June 1, 1995Journal of Medicinal ChemistryOpen Access

Potent in Vitro and in Vivo Inhibitors of Platelet Aggregation Based Upon the Arg-Gly-Asp Sequence of Fibrinogen. (Aminobenzamidino)succinyl (ABAS) Series of Orally Active Fibrinogen Receptor Antagonists

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Population

Canine models and dog platelet-rich plasma

Comparison

succinyl series of orally active fibrinogen… vs Benzamidinopentanoyl series and intravenous…

Design

Preclinical

Authors

JZJeffery A. Zablocki JRJoseph G. RicoPfizer (United States)RGRobert B. GarlandBiogen (United States)

Discussion

Member takes

Implication

Provides preclinical support for ABAS fibrinogen antagonists; leaves open translation of potency and bioavailability to human antiplatelet therapy.

Structured PICO

Population

Canine models and dog platelet-rich plasma

Intervention

(Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists (specifically ester prodrug/acid active metabolite pairs such as 2e/2a)

Comparator

Benzamidinopentanoyl (BAP) series and intravenous administration of the same compounds

Outcome

Inhibition of collagen-induced platelet aggregation (IC50), elimination half-life (t1/2 beta-phase), and oral systemic availabilitysurrogate

The ABAS series of fibrinogen receptor antagonists, particularly compound 2e/2a, demonstrates potent in vitro antiplatelet activity and favorable oral bioavailability in canine models.

Cite This Study

Zablocki et al. (1995) studied this question.

synapsesocial.com/papers/6a90ee55647f40dea9c1a862 https://doi.org/10.1021/jm00013a014

Topics

Dual antiplatelet therapy

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Implication

Provides preclinical support for ABAS fibrinogen antagonists; leaves open translation of potency and bioavailability to human antiplatelet therapy.

Potent in Vitro and in Vivo Inhibitors of Platelet Aggregation Based Upon the Arg-Gly-Asp Sequence of Fibrinogen. (Aminobenzamidino)succinyl (ABAS) Series of Orally Active Fibrinogen Receptor Antagonists

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

Potent in Vitro and in Vivo Inhibitors of Platelet Aggregation Based Upon the Arg-Gly-Asp Sequence of Fibrinogen. (Aminobenzamidino)succinyl (ABAS) Series of Orally Active Fibrinogen Receptor Antagonists

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Topics

Also Consider