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RUC-4: a novel αIIbβ3 antagonist for prehospital therapy of myocardial infarction.
Li J, Vootukuri S, Shang Y, Negri A, Jiang JK, Nedelman M, Diacovo TG, Filizola M, Thomas CJ, Coller BS. Li J, et al. Arterioscler Thromb Vasc Biol. 2014 Oct;34(10):2321-9. doi: 10.1161/ATVBAHA.114.303724. Epub 2014 Aug 21. Arterioscler Thromb Vasc Biol. 2014. PMID: 25147334 Free PMC article.
Here, we report the properties of RUC-4 and the antiplatelet and antithrombotic effects of RUC-2 and RUC-4 in animal models. APPROACH AND RESULTS: RUC-4 was 20% more potent than RUC-2 in inhibiting human ADP-induced platelet …
Here, we report the properties of RUC-4 and the antiplatelet and antithrombotic effects of RUC-2 and RUC-4 …
Preclinical Studies of RUC-4, a Novel Platelet αIIbβ3 Antagonist, in Non-Human Primates and With Human Platelets.
Vootukuri S, Li J, Nedelman M, Thomas C, Jiang JK, Babayeva M, Coller BS. Vootukuri S, et al. J Clin Transl Sci. 2019 Jun;3(2-3):65-74. doi: 10.1017/cts.2019.382. Epub 2019 Jun 28. J Clin Transl Sci. 2019. PMID: 31544007 Free PMC article.
METHODS: We studied the: 1. pharmacokinetics (PK) of RUC-4 at 1.0, 1.93, and 3.86 mg/kg IV, IM, and SC in non-human primates (NHPs); 2. impact of aspirin on RUC-4 IC(50) in human platelet-rich plasma (PRP); 3. effect of different anticoagulants on the …
METHODS: We studied the: 1. pharmacokinetics (PK) of RUC-4 at 1.0, 1.93, and 3.86 mg/kg IV, IM, and SC in non-human primates ( …
First Human Use of RUC-4: A Nonactivating Second-Generation Small-Molecule Platelet Glycoprotein IIb/IIIa (Integrin αIIbβ3) Inhibitor Designed for Subcutaneous Point-of-Care Treatment of ST-Segment-Elevation Myocardial Infarction.
Kereiakes DJ, Henry TD, DeMaria AN, Bentur O, Carlson M, Seng Yue C, Martin LH, Midkiff J, Mueller M, Meek T, Garza D, Gibson CM, Coller BS. Kereiakes DJ, et al. J Am Heart Assoc. 2020 Sep;9(17):e016552. doi: 10.1161/JAHA.120.016552. Epub 2020 Aug 26. J Am Heart Assoc. 2020. PMID: 32844723 Free PMC article. Clinical Trial.
Inhibition of platelet aggregation (IPA) to ADP (20 mumol/L), RUC-4 blood levels, laboratory evaluations, and clinical assessments were made through 24 hours and at 7 days. ...RUC-4 blood levels correlated with IPA. Aspirin did not affect IPA or RUC …
Inhibition of platelet aggregation (IPA) to ADP (20 mumol/L), RUC-4 blood levels, laboratory evaluations, and clinical assessm …
Application of Auxiliary VerifyNow Point-of-Care Assays to Assess the Pharmacodynamics of RUC-4, a Novel αIIbβ3 Receptor Antagonist.
Bentur OS, Li J, Jiang CS, Martin LH, Kereiakes DJ, Coller BS. Bentur OS, et al. TH Open. 2021 Sep 28;5(3):e449-e460. doi: 10.1055/s-0041-1732343. eCollection 2021 Jul. TH Open. 2021. PMID: 34604694 Free PMC article.
RUC-4's antiplatelet effects were potentiated in citrate compared with PPACK. ...These pharmacodynamic assays can help guide the clinical development of RUC-4 and potentially be used to monitor RUC-4's effects in clinical practice....
RUC-4's antiplatelet effects were potentiated in citrate compared with PPACK. ...These pharmacodynamic assays can help guide t …
Pharmacokinetics, pharmacodynamics, and tolerability of subcutaneous administration of a novel glycoprotein IIb/IIIa inhibitor, RUC-4, in patients with ST-segment elevation myocardial infarction.
Bor WL, Zheng KL, Tavenier AH, Gibson CM, Granger CB, Bentur O, Lobatto R, Postma S, Coller BS, van 't Hof AWJ, Ten Berg JM. Bor WL, et al. EuroIntervention. 2021 Aug 6;17(5):e401-e410. doi: 10.4244/EIJ-D-21-00287. EuroIntervention. 2021. PMID: 34031019 Free PMC article. Clinical Trial.
AIMS: The open-label, phase 2A, CEL-02 trial aimed to assess the pharmacodynamics (PD), pharmacokinetics (PK), and tolerability of RUC-4 in STEMI patients undergoing primary PCI (pPCI). METHODS: A total of 27 STEMI patients received a weight-adjusted subcutaneous in …
AIMS: The open-label, phase 2A, CEL-02 trial aimed to assess the pharmacodynamics (PD), pharmacokinetics (PK), and tolerability of RUC …
Prehospital treatment with zalunfiban (RUC-4) in patients with ST- elevation myocardial infarction undergoing primary percutaneous coronary intervention: Rationale and design of the CELEBRATE trial.
Rikken SAOF, Selvarajah A, Hermanides RS, Coller BS, Gibson CM, Granger CB, Lapostolle F, Postma S, van de Wetering H, van Vliet RCW, Montalescot G, Ten Berg JM, van 't Hof AWJ; CELEBRATE investigators. Rikken SAOF, et al. Am Heart J. 2023 Apr;258:119-128. doi: 10.1016/j.ahj.2022.12.015. Epub 2022 Dec 31. Am Heart J. 2023. PMID: 36592878 Free article. Clinical Trial.
Rising like the phoenix?
Plow EF, Das M. Plow EF, et al. Arterioscler Thromb Vasc Biol. 2014 Oct;34(10):2182-3. doi: 10.1161/ATVBAHA.114.304486. Arterioscler Thromb Vasc Biol. 2014. PMID: 25231635 Free PMC article. No abstract available.