Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress and Afinitorm is an mTOR inhibitor with IC50 of 0.63 nM. Everolimus is an immunosuppressant analog of rapamycin (sirolimus) and inhibits growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells. Everolimus shows a potent inhibitory effect on posttransplant lymphoproliferative disorder (PTLD)-derived cells in vitro and in vivo.
|Cell lines||NCI-N87 and MKN45 cells|
|Preparation method||Proliferation assay. Gastric cancer cells (10,000 cells re-suspended in 1 ml medium) were seeded in 24-well plates. 24 h after seeding,0.5 ml medium containing RAD001 was added to yield desired concentrations of RAD001. At the time points indicated, gastric cancer cells were harvested and counted with a Coulter Z1 electronic cell counter (Beckman Coulter, UK).|
|Concentrations||2.5–160 n M|
|Incubation time||72 h|
|Animal models||NCI-N87 Tumor xenograft model with Pathogen-free, 4–6 week old, female CB-17 SCID mice|
|Dosages||5 mg/kg qd for 121 days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||Breast Cancer Res Treat (2015). Figure 2. Everolimus|
|Cell Lines||KPL-1 cell|
|Incubation Time||5 d|
|Results||Cells were exposed to everolimus at 10 nM for 5 days, and then flow cytometry was performed using Nim- DAPI staining. G0/G1 cell cycle arrest was observed in the two sensitive and the one intermediate cell line tested but was not observed in resistant lines|
|Source||Breast Cancer Res Treat (2015). Figure 1. Everolimus|
|Cell Lines||KPL-1 cell|
|Incubation Time||10 min–48 h|
|Results||We observed a significant inhibition of S6 phosphorylation in all tested cell lines after 30 min exposure to everolimus regardless of sensitivity to growth inhibitory effects.|
Everolimus and enteric-coated mycophenolate sodium ab initio after liver transplantation: midterm results.
Manzia et al. Transplant Proc. 2012 Sep;44(7):1942-5. PMID: 22974878.
Conversion from calcineurin inhibitors to everolimus with low-dose cyclosporine in renal transplant recipients with squamous cell carcinoma of the skin.
Caroti et al. Transplant Proc. 2012 Sep;44(7):1926-7. PMID: 22974873.
Everolimus and Erlotinib as Second- or Third-Line Therapy in Patients with Advanced Non-Small-Cell Lung Cancer.
Papadimitrakopoulou et al. J Thorac Oncol. 2012 Sep 10. PMID: 22968184.
Comparison of Outcomes in Patients With Versus Without Diabetes Mellitus After Revascularization With Everolimus- and Sirolimus-Eluting Stents (from the SORT OUT IV Trial).
Jensen et al. Am J Cardiol. 2012 Sep 4. PMID: 22959714.
Virtual Histology Assessment of Cardiac Allograft Vasculopathy Following Introduction of Everolimus-Results of a Multicenter Trial.
Arora et al. Am J Transplant. 2012 Sep 7. PMID: 22958738.
Mid-Term Results of Everolimus-Eluting Stent in a Japanese Population Compared With a US Randomized Cohort: SPIRIT III Japan Registry With Harmonization by Doing.
Saito et al. J Invasive Cardiol. 2012 Sep;24(9):444-50. PMID: 22954564.
A drug safety evaluation of everolimus in kidney transplantation.
Holdaas et al. Expert Opin Drug Saf. 2012 Sep 6. PMID: 22954349.
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