Tavapadon (developmental code names CVL-751, PF-06649751) is a

dopamine receptor agonist A dopamine agonist is a compound that activates dopamine receptors. There are two families of dopamine receptors, D1-like and D2-like. They are all G protein-coupled receptors. D1- and D5-receptors belong to the D1-like family and the D2-like ...

which is under development for the treatment of

Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become ...

. It is under development by

Cerevel Therapeutics Cerevel Therapeutics Holdings, Inc. was an American biotechnology and pharmaceuticals company based in Cambridge, Massachusetts, focused on the development of novel therapies for mental and neurological illnesses. History Cerevel was establish ...

, which acquired tavapadon from

Pfizer Pfizer Inc. ( ) is an American Multinational corporation, multinational Pharmaceutical industry, pharmaceutical and biotechnology corporation headquartered at The Spiral (New York City), The Spiral in Manhattan, New York City. Founded in 184 ...

in 2018. It is taken

by mouth Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administ ...

. Tavapadon acts as a highly selective

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...

of the

dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized ...

D₁ receptor (K_i = 9nM; = 65%) and the dopamine D₅ receptor (K_i = 13nM; = 81%). It has no significant

affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ...

functional activity An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agoni ...

at the D₂-like receptors ( D₂, D₃, D₄) (K_i ≥ 4,870 to 6,720nM). Tavapadon also shows

biased agonism Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the end ...

for G_s-coupled

signaling A signal is both the process and the result of transmission of data over some media accomplished by embedding some variation. Signals are important in multiple subject fields including signal processing, information theory and biology. ...

at the D₁-like receptors. As of December 2024, tavapadon has completed phase 3

clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

s for Parkinson's disease.

References

Biased ligands D1 receptor agonists D5 receptor agonists Diketones Experimental drugs Pyridines Pyrimidines Trifluoromethyl compounds {{Nervous-system-drug-stub

See also

References