Tavapadon (CVL-75, PF-06649751) is a potent, selective orally available dopamine D1/D5 receptor partial agonist with Ki of 9 nM/13 nM, respectively.
Tavapadon (CVL-75, PF-06649751) shows a low affinity at D2 (Ki ≥ 6210 nM), D3 (Ki ≥ 6720 nM), and D4 (Ki ≥ 4870 nM).
Tavapadon (CVL-75, PF-06649751) acts as a partial agonist by binding at D1 and D5 receptors, corresponding to 65% and 81% of dopamine’s intrinsic activity, respectively, and inducing functional receptor activation, with half-maximal effective concentration (EC50) values of 19 nM and 17 nM.
Tavapadon (CVL-75, PF-06649751) shows potential for the treatment of early through advanced Parkinson's disease (PD), as well as adjunctive therapy in combination with levodopa produce dose-proportional occupancy of D1/D5 receptors.
