November 13, 1999Journal of Medicinal ChemistryOpen Access

Potent, Orally Active GPIIb/IIIa Antagonists Containing a Nipecotic Acid Subunit. Structure−Activity Studies Leading to the Discovery of RWJ-53308

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Population

Preclinical models including dogs and guinea pigs, as well as in vitro assays for fibrinogen receptor…

Design

Preclinical

Authors

WHWilliam J. HoekstraUniversity of Minnesota BMBruce E. MaryanoffScripps Institution of Oceanography BDBruce P. DamianoJanssen (Belgium)

Discussion

Member takes

Implication

Supports progression to human trials of oral GPIIb/IIIa antagonists; leaves open clinical efficacy and safety.

Structured PICO

Population

Preclinical models including dogs and guinea pigs, as well as in vitro assays for fibrinogen receptor affinity and platelet aggregation.

Intervention

RWJ-53308, an orally active GPIIb/IIIa antagonist.

Outcome

Fibrinogen receptor affinity, inhibition of platelet aggregation, ex vivo antiplatelet activity, and in vivo antithrombotic efficacy.surrogate

RWJ-53308 is a novel, orally active GPIIb/IIIa antagonist with promising preclinical antiplatelet and antithrombotic efficacy, leading to its selection for clinical evaluation.

Cite This Study

Hoekstra et al. (1999) studied this question.

synapsesocial.com/papers/6a89a112851416c68bf7da2f https://doi.org/10.1021/jm990418b

Topics

Dual antiplatelet therapy

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Potent, Orally Active GPIIb/IIIa Antagonists Containing a Nipecotic Acid Subunit. Structure−Activity Studies Leading to the Discovery of RWJ-53308

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

Potent, Orally Active GPIIb/IIIa Antagonists Containing a Nipecotic Acid Subunit. Structure−Activity Studies Leading to the Discovery of RWJ-53308

Discussion

Member takes

Implication

Structured PICO

Cite This Study

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Topics

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