Zotarolimus(ABT-578)

For research use only. Not for therapeutic Use.

  • CAT Number: A000134
  • CAS Number: 221877-54-9
  • Molecular Formula: C52H79N5O12
  • Molecular Weight: 966.2
  • Purity: ≥95%
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Zotarolimus(cas 221877-54-9), also known as ABT-578, is a semi-synthetic macrocyclic lactone prepared from rapamycin by preparation of the 42-triflate ester, followed by displacement with tetrazole and purification of the two isomeric products. This structural change affords a less bioavailable product, a preferred profile for some applications. Zotarolimus is extensively cited in the literature with over 200 citations. Zotarolimus binds to a receptor protein (FKBP12). The complex then binds to mTOR preventing it from interacting with target proteins.


Catalog Number A000134
CAS Number 221877-54-9
Synonyms

Zotarolimus(ABT-578);A-179578; A 179578; A179578; ABT578; ABT-578; ABT 578; Endeavor; Zotarolimus

Molecular Formula C52H79N5O12
Purity ≥95%
Target FKBP12
Storage Store at -20°C
Overview of Clinical Research

Originator: Abbott Laboratories<br />
Developer: Medtronic<br />
Class: Ischaemic heart disorder therapies; Lactones; Macrolides; Polyenes; Tetrazoles<br />
Mechanism of Action: MTOR protein inhibitors<br />
Orphan Drug Status: No<br />

InChI CGTADGCBEXYWNE-JUKNQOCSSA-N
Reference

1. Circ Cardiovasc Interv. 2015 Apr;8(4). pii: e002223. doi:
10.1161/CIRCINTERVENTIONS.114.002223.
<br>
Safety and efficacy of resolute zotarolimus-eluting stents compared with
everolimus-eluting stents: a meta-analysis.
<br>
Piccolo R(1), Stefanini GG(1), Franzone A(1), Spitzer E(1), Bl&#246;chlinger S(1), Heg
D(1), Jüni P(1), Windecker S(2).
<br>
Author information: <br>
(1)From the Department of Cardiology, Bern University Hospital, Bern, Switzerland
(R.P., G.G.S., A.F., E.S., S.B., S.W.); and Clinical Trials Unit (D.H., P.J.,
S.W.), Institute of Social and Preventive Medicine (D.H.), Institute of Primary
Health Care (BIHAM) (P.J.), University of Bern, Bern, Switzerland.
(2)From the Department of Cardiology, Bern University Hospital, Bern, Switzerland
(R.P., G.G.S., A.F., E.S., S.B., S.W.); and Clinical Trials Unit (D.H., P.J.,
S.W.), Institute of Social and Preventive Medicine (D.H.), Institute of Primary
Health Care (BIHAM) (P.J.), University of Bern, Bern, Switzerland.
[email protected].
<br>
BACKGROUND: Although new-generation drug-eluting stents represent the standard of
care among patients undergoing percutaneous coronary intervention, there remains
debate about differences in efficacy and the risk of stent thrombosis between the
Resolute zotarolimus-eluting stent (R-ZES) and the everolimus-eluting stent
(EES). The aim of this study was to evaluate the safety and efficacy of the R-ZES
compared with EES in patients undergoing percutaneous coronary intervention.
METHODS AND RESULTS: A systematic literature search of electronic resources was
performed using specific search terms until September 2014. Random-effects
meta-analysis was performed comparing clinical outcomes between patients treated
with R-ZES and EES up to maximum available follow-up. The primary efficacy end
point was target-vessel revascularization. The primary safety end point was
definite or probable stent thrombosis. Secondary safety end points were cardiac
death and target-vessel myocardial infarction. Five trials were identified,
including a total of 9899 patients. Compared with EES, R-ZES had similar risks of
target-vessel revascularization (risk ratio [RR], 1.06; 95% confidence interval
[CI], 0.90-1.24; P=0.50), definite or probable stent thrombosis (RR, 1.26; 95%
CI, 0.86-1.85; P=0.24), cardiac death (RR, 1.01; 95% CI, 0.79-1.30; P=0.91), and
target-vessel myocardial infarction (RR, 1.10; 95% CI, 0.89-1.36; P=0.39).
Moreover, R-ZES and EES had similar risks of late definite or probable very late
stent thrombosis (RR, 1.06; 95% CI, 0.53-2.11; P=0.87). No evidence of
significant heterogeneity was observed across trials.<br>
CONCLUSIONS: R-ZES and EES provide similar safety and efficacy among patients
undergoing percutaneous coronary intervention.
<br>

2. J Interv Cardiol. 2013 Jun;26(3):278-86. doi: 10.1111/joic.12028. Epub 2013 Apr
22.
<br>
New-generation drug-eluting stents: focus on Xience V&#174; everolimus-eluting stent
and Resolute&#174; zotarolimus-eluting stent.
<br>
Van Dyck CJ(1), Hoymans VY, Haine S, Vrints CJ.
<br>
Author information: <br>
(1)Laboratory for Cellular and Molecular Cardiology, Department of Cardiology,
Antwerp University Hospital, Antwerp, Belgium.
<br>
Compared to bare metal stent angioplasty, first-generation drug-eluting stents
(DES) have markedly reduced the incidence of in-stent restenosis. However, given
the increased concerns over late and very late stent thrombosis, newer-generation
DES were developed. To date, these DES have virtually replaced the use of
first-generation DES worldwide. In this review article, we carefully consider the
pre-clinical and clinical trials that have been performed with currently
available, european conformity-marked and Food and Drug Administration-approved
new-generation Resolute(&#174;) and Xience V(&#174;) DES.
<br>

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