Journal of Bioenergetics and Biomembranes

, Volume 48, Issue 4, pp 349–362 | Cite as

The anticancer agent 3-bromopyruvate: a simple but powerful molecule taken from the lab to the bedside

  • J. Azevedo-SilvaEmail author
  • O. Queirós
  • F. Baltazar
  • S. Ułaszewski
  • A. Goffeau
  • Y. H. Ko
  • P. L. Pedersen
  • A. Preto
  • M. CasalEmail author


At the beginning of the twenty-first century, 3-bromopyruvate (3BP), a simple alkylating chemical compound was presented to the scientific community as a potent anticancer agent, able to cause rapid toxicity to cancer cells without bystander effects on normal tissues. The altered metabolism of cancers, an essential hallmark for their progression, also became their Achilles heel by facilitating 3BP’s selective entry and specific targeting. Treatment with 3BP has been administered in several cancer type models both in vitro and in vivo, either alone or in combination with other anticancer therapeutic approaches. These studies clearly demonstrate 3BP’s broad action against multiple cancer types. Clinical trials using 3BP are needed to further support its anticancer efficacy against multiple cancer types thus making it available to more than 30 million patients living with cancer worldwide. This review discusses current knowledge about 3BP related to cancer and discusses also the possibility of its use in future clinical applications as it relates to safety and treatment issues.


3-bromopyruvate Monocarboxylate transporter Cancer metabolism Tumor microenvironment Cancer therapy Clinical studies 



This work was supported by the strategic programme UID/BIA/04050/2013 (POCI-01-0145-FEDER-007569) funded by national funds through the FCT I.P. and by the ERDF through the COMPETE2020 - Programa Operacional Competitividade e Internacionalização (POCI). João Azevedo-Silva received a fellowship from the Portuguese government from the FCT through FSE (Fundo Social Europeu) and POPH (Programa Operacional Potencial Humano) [grant number SFRH/BD/76038/2011]. Co-author Peter L. Pedersen was supported by NIH grant NCI CA l0951 for many years for cancer research that led to a number of the findings described in this review.


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Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  • J. Azevedo-Silva
    • 1
    Email author
  • O. Queirós
    • 1
    • 2
  • F. Baltazar
    • 3
    • 4
  • S. Ułaszewski
    • 5
  • A. Goffeau
    • 6
  • Y. H. Ko
    • 7
  • P. L. Pedersen
    • 8
  • A. Preto
    • 1
  • M. Casal
    • 1
    Email author
  1. 1.Centre of Molecular and Environmental Biology (CBMA), Department of BiologyUniversity of MinhoBragaPortugal
  2. 2.CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de GandraGandraPortugal
  3. 3.Life and Health Sciences Research Institute (ICVS), School of Health SciencesUniversity of MinhoBragaPortugal
  4. 4.ICVS/3B’s - PT Government Associate LaboratoryGuimarãesPortugal
  5. 5.Institute of Genetics and MicrobiologyUniversity of WroclawWroclawPoland
  6. 6.Institut des Sciences de la VieUniversité Catholique de Louvain-la-NeuveLouvain-la-NeuveBelgium
  7. 7.KoDiscovery, LLCUniversity of Maryland BioParkBaltimoreUSA
  8. 8.Departments of Biological Chemistry and Oncology, Member at Large, Sidney Kimmel Comprehensive Cancer Center, School of MedicineJohn Hopkins UniversityBaltimoreUSA

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