Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease.
[1] Tavapadon acts as a highly selective partial agonist of the dopamine D1 receptor (Ki = 9 nM; IATooltip Intrinsic activity = 65%) and the dopamine D5 receptor (Ki = 13 nM; IA = 81%).
[3][4][1] It has no significant affinity or functional activity at the D2-like receptors (D2, D3, D4) (Ki ≥ 4,870 to 6,720 nM).
[1] Tavapadon also shows biased agonism for Gs-coupled signaling at the D1-like receptors.
[1][3] As of December 2024, tavapadon has completed phase 3 clinical trials for Parkinson's disease.