Tozadenant

Last updated

Tozadenant
Tozadenant.svg
Clinical data
Other namesRO4494351; RO-4494351; SYN-115; SYN115
Routes of
administration 		Oral [1]
Drug class Adenosine A2A receptor antagonist; Antiparkinsonian agent
ATC code
  • None
Pharmacokinetic data
Elimination half-life 15 hours [2]
Identifiers
  • 4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
Chemical and physical data
Formula C19H26N4O4S
Molar mass 406.50 g·mol−1
3D model (JSmol)
  • CC1(CCN(CC1)C(=O)NC2=NC3=C(C=CC(=C3S2)N4CCOCC4)OC)O
  • InChI=1S/C19H26N4O4S/c1-19(25)5-7-23(8-6-19)18(24)21-17-20-15-14(26-2)4-3-13(16(15)28-17)22-9-11-27-12-10-22/h3-4,25H,5-12H2,1-2H3,(H,20,21,24)
  • Key:XNBRWUQWSKXMPW-UHFFFAOYSA-N

Tozadenant (INN Tooltip International Nonproprietary Name, USAN Tooltip United States Adopted Name; developmental code names RO4494351 and SYN-115) is an adenosine A2A receptor antagonist which was under development for the treatment of Parkinson's disease and liver disorders but was never marketed due to safety concerns. [1] [3] It is taken orally. [1] Tozadenant was under development by Roche, Acorda Therapeutics, and Biotie Therapies. [1] It reached phase 3 clinical trials for Parkinson's disease prior to the discontinuation of its development. [1] The development of tozadenant was discontinued due to findings of agranulocytosis and associated serious adverse effects in clinical trials including five patient deaths. [1] [4] [5]

See also

References

  1. 1 2 3 4 5 6 "Acorda Therapeutics". AdisInsight. 5 November 2023. Retrieved 28 January 2026.
  2. ↑ Mancel V, Mathy FX, Boulanger P, English S, Croft M, Kenney C, et al. (August 2017). "Pharmacokinetics and metabolism of [14C]-tozadenant (SYN-115), a novel A2a receptor antagonist ligand, in healthy volunteers". Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 47 (8): 705–718. doi:10.1080/00498254.2016.1221164. PMID   27489076.
  3. ↑ Perez-Lloret S, Merello M (June 2014). "Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant". Expert Opinion on Pharmacotherapy. 15 (8): 1097–1107. doi:10.1517/14656566.2014.903924. PMID   24673462.
  4. ↑ Taylor P (15 November 2017). "Acorda slumps on safety fears for Parkinson's drug tozadenant". Fierce Biotech. Retrieved 28 January 2026.
  5. ↑ Taylor NP (20 November 2017). "Acorda dumps $363M Parkinson's drug after patient deaths". Fierce Biotech. Retrieved 28 January 2026.
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