Category: pharmacological
Aliases: DCA, Sodium dichloroacetate
Small organic acid that inhibits pyruvate dehydrogenase kinase (PDK1–4), locking pyruvate dehydrogenase (PDH) in its active, dephosphorylated form. Shifts metabolism from glycolysis / lactate production toward mitochondrial oxidative phosphorylation — lowers circulating lactate and, in cancer cells exhibiting the Warburg effect, restores apoptotic competence by repolarising mitochondria. Metabolised by glutathione-transferase-zeta-1 (GSTZ1); DCA itself inactivates GSTZ1, so terminal t½ lengthens dramatically with chronic dosing (from ~1 h initially to 10+ h after weeks). Dose-limiting toxicity: reversible peripheral neuropathy.
PO: 1h, IV: 1h