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Related Experiment Videos

[Research and development of clarithromycin].

S Omura1, S Morimoto, T Nagate

  • 1Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan
|September 1, 1992
PubMed
Summary

Clarithromycin (CAM) is a potent O-alkylated erythromycin derivative with enhanced antibacterial activity and acid stability. Its improved synthesis and favorable pharmacokinetics, including high lung distribution and active metabolites, contribute to its superior clinical efficacy against various infections.

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Area of Science:

  • Medicinal Chemistry
  • Microbiology
  • Pharmacology

Context:

  • Erythromycin (EM) derivatives were synthesized to improve antibacterial properties.
  • Clarithromycin (CAM), a 6-O-methylerythromycin derivative, demonstrated superior in vitro and in vivo activity.
  • Existing synthesis methods for CAM had low yields due to poor methylation selectivity.

Purpose:

  • To develop a more selective and efficient synthesis for clarithromycin (CAM).
  • To evaluate the antibacterial spectrum, potency, and pharmacokinetic properties of CAM.
  • To investigate the metabolism and clinical efficacy of CAM and its active metabolite.

Summary:

  • A novel industrial-scale synthesis of CAM was established using erythromycin 9-oxime derivatives, achieving over 45% yield.

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  • CAM exhibits broad-spectrum activity against Gram-positive, Gram-negative, anaerobic bacteria, Mycoplasma, and Chlamydia, with significantly higher potency than EM.
  • CAM demonstrates superior efficacy in treating systemic and respiratory tract infections in animal models and favorable pharmacokinetic profiles in humans, including high lung tissue penetration.

    • Impact:

    • The development of an efficient CAM synthesis enables large-scale production of this potent macrolide antibiotic.
    • CAM offers a valuable therapeutic option with enhanced activity and improved drug delivery compared to erythromycin.
    • Understanding CAM's metabolism reveals the contribution of its active metabolite to its overall clinical effectiveness.