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Doramectin--a potent novel endectocide

A C Goudie1, N A Evans, K A Gration

  • 1Pfizer Central Research, Sandwich, UK.

Veterinary Parasitology
|July 1, 1993
PubMed
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Doramectin, a novel avermectin, shows potent antiparasitic activity in animal models and cattle. This compound demonstrates favorable efficacy and persistent action against key gastrointestinal and lung parasites in cattle.

Area of Science:

  • Veterinary Parasitology
  • Drug Discovery
  • Pharmacokinetics

Background:

  • Novel avermectins were synthesized via mutational biosynthesis.
  • Doramectin emerged as the lead compound from this series.
  • Existing avermectins like ivermectin are crucial antiparasitic agents.

Purpose of the Study:

  • To evaluate the in vivo antiparasitic efficacy of doramectin.
  • To compare doramectin's performance against dihydroavermectin B1a (DHAVM).
  • To assess doramectin's pharmacokinetics and persistent activity in cattle.

Main Methods:

  • In vivo testing in rat Trichostrongylus colubriformis and rabbit Psoroptes cuniculi models.
  • Subcutaneous administration of doramectin in a micelle formulation to cattle.

Related Experiment Videos

  • Intravenous administration for pharmacokinetic analysis in cattle.
  • Experimental infection models for Ostertagia ostertagi, Cooperia oncophora, and Dictyocaulus viviparus.

    • Main Results:

    • Doramectin demonstrated superior or comparable efficacy to DHAVM in initial models.
    • Highly effective subcutaneous administration (200 µg/kg) against O. ostertagi, C. oncophora, and D. viviparus in cattle.
    • Plasma half-life of doramectin in cattle was approximately 89 hours.
    • Persistent activity observed for 8 and 12 days against C. oncophora and O. ostertagi, respectively, at 400 µg/kg.

    Conclusions:

    • Doramectin is a highly effective novel avermectin with significant antiparasitic properties.
    • Its pharmacokinetic profile supports sustained activity, making it a promising candidate for parasitic disease control in cattle.
    • Doramectin offers a valuable new therapeutic option for managing common cattle parasites.