For research use only.
CAS No. 221877-54-9
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)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01239654||Completed||Device: stent implantation||Acute Coronary Syndrome||IRCCS San Raffaele|Mediolanum Cardio Research|Cardiovascular Research Foundation New York||September 2010||Phase 3|
|NCT01003717||Completed||--||Coronary Artery Disease||Rebecca Torguson|Medstar Health Research Institute||October 2009||--|
|NCT00846846||Completed||Device: Endeavor® Zotarolimus Eluting Coronary Stent System||Coronary Artery Disease Autosomal Dominant 1||Medtronic Vascular||January 2009||Phase 4|
|NCT00815139||Completed||--||Coronary Artery Disease||Yonsei University||February 2008||--|
|NCT00599885||Completed||Drug: telmisartan|Drug: valsartan||Hypertension|Diabetes|Coronary Artery Disease||Korea University Anam Hospital||September 2007||Phase 4|
|NCT00476957||Completed||Device: Stent||Ischemic Heart Disease||Medtronic Vascular|Medtronic Bakken Research Center||June 2007||Phase 4|
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