PF-06649751 + itraconazole

PF-06649751 + itraconazole is a combination of PF-06649751, a novel orally administered, non-catechol-based, dopamine D1/D5 receptor partial agonist developed for symptomatic treatment of motor symptoms in Parkinson’s disease, and itraconazole, an oral antifungal that acts as a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme. PF-06649751 improves motor symptoms through stimulation of dopamine D1/D5 receptors, providing a new pharmacological approach beyond traditional catecholamine-based therapies. The combination with itraconazole is typically utilized in clinical pharmacokinetic studies to assess potential drug-drug interactions, as itraconazole can markedly increase plasma concentrations of PF-06649751 by inhibiting its CYP3A4-mediated metabolism. PF-06649751 has shown statistically significant improvements in motor function ratings and established safety in early-stage Parkinson’s disease clinical trials.[1][2][3][5] Itraconazole itself is not indicated for Parkinson’s disease but is included for drug–drug interaction studies.[1][2][3][5]

Other names

PF-06649751 + itraconazole