- Source: Tavapadon
Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease. It is under development by Cerevel Therapeutics, which acquired tavapadon from Pfizer in 2018. It is taken by mouth.
Tavapadon acts as a highly selective partial agonist of the dopamine D1 receptor (Ki = 9 nM; IATooltip Intrinsic activity = 65%) and the dopamine D5 receptor (Ki = 13 nM; IA = 81%). It has no significant affinity or functional activity at the D2-like receptors (D2, D3, D4) (Ki ≥ 4,870 to 6,720 nM). Tavapadon also shows biased agonism for Gs-coupled signaling at the D1-like receptors.
As of April 2024, tavapadon is in phase 3 clinical trials for Parkinson's disease.
See also
Mevidalen (LY-3154207)
Razpipadon (CVL-871)
References
Kata Kunci Pencarian:
- Tavapadon
- Cerevel Therapeutics
- L-DOPA
- Prochlorperazine
- Promethazine
- Risperidone
- Dopamine
- Buspirone
- Modafinil
- Cariprazine