Tavapadon

Tavapadon
Clinical data
Other names	CVL-751; PF-6649751; PF-06649751
Identifiers
	IUPAC name (−)-(6Ξ)-1,5-dimethyl-6-(2-methyl-4-trifluoromethylpyridin-2-yl)oxyphenyl)pyrimidine-2,4(1H,3H)-dione;
CAS Number	1643489-24-0;
PubChem CID	86764100;
ChemSpider	48062699;
UNII	PT4P8MJP8L;
KEGG	D11431;
ChEMBL	ChEMBL3697617;
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 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 (K_i = 8.54 nM) and D₅ receptors.^[2]^[3] It also shows biased agonism for G_s-coupled signaling.^[2] As of July 2021, tavapadon is in phase 3 clinical trials for Parkinson's disease.^[1]

Referencesedit

^ ^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.

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[AdisInsight-1] "Tavapadon - Cerevel Therapeutics". Adis Insight. Springer Nature Switzerland AG.

[pmid32804544-2] 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.

[pmid30525590-3] 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.

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[3]

See alsoedit

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