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Tranexamic acid derivatives with enhanced absorption.

C M Svahn, F Merenyi, L Karlson

    Journal of Medicinal Chemistry
    |April 1, 1986
    PubMed
    Summary
    This summary is machine-generated.

    New tranexamic acid derivatives were synthesized, showing improved oral absorption in rats compared to the original drug. One promising derivative was selected for human studies, offering potential advancements in antifibrinolytic therapy.

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    Area of Science:

    • Pharmacology
    • Medicinal Chemistry
    • Drug Development

    Background:

    • Tranexamic acid is a widely used antifibrinolytic agent.
    • Development of novel tranexamic acid derivatives aims to improve pharmacokinetic properties.
    • Understanding derivative stability and absorption is crucial for therapeutic efficacy.

    Purpose of the Study:

    • To synthesize novel tranexamic acid derivatives.
    • To evaluate the stability and oral absorption of these derivatives.
    • To identify a derivative suitable for human clinical trials.

    Main Methods:

    • Chemical synthesis of tranexamic acid derivatives with one or two moieties.
    • Assessment of derivative stability in acidic, neutral, and plasma conditions.
    • Estimation of relative oral absorption in rats via urinary excretion analysis of tranexamic acid.

    Main Results:

    • Synthesized derivatives exhibited good stability in acidic and neutral solutions.
    • Derivatives were readily hydrolyzed in plasma.
    • Most derivatives demonstrated enhanced oral absorption in rats compared to tranexamic acid.
    • 1-[(Ethoxycarbonyl)oxy]ethyl trans-4-(aminomethyl)cyclohexanecarboxylate hydrochloride was identified as a lead candidate.

    Conclusions:

    • Novel tranexamic acid derivatives can be synthesized with improved oral absorption characteristics.
    • Plasma hydrolysis is a key factor influencing derivative bioavailability.
    • The selected derivative warrants further investigation in human subjects for antifibrinolytic applications.