Tavapadon

Tavapadon
	File:Tavapadon.svg
Clinical data
Other names	CVL-751; PF-6649751; PF-06649751
Routes of; administration	By mouth
Drug class	Dopamine receptor agonist
Identifiers
	IUPAC name (−)-(6Ξ)-1,5-dimethyl-6-(2-methyl-4-[(3-[trifluoromethyl]pyridin-2-yl)oxy]phenyl)pyrimidine-2,4(1H,3H)-dione;
CAS Number	1643489-24-0;
PubChem CID	86764100;
ChemSpider	48062699;
UNII	PT4P8MJP8L;
KEGG	D11431;
ChEMBL	ChEMBL3697617;
E number	{{#property:P628}}
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Chemical and physical data
Formula	C19H16F3N3O3
Molar mass	391.350 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C;
	InChI 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-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 (K_i = 9 nM; IATooltip Intrinsic activity = 65%) and the dopamine D₅ receptor (K_i = 13 nM; IA = 81%).^[3]^[4]^[1] It has no significant affinity or functional activity at the D₂-like receptors (D₂, D₃, D₄) (K_i ≥ 4,870 to 6,720 nM).^[1] Tavapadon also shows biased agonism for G_s-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]

References

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