What question did this study set out to answer?

To review the therapeutic importance of thrombin and examine the structural and pharmacological hurdles in developing orally bioavailable direct active site inhibitors.

September 1, 1995Blood Coagulation & Fibrinolysis

Challenges in the development of orally bioavailable thrombin active site inhibitors

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Authors

SKS. David KimballRutgers, The State University of New Jersey

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Implication

Pharmacological review discusses challenges in designing oral thrombin active site inhibitors for cardiovascular disease, highlighting requirements for bioavailability, selectivity, and sustained...

Key Points

To review the therapeutic importance of thrombin and examine the structural and pharmacological hurdles in developing orally bioavailable direct active site inhibitors.
Assessed the physiological functions of activated thrombin in coagulation cascades and cellular receptor activation.
Profiled the pharmacokinetics and structural properties of small-molecule active site inhibitors relative to clinical drug criteria.
Direct small-molecule inhibition of the thrombin active site has remained elusive despite its high therapeutic value across venous and arterial thrombosis indications.
Developing clinically successful oral inhibitors requires surmounting key pharmacological hurdles, specifically low oral bioavailability, inadequate target selectivity, and short duration of action.

Cite This Study

S. David Kimball (1995) studied this question.

synapsesocial.com/papers/6a7100cce71d69abee08fcbc https://doi.org/10.1097/00001721-199509000-00002

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Implication

Pharmacological review discusses challenges in designing oral thrombin active site inhibitors for cardiovascular disease, highlighting requirements for bioavailability, selectivity, and sustained...

Challenges in the development of orally bioavailable thrombin active site inhibitors

Discussion

Member takes

Implication

Key Points

Cite This Study

Challenges in the development of orally bioavailable thrombin active site inhibitors

Discussion

Member takes

Implication

Key Points

Cite This Study

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