The antitumor agent 3-bromopyruvate has a short half-life at physiological conditions.

Abstract

Clinical research is currently exploring the validity of the anti-tumor candidate 3-bromopyruvate (3-BP) as a novel treatment for several types of cancer. However, recent publications have overlooked rarely-cited earlier work about the instability of 3-BP and its decay to 3-hydroxypyruvate (3-HP) which have obvious implications for its mechanism of action against tumors, how it is administered, and for precautions when preparing solutions of 3-BP. This study found the first-order decay rate of 3-BP at physiological temperature and pH has a half-life of only 77 min. Lower buffer pH decreases the decay rate, while choice of buffer and concentration do not affect it. A method for preparing more stable solutions is also reported.

• Authors: Matthew Glick, Perry Biddle, Josh Jantzi, Samantha Weaver, Doug Schirch
• Journal: Biochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 452 Issue 1 Pg. 170-3 (Sep 12 2014) ISSN: 1090-2104 [Electronic] United States
• PMID: 25152397 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014 Elsevier Inc. All rights reserved.

Chemical References

• Antineoplastic Agents
• Pyruvates
• bromopyruvate

Topics

• Antineoplastic Agents (pharmacokinetics, therapeutic use)
• Half-Life
• Hydrogen-Ion Concentration
• Magnetic Resonance Spectroscopy
• Pyruvates (pharmacokinetics, therapeutic use)