Stiripentol is a third-generation anti-epileptic drug that is known to inhibit the synaptosomal uptake of GABA, increasing the activation of GABAA receptors. It also inhibits microsomal cytochrome P450 (CYP) isoforms CYP3A4, CYP1A2, and CYP2C19. More recently, stiripentol and analogs have been shown to inhibit lactate dehydrogenase (LDH), blocking both lactate to pyruvate and pyruvate to lactate conversions by human LDH isoforms 1 and 5 at 500 μM. In this way, stiripentol mimics ketogenic diets, which can also lower lactate levels in the brain and prevent seizures.
