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| Other names | CVL-751; PF-6649751; PF-06649751 |
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| 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 for the treatment of Parkinson's disease.[1][2][3], under development by Cerevel Therapeutics who acquired Tavapadon from Pfizer in 2018. It acts as a selective partial agonist of the dopamine D1 (Ki = 8.54 nM) and D5 receptors.[2][3] It also shows biased agonism for Gs-coupled signaling.[2] As of July 2021, tavapadon is in phase 3 clinical trials for Parkinson's disease.[1]
See also
[edit]References
[edit]- ^ a b "Tavapadon - Cerevel Therapeutics". Adis Insight. Springer Nature Switzerland AG.
- ^ a b c Cerri S, Blandini F (December 2020). "An update on the use of non-ergot dopamine agonists for the treatment of Parkinson's disease". Expert Opinion on Pharmacotherapy. 21 (18): 2279–2291. doi:10.1080/14656566.2020.1805432. PMID 32804544. S2CID 221163451.
- ^ a b Hall A, Provins L, Valade A (January 2019). "Novel Strategies To Activate the Dopamine D1 Receptor: Recent Advances in Orthosteric Agonism and Positive Allosteric Modulation". Journal of Medicinal Chemistry. 62 (1): 128–140. doi:10.1021/acs.jmedchem.8b01767. PMID 30525590. S2CID 54469910.