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Updated: Jul 19, 2026

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation
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Published on: January 19, 2019

Potential use of alexidine dihydrochloride as an apoptosis-promoting anticancer agent

Kenneth W Yip1, Emma Ito, Xinliang Mao

  • 1Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada.

Molecular Cancer Therapeutics
|September 21, 2006
PubMed

Insights

Alexidine dihydrochloride shows anticancer specificity against head and neck cancers, inducing apoptosis and reducing tumor formation. This novel bisbiguanide compound offers a promising therapeutic lead for these challenging malignancies.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Head and neck cancers require novel therapeutic strategies beyond current treatments.
  • Alexidine dihydrochloride is investigated as a potential new agent.

Purpose of the Study:

  • To evaluate alexidine dihydrochloride's efficacy and specificity in head and neck cancer treatment.
  • To elucidate the mechanisms of action for alexidine dihydrochloride.

Main Methods:

  • Cell viability assays (ED50 determination) in cancer and normal cells.
  • Assays for drug interaction, apoptosis induction (DNA content, Hoechst staining), and mitochondrial damage (TEM, membrane potential).
  • Caspase activity assays and in vivo tumor formation studies.

Main Results:

  • Alexidine dihydrochloride demonstrated selective toxicity towards head and neck cancer cells (FaDu, C666-1) compared to normal cells.
  • The compound induced apoptosis via mitochondrial damage and caspase activation.
  • It reduced cancer cell clonogenic survival and in vivo tumor-forming potential without interfering with standard therapies.

Conclusions:

  • Alexidine dihydrochloride is the first bisbiguanide compound identified with anticancer specificity for head and neck cancers.
  • It represents a promising novel therapeutic lead for head and neck cancer treatment.

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