Molecular Weight(MW): 966.21
Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
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|Description||Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.|
|Features||Zotarolimus has a shorter in vivo half-life and is also demonstrated in rats to have less potent systemic immunosuppression than rapamycin.|
Zotarolimus (ABT-578) is a semi-synthetic analogue of rapamycin, made by substituting a tetrazole ring for the native hydroxyl group at position 42 in rapamycin. Zotarolimus is highly effective in inhibiting both smooth muscle cell and endothelial cell proliferation, with IC50 values of 2.9 nM and 2.6 nM, respectively.  Zotarolimus is mechanistically similar to sirolimus in having high-affinity binding to the immunophilin FKBP12 and comparable potency for inhibiting in vitro proliferation of both human and rat T cells. Zotarolimus inhibits Con A-induced human T cells and rat T cells proliferation with IC50 of 7.0 nM and 1337 nM respectively. 
|In vivo||Zotarolimus-eluting stents effectively reduce neointima formation in a 28-day, well-characterized swine model of coronary artery restenosis. Zotarolimus appears effective in preventing neointimal thickening, reducing late loss from 1.03 to 0.62 mm with a 47% reduction in TVF compared with bare metal stents (15.4% with the Driver stent to 8.1% with the Endeavor stent).  Zotarolimus is efficacious in suppressing adjuvant DTH, EAE, and cardiac allograft rejection with ED50 values of 1.72, 1.17, and 3.71 mg/kg/day, respectively. |
Binding Affinity to FKBP12:96-well microtiter plates are first coated with FKBP-12 CMP-KDO synthetase fusion protein at 10 μg/mL, 100 μL/well for 2-3 h, followed by addition of 50 μL/well of buffer A (2% BSA and 0.2% Tween-20 in D-PBS) for 30-60 min. Microtiter plates are then washed three times with buffer B (0.2% Tween in D-PBS, pH adjusted to 7.4). Fifty microlitres of buffer A (for maximum), 20 μM FK506 in buffer A (for background), or various concentrations of zotarolimus (10 pM-1 μM) in buffer A are added to each well followed by addition of 50 μL of A-79397 (an FK506 analogue)-alkaline phosphatase conjugate in buffer A. Microtiter plates are incubated at room temperature for 2-2.5 h followed by three washes with buffer B. About 100 μL of pNPP (p-nitrophenyl-phosphate) in 0.1 M aminomethylpropanol are added to each well and plates are incubated at room temperature for 90-120 min. Absorbance at 405 nM is read using an ELISA plate
|In vitro||DMSO||100 mg/mL (103.49 mM)|
|Ethanol||100 mg/mL (103.49 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02939976||Not yet recruiting||Myocardial Infarction||David Kong, M.D.|Medtronic Vascular|Volcano Corporation|Terumo Medical Corporation|Duke University||December 2016||--|
|NCT02770651||Recruiting||Coronary Artery Disease|Coronary Disease|Myocardial Ischemia|Arterial Occlusive Diseases|Arteriosclerosis|Cardiovascular Diseases|Heart Diseases|Vascular Diseases||Keimyung University Dongsan Medical Center||May 2016||--|
|NCT02452736||Completed||Ischemic Heart Disease|Cardiovascular Diseases|Arteriosclerosis|Coronary Artery Disease||Medtronic Vascular||May 2015||Phase 3|
|NCT02360423||Recruiting||Coronary Artery Disease||CID S.p.A.||November 2014||Phase 3|
|NCT02098876||Recruiting||Coronary Artery Disease||Emory University|Medtronic||May 2014||Phase 4|
|NCT01397175||Active, not recruiting||Coronary Artery Disease||Yonsei University|Gangwon Cardiovascular Health Research Institute||January 2013||Phase 4|
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