Tavapadon
Clinical data
Other namesCVL-751; PF-6649751; PF-06649751
Identifiers
  • 1,5-dimethyl-6-[2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]oxyphenyl]pyrimidine-2,4-dione
CAS Number
  • 1643489-24-0
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC19H16F3N3O3
Molar mass391.350 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C
  • InChI=1S/C19H16F3N3O3/c1-10-9-12(28-17-14(19(20,21)22)5-4-8-23-17)6-7-13(10)15-11(2)16(26)24-18(27)25(15)3/h4-9H,1-3H3,(H,24,26,27)
  • Key:AKQXQLUNFKDZBN-UHFFFAOYSA-N

Tavapadon (developmental code names CVL-751, PF-6649751, PF-06649751) is a dopamine receptor agonist which is under development by Pfizer and Cerevel Therapeutics for the treatment of Parkinson's disease.[1][2][3] 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]

References

  1. ^ a b https://adisinsight.springer.com/drugs/800039248
  2. ^ 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 Opin Pharmacother. 21 (18): 2279–2291. doi:10.1080/14656566.2020.1805432. PMID 32804544.
  3. ^ 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". J Med Chem. 62 (1): 128–140. doi:10.1021/acs.jmedchem.8b01767. PMID 30525590.