Arbaclofen placarbil

Arbaclofen placarbil (/ɑːrˈbækloʊfɛn pləˈkɑːrbɪl/ ar-BAK-loh-fen plə-KAR-bil, also known as XP19986) is a prodrug of R-baclofen. Arbaclofen placarbil possesses more favorable pharmacokinetic profile than baclofen, with less fluctuations in plasma drug levels. It was being developed as a potential treatment for patients with GERD and spasticity due to multiple sclerosis; however, in May 2013 XenoPort announced the termination of development because of unsuccessful results in phase III clinical trials.[1]

Arbaclofen placarbil
Clinical data
Pregnancy
category
  • N/A
ATC code
  • none
Legal status
Legal status
  • Development terminated
Identifiers
IUPAC name
  • (3R)-3-(4-chlorophenyl)-4-[[[(1S)-2-methyl-1-[(2-methylpropanoyl)oxy]propoxy]carbonyl]amino]butanoic acid
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.221.150
Chemical and physical data
FormulaC19H26ClNO6
Molar mass399.87 g·mol−1
3D model (JSmol)
SMILES
  • CC(C)C(=O)O[C@@H](OC(=O)NC[C@H](CC(=O)O)c1ccc(Cl)cc1)C(C)C
InChI
  • InChI=1S/C19H26ClNO6/c1-11(2)17(24)26-18(12(3)4)27-19(25)21-10-14(9-16(22)23)13-5-7-15(20)8-6-13/h5-8,11-12,14,18H,9-10H2,1-4H3,(H,21,25)(H,22,23)/t14-,18-/m0/s1
  • Key:JXTAALBWJQJLGN-KSSFIOAISA-N

It is being developed as an addiction medicine to treat alcoholism. [2] It is also studied as a potential therapeutic for some autistic subjects.[3]

See also

References
  1. "XenoPort Reports Top-Line Results of Phase 3 Trial of Arbaclofen Placarbil for Spasticity in Multiple Sclerosis Patients". XenoPort, Inc. May 20, 2013. Archived from the original on 2013-12-02. Retrieved 2013-06-03.
  2. Anderson E (3 July 2020). "Pill that replaces alcohol aims to end 'glass of wine' craving". The i newspaper. Associated Newspapers Limited.
  3. Huang, Qiyun; Pereira, Andreia C.; Velthuis, Hester; Wong, Nichol M. L.; Ellis, Claire L.; Ponteduro, Francesca M.; Dimitrov, Mihail; Kowalewski, Lukasz; Lythgoe, David J.; Rotaru, Diana; Edden, Richard A. E.; Leonard, Alison; Ivin, Glynis; Ahmad, Jumana; Pretzsch, Charlotte M.; Daly, Eileen; Murphy, Declan G. M.; McAlonan, Gráinne M. (2022-01-05). "GABAB receptor modulation of visual sensory processing in adults with and without autism spectrum disorder". Science Translational Medicine. 14 (626): eabg7859. doi:10.1126/scitranslmed.abg7859. PMID 34985973. S2CID 245771626.


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