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Boron-Containing Drug Candidates in Clinical Trials
Billy Vuong1, Nitesh Sanghai1, Muhammad Shaharyar Khan Afridi1
1Rady Faculty of Health Science, College of Pharmacy, University of Manitoba, Winnipeg, MB, Canada.
Handbook of Experimental Pharmacology
|August 5, 2026
Summary
Boron compounds show great promise in medicine, treating various diseases through unique interactions. Clinical trials reveal their potential, with success depending on factors beyond inherent boron toxicity.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Boron Chemistry
Background:
- Boron's unique electronic properties facilitate reversible covalent interactions.
- Boron-containing drugs have expanded beyond proteasome inhibition to diverse therapeutic areas.
- Several boron scaffolds are being investigated in clinical trials.
Purpose of the Study:
- To critically survey boron-containing drug candidates in clinical trials.
- To organize and compare these agents by scaffold class.
- To analyze their mechanisms, efficacy, safety, and development trajectories.
Main Methods:
- Review of clinical trial data for boron-containing agents.
- Categorization of agents by chemical scaffold (boronic acids, benzoxaboroles, etc.).
- Comparative analysis of mechanisms, pharmacokinetics, efficacy, and safety.
Main Results:
- Boron chemistry enables selective target engagement via reversible covalent inhibition, tRNA trapping, and β-lactamase blockade.
- Notable advances include borofalan for BNCT, acoziborole for trypanosomiasis, and ganfeborole for tuberculosis.
- Most candidates were well-tolerated; discontinuations often due to efficacy or commercial factors, not boron toxicity.
Conclusions:
- Boron's versatility, low toxicity, and precise target binding support clinical translation.
- Clinical success hinges on matching pharmacology with unmet needs and strategic development.
- Advances in scaffold design and therapy selection will expand the impact of boron-containing medicines.
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