What is the clinical evidence from this study?

Study design: Other. Population: Thrombosis. Intervention: SAR216471 vs. clopidogrel. Primary outcome: ADP-induced platelet aggregation.

July 30, 2014Journal of Medicinal ChemistryOpen Access

N-6-(4-Butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl-5-chloro-1-2-(4-methylpiperazin-1-yl)-2-oxoethyl-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist

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Key result

Reversible P2Y12 antagonist SAR216471 displays potent in vivo antiplatelet and antithrombotic activities.

Population

Preclinical models (in vitro and in vivo) for testing P2Y12 antagonists

Design

Preclinical

Authors

CBChristophe BoldronEvotec (United States)ABAngélina BesseSanofi (France)MBMarie-Françoise BordesSanofi (France)

Discussion

Member takes

Implication

Supports clinical development of reversible P2Y12 antagonists; leaves open human efficacy and safety confirmation.

Structured PICO

Population

Preclinical models (in vitro and in vivo) for testing P2Y12 antagonists

Intervention

SAR216471 (novel intravenous and oral, reversible, directly acting P2Y12 antagonist)

Outcome

P2Y12 receptor antagonism and inhibition of ADP-induced platelet aggregationsurrogate

SAR216471 is identified as a potent, reversible P2Y12 antagonist with promising preclinical antiplatelet and antithrombotic properties.

Cite This Study

Boldron et al. (2014) studied Thrombosis. SAR216471 vs. clopidogrel was evaluated on ADP-induced platelet aggregation. SAR216471 is a potent, highly selective, and reversible P2Y12 receptor antagonist that displays potent in vivo antiplatelet and antithrombotic activities.

synapsesocial.com/papers/6a0ecbee2eca052da647ca3e https://doi.org/10.1021/jm500588w

Topics

Dual antiplatelet therapy

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N-6-(4-Butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl-5-chloro-1-2-(4-methylpiperazin-1-yl)-2-oxoethyl-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Topics

N-6-(4-Butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl-5-chloro-1-2-(4-methylpiperazin-1-yl)-2-oxoethyl-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Topics

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