January 1, 2001Chemical and Pharmaceutical BulletinOpen Access

Novel Non-Peptide GPIIb/IIIa Antagonists. Synthesis and Biological Activities of 2-4-[2-(4-Amidinobenzoylamino)-2-(substituted)acetyl-3-(2-methoxy-2-oxoethyl)-2-oxopiperazinyl] acetic Acids.

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Why the study?

Does the novel GPIIb/IIIa antagonist 4h inhibit platelet aggregation more potently than TAK-029 in preclinical models?

Population

Guinea pig platelet rich plasma (PRP), human and monkey platelets, and guinea pigs (in vivo/ex vivo models)

Comparison

Compound 4h (a novel non-peptide GPIIb/IIIa… vs Compound 1 (TAK-029)

Design

Preclinical

Follow-up

up to 24 hours (ex vivo)

Authors

SKShuji KitamuraKeio University HFHideto FukushiThe Open University of Japan TMToshio MiyawakiTakeda (Japan)

Discussion

Member takes

Implication

Warrants progression to higher-species PK/safety studies; leaves open clinical translation or advantage over prior agents.

Structured PICO

Does the novel GPIIb/IIIa antagonist 4h inhibit platelet aggregation more potently than TAK-029 in preclinical models?

Population

Guinea pig platelet rich plasma (PRP), human and monkey platelets, and guinea pigs (in vivo/ex vivo models)

Intervention

Compound 4h (a novel non-peptide GPIIb/IIIa antagonist, (3S,2S)-4-methoxyphenylalanine derivative) administered orally (0.3-1.0 mg/kg) or intravenously (0.003-0.01 mg/kg)

Comparator

Compound 1 (TAK-029)

Outcome

Inhibition of in vitro adenosine 5'-diphosphate (ADP)-induced platelet aggregation (IC50)surrogate

The novel non-peptide GPIIb/IIIa antagonist 4h demonstrated potent in vitro and long-lasting ex vivo antiplatelet effects, suggesting potential suitability for once-daily oral dosing.

Cite This Study

Kitamura et al. (2001) studied this question.

synapsesocial.com/papers/6a85afe137bcb8373dadb5f7 https://doi.org/10.1248/cpb.49.258

Topics

Dual antiplatelet therapy

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Novel Non-Peptide GPIIb/IIIa Antagonists. Synthesis and Biological Activities of 2-4-[2-(4-Amidinobenzoylamino)-2-(substituted)acetyl-3-(2-methoxy-2-oxoethyl)-2-oxopiperazinyl] acetic Acids.

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

Novel Non-Peptide GPIIb/IIIa Antagonists. Synthesis and Biological Activities of 2-4-[2-(4-Amidinobenzoylamino)-2-(substituted)acetyl-3-(2-methoxy-2-oxoethyl)-2-oxopiperazinyl] acetic Acids.

Discussion

Member takes

Implication

Structured PICO

Cite This Study

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