Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease. It is under development by Cerevel Therapeutics, which acquired tavapadon from Pfizer in 2018. It is taken by mouth.
Tavapadon acts as a highly selective partial agonist of the dopamine D<sub>1</sub> receptor (K<sub>i</sub> = 9nM; = 65%) and the dopamine D<sub>5</sub> receptor (K<sub>i</sub> = 13nM; = 81%). It has no significant affinity or functional activity at the D<sub>2</sub>-like receptors (D<sub>2</sub>, D<sub>3</sub>, D<sub>4</sub>) (K<sub>i</sub> âÂÂ¥ 4,870 to 6,720nM). Tavapadon also shows biased agonism for G<sub>s</sub>-coupled signaling at the D<sub>1</sub>-like receptors.
As of December 2024, tavapadon has completed phase 3 clinical trials for Parkinson's disease.