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| Other names | CVL-751; PF-6649751; PF-06649751 |
| Routes of administration | By mouth[1] |
| Drug class | Dopamine receptor agonist |
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| Formula | C19H16F3N3O3 |
| Molar mass | 391.350 g·mol−1 |
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Tavapadon (developmental code namesCVL-751,PF-06649751) is adopamine receptor agonist which is under development for the treatment ofParkinson's disease.[2][3][4] It is under development byCerevel Therapeutics, which acquired tavapadon fromPfizer in 2018.[2] It is takenby mouth.[1]
Tavapadon acts as a highlyselectivepartial agonist of thedopamineD1 receptor (Ki = 9 nM;IATooltip Intrinsic activity = 65%) and the dopamineD5 receptor (Ki = 13 nM;IA = 81%).[3][4][1] It has no significantaffinity orfunctional activity at theD2-like receptors (D2,D3,D4) (Ki ≥ 4,870 to 6,720 nM).[1] Tavapadon also showsbiased agonism forGs-coupledsignaling at theD1-like receptors.[1][3]
As of December 2024, tavapadon has completedphase 3clinical trials for Parkinson's disease.[2]
Tavapadon is a highly selective partial agonist at D1 and D5 dopamine receptors, [52] with little to no functional activity at D2, D3, or D4 receptors in vitro (unpublished data). Assays measuring the displacement of radioligand binding in cell lines expressing recombinant human dopamine receptors have shown that tavapadon has a high affinity for both D1 (Ki = 9 nM) and D5 (Ki = 13 nM) (unpublished data). Conversely, tavapadon had a low affinity at D2 (Ki ≥ 6210 nM), D3 (Ki ≥ 6720 nM), and D4 (Ki ≥ 4870 nM) (unpublished data). [...] In vitro assays of functional activity have confirmed that tavapadon 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inducing functional receptor activation, with half-maximal effective concentration (EC50) values of 19 nM and 17 nM (unpublished data).
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