August 30, 2002Journal of Medicinal ChemistryOpen Access

Unique Overlap in the Prerequisites for Thrombin Inhibition and Oral Bioavailability Resulting in Potent Oral Antithrombotics

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Population

Preclinical models (rats, dogs, and an in vivo arterial flow model)

Comparison

Compound 27, a tripeptide transition state… vs Known non-TSA inhibitors

Design

Preclinical

Authors

AAAnton E.P. AdangLeiden University AMAdrianus P. A. de Man GVG.M.T. VogelSanofi (France)

Discussion

Member takes

Implication

Supports advancement to human studies; leaves open clinical translation of potency and bioavailability.

Structured PICO

Population

Preclinical models (rats, dogs, and an in vivo arterial flow model)

Intervention

Compound 27, a tripeptide transition state analogue (TSA) inhibitor of thrombin

Comparator

Known non-TSA inhibitors

Outcome

Oral bioavailability, elimination half-life, thrombin inhibition constant, and ED50surrogate

A novel tripeptide transition state analogue, Compound 27, demonstrates potent thrombin inhibition and high oral bioavailability in preclinical models.

Cite This Study

Adang et al. (2002) studied this question.

synapsesocial.com/papers/6a72a1065671bbf00bc31a0b https://doi.org/10.1021/jm011110z

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Unique Overlap in the Prerequisites for Thrombin Inhibition and Oral Bioavailability Resulting in Potent Oral Antithrombotics

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Unique Overlap in the Prerequisites for Thrombin Inhibition and Oral Bioavailability Resulting in Potent Oral Antithrombotics

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider