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Tavapadon

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 December 2024, tavapadon has completed phase 3 clinical trials for Parkinson's disease.

See also List of investigational Parkinson's disease drugs Glovadalen (UCB-0022) Mevidalen (LY-3154207) PF-06412562 (CVL-562) Razpipadon (CVL-871)

References

Tags

  • Biased ligands
  • D1 receptor agonists
  • D5 receptor agonists
  • Diketones
  • Experimental drugs
  • Nervous system drug stubs
  • Pyridines
  • Pyrimidines
  • Trifluoromethyl compounds