Developmental toxicity assessment of the new fluoroquinolone antibacterial DW-116 in rabbits

J Appl Toxicol. 2005 Jan-Feb;25(1):52-9. doi: 10.1002/jat.1033.

Abstract

DW-116 is a newly developed fluoroquinolone antibacterial with a broad spectrum against both Gram-positive and Gram-negative bacteria. We have reported recently that DW-116 is embryotoxic and teratogenic in rats. The present study was conducted to investigate the teratogenicity of DW-116, together with maternal toxicity and developmental toxicity using New Zealand White rabbits. The test chemical was administered by gavage to pregnant rabbits from gestational day (GD) 6 through to GD 18 at dose levels of 0, 5, 19.5 and 76.1 mg kg(-1) day(-1). All does were subjected to caesarean section on day 28 of gestation and their foetuses were examined for external, visceral and skeletal abnormalities. In the 76.1 mg kg(-1) group, a minimal maternal toxicity, as evidenced by decreased body weight gain during treatment period, was observed in pregnant rabbits. Significant embryo-foetal toxicity, including increased number of foetal deaths and delayed foetal ossification, was seen. However, no treatment-related morphological changes were detected in foetal external, visceral and skeletal examinations. There were no adverse effects on either pregnant dams or embryo-foetal development at 19.5 and 5 mg kg(-1). It was concluded that administration of DW-116 during the major organogenetic period in rabbits produced decreased maternal body weight gain, increased number of foetal deaths and foetal developmental delay but no evidence of teratogenicity. The no-observed-adverse-effect levels (NOAELs) of DW-116 are considered to be 19.5 mg kg(-1) day(-1) for does and embryo-foetuses, respectively.

Publication types

  • Evaluation Study

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / toxicity*
  • Body Weight / drug effects
  • Drug Evaluation, Preclinical*
  • Embryonic Development / drug effects*
  • Female
  • Fetal Death / chemically induced
  • Fluoroquinolones / chemistry
  • Fluoroquinolones / toxicity*
  • Gestational Age
  • Molecular Structure
  • No-Observed-Adverse-Effect Level
  • Piperazines / chemistry
  • Piperazines / toxicity*
  • Pregnancy
  • Quinolones / chemistry
  • Quinolones / toxicity*
  • Rabbits

Substances

  • Anti-Bacterial Agents
  • DW-116
  • Fluoroquinolones
  • Piperazines
  • Quinolones