CAS number: 159351-69-6
Indication: Investigated for use/treatment in transplant (rejection) and renal cell carcinoma.
Mechanism of Action:
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 a...
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Route of elimination: 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.
Drug interaction:
BicalutamideCYP3A4 Inhibitors like bicalutamide may increase the serum concentration of everolimus. Consider therapy modification. Recommendations regarding optimal management of this interaction vary according to specific indication and product used.
ItraconazoleItraconazole may increase everolimus levels/toxicity.
ErythromycinThe macrolide, erythromycin, may increase the serum concentration and toxicity of everolimus.
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Everolimus. Everolimus prescribing information recommends avoiding concurrent use with strong CYP3A4 inhbitors.
ClarithromycinThe macrolide, clarithromycin, may increase the serum concentration and toxicity of everolimus.
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