ondansetron + tariquidar

Ondansetron + tariquidar is an investigational drug combination consisting of ondansetron, a selective serotonin 5-HT3 receptor antagonist, and tariquidar, a potent P-glycoprotein (Pgp) inhibitor. Ondansetron is primarily used as an antiemetic but has shown promise in treating neuropathic pain; however, its efficacy may be limited by poor central nervous system (CNS) penetration due to active efflux by P-glycoprotein at the blood-brain barrier. Tariquidar inhibits this efflux transporter, thereby increasing CNS exposure to ondansetron. Preclinical studies have demonstrated that co-administration of these agents results in significantly higher concentrations of ondansetron in brain and spinal cord tissues compared to administration of ondansetron alone. This pharmacokinetic enhancement is being evaluated clinically for potential benefit in patients with neuropathic pain[1][2][3][4].