What is the clinical evidence from this study?

Study design: Other. Population: Acute thrombosis and chronic neointima formation. Intervention: YM-254890 vs. Clopidogrel. Primary outcome: Thrombus and neointima formation.

What question did this study set out to answer?

Investigate the pharmacological effects of the specific Gαq/11 inhibitor YM-254890 on acute arterial thrombosis and chronic neointima formation following vascular injury.

January 1, 2005Thrombosis and Haemostasis

Pharmacological properties of YM-254890, a specific Gαq/11 inhibitor, on thrombosis and neointima formation in mice

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Key result

YM-254890 significantly inhibited thrombus and neointima formation in mice, with greater inhibitory potency than clopidogrel, though it reduced systemic blood pressure at higher doses.

Why the study?

Does YM-254890 inhibit acute thrombosis and chronic neointima formation in mice with vascular injury?

Population

Mice with FeCl3-induced vascular injury in the carotid artery

Comparison

YM-254890 vs Clopidogrel (for neointima studies)

Design

Preclinical

Follow-up

3 weeks

Authors

MTMasatoshi TaniguchiPhotonics Electronics Technology Research Association YMYumiko MoritaniAstellas Pharma (Japan)TUToshio UemuraAstellas Pharma (Japan)

Discussion

Member takes

Implication

Hypothesis-generating for Gq inhibition in vascular injury; should not yet influence clinical antithrombotic practice.

Key Points

Investigate the pharmacological effects of the specific Gαq/11 inhibitor YM-254890 on acute arterial thrombosis and chronic neointima formation following vascular injury.
FeCl3 was applied to induce vascular injury in mouse carotid arteries.
YM-254890 was administered intravenously or orally before injury for thrombosis evaluation, and orally (1 hour before and twice daily for 1 week) for neointima assessment after 3 weeks.
Platelet aggregation, tail transection bleeding time, systemic blood pressure, and histological neointima formation were measured and compared with clopidogrel.
YM-254890 significantly inhibited platelet aggregation and thrombus formation at 0.03 mg/kg intravenously and 1 mg/kg orally, though bleeding time was prolonged at 0.1 mg/kg intravenously and 3 mg/kg orally.
Oral YM-254890 dose-dependently inhibited neointima formation 3 weeks post-injury at 1 mg/kg twice daily, demonstrating greater inhibitory potency than clopidogrel.
Systemic blood pressure was significantly reduced at doses three times higher than the antithrombotic and anti-neointimal effective doses.

Structured PICO

Does YM-254890 inhibit acute thrombosis and chronic neointima formation in mice with vascular injury?

Population

Mice with FeCl3-induced vascular injury in the carotid artery evaluated for acute thrombosis and chronic neointima formation.

Intervention

YM-254890 (intravenous bolus or oral administration)

Comparator

Clopidogrel (for neointima studies)

Outcome

Acute thrombosis and chronic neointima formationsurrogate

YM-254890 effectively inhibits thrombosis and neointima formation in mice, but its systemic use may be limited by a narrow therapeutic window regarding blood pressure reduction.

Limitations

Systemic use of YM-254890 may be limited owing to its narrow therapeutic window.
Narrow therapeutic window due to systemic blood pressure reduction at higher doses

Cite This Study

Taniguchi et al. (2005) studied Acute thrombosis and chronic neointima formation. YM-254890 vs. Clopidogrel was evaluated on Thrombus and neointima formation. YM-254890 significantly inhibited thrombus and neointima formation in mice, with greater inhibitory potency than clopidogrel, though it reduced systemic blood pressure at higher doses.

synapsesocial.com/papers/6a9b87ab7cb3b62bb4a73b40 https://doi.org/10.1160/th04-09-0635

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Pharmacological properties of YM-254890, a specific Gαq/11 inhibitor, on thrombosis and neointima formation in mice

Discussion

Member takes

Implication

Key Points

Structured PICO

Limitations

Cite This Study

Pharmacological properties of YM-254890, a specific Gαq/11 inhibitor, on thrombosis and neointima formation in mice

Discussion

Member takes

Implication

Key Points

Structured PICO

Limitations

Cite This Study

Also Consider

Also Consider