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Genotoxicity and carcinogenicity studies of antihistamines

Giovanni Brambilla1, Francesca Mattioli, Luigi Robbiano

  • 1Department of Internal Medicine, Division of Clinical Pharmacology and Toxicology, University of Genoa, Viale Benedetto XV 2, 16132 Genoa, Italy.

Archives of Toxicology
|February 18, 2011
PubMed

Insights

Many marketed antihistamines lack complete genotoxicity and carcinogenicity data. A significant portion of tested drugs showed positive results in these safety assays, highlighting potential risks.

Area of Science:

  • Pharmacology
  • Toxicology
  • Drug Safety Evaluation

Background:

  • Antihistamines are widely used medications for allergic conditions.
  • Comprehensive safety data, including genotoxicity and carcinogenicity, is crucial for marketed drugs.
  • Regulatory requirements for drug safety testing have evolved over time.

Purpose of the Study:

  • To review and compile genotoxicity and carcinogenicity assay results for marketed antihistamines.
  • To assess the completeness of safety data for these drugs based on current guidelines.
  • To identify antihistamines with positive findings in safety assays.

Main Methods:

  • Systematic review of published literature and regulatory documents.
  • Compilation of genotoxicity assay data (e.g., Ames test, chromosomal aberration assays).
  • Compilation of carcinogenicity assay data from rodent studies.

Main Results:

  • Out of 70 examined antihistamines, 29 (41.4%) had available genotoxicity and/or carcinogenicity data.
  • 12 drugs tested positive in genotoxicity assays, six in carcinogenicity assays, and four in both.
  • Only 12 (17.1%) of the drugs met all current data requirements, with many developed before stringent regulations.

Conclusions:

  • A substantial number of marketed antihistamines lack comprehensive genotoxicity and carcinogenicity data.
  • Positive findings in safety assays were observed for several drugs, warranting further investigation.
  • The review underscores the need for updated safety assessments, especially for older medications.

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