Drug intelligence / Profile preview

3-bromopyruvate

Development stage
Preclinical
Lead developer
Johns Hopkins University
Modality
Small Molecules
Administration
Intravenous, Intratumoral, Intra-arterial
01

Overview

3-Bromopyruvate (3-BP) is a small molecule alkylating agent and a potent inhibitor of glycolysis. It acts primarily by inhibiting hexokinase-2 (HK2) and glyceraldehyde-3-phosphate dehydrogenase (GAPDH), thereby disrupting the Warburg effect in cancer cells. By blocking glycolytic flux and the pentose phosphate pathway (PPP), it depletes cellular ATP and nucleotide precursors, which sensitizes tumors to other treatments such as radiation or chemotherapy. 3-BP has been investigated for various cancers with high glycolytic rates, including pancreatic cancer and hepatocellular carcinoma, and is often studied as a metabolic sensitizer in combination therapies.

Other names
3-bromopyruvic acidbromopyruvic acidbromopyruvate
02

Targets

GSH (Glutathione)GAPDH (Glyceraldehyde-3-phosphate dehydrogenase)HK2 (Hexokinase Type II)SLC16A1 (Mitochondrial Pyruvate Carrier)

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