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| Clinical data | |
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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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| Chemical and physical data | |
| Formula | C19H16F3N3O3 |
| Molar mass | 391.350 g·mol−1 |
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Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease.[2][3][4] It is under development by Cerevel Therapeutics, which acquired tavapadon from Pfizer in 2018.[2] It is taken by mouth.[1]
Tavapadon acts as a highly selective partial agonist of the dopamine D1 receptor (Ki = 9 nM; IA = 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.[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at D1 and D5 dopamine receptors, [52] with little to no functional activity at D2, D3, or D4 receptors in vitro (unpublished data).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human dopamine receptors have shown that tavapadon has a high affinity for both D1 (Ki = 9 nM) and D5 (Ki = 13 nM) (unpublished data). Conversely, tavapadon had a low affinity at D2 (Ki ≥ 6210 nM), D3 (Ki ≥ 6720 nM), and D4 (Ki ≥ 4870 nM) (unpublished data).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inducing functional receptor activation, with half-maximal effective concentration (EC50) values of 19 nM and 17 nM (unpublished data).
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