Target organ profiles in toxicity studies supporting human dosing: an assessment of recovery and chronic dosing

Steve Horner1, Sally Robinson1, David Lees1

  • 1Drug Safety and Metabolism, AstraZeneca, Alderley Park, Macclesfield, UK.

Insights

Most target organ toxicities from early drug development studies resolve after a recovery period. Chronic studies reveal additional toxicities, crucial for assessing long-term human dosing risks.

Area of Science:

  • Preclinical toxicology
  • Drug development

Background:

  • Previous studies characterized target organ toxicities for 77 candidate drugs (CDs) before first-time in man (FTIM) studies.
  • Understanding toxicity resolution and identifying additional targets in chronic studies is vital for drug safety.

Purpose of the Study:

  • To assess target organ recovery after a dose-free period in FTIM studies.
  • To identify additional target organs affected in chronic (>=3 month) studies supporting long-term clinical dosing.

Main Methods:

  • Analysis of histopathological changes in target organs from rodent and non-rodent toxicity studies.
  • Evaluation of recovery following a dose-free period post-FTIM studies.
  • Comparison of findings between FTIM and chronic toxicity studies.

Main Results:

  • Over 86% of FTIM-related findings showed full or partial resolution post-recovery.
  • Recovery profiles were consistent across different therapy areas and drug progression.
  • Chronic studies revealed toxicities in 39% more target organs compared to FTIM studies.

Conclusions:

  • Chronic toxicity studies provide essential data for long-term human dosing risk assessment.
  • Recovery assessments in FTIM studies should be case-by-case, based on specific needs.
  • Findings align with International Council for Harmonisation (ICH) guidance on assessing toxicity reversibility.

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