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Xaliproden
Systematic (IUPAC) name
1-[2-(2-naphthyl)ethyl]-4-[3-(trifluoromethyl)phenyl]-1,2,3,6-tetrahydropyridine
Identifiers
CAS number 135354-02-8
ATC code N07XX03
PubChem 128919
Chemical data
Formula C 24H22F3N 
Mol. mass 381.433 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Xaliproden (codenamed SR57746) is a drug which acts as a 5HT1A agonist.[1] It has neurotrophic and neuroprotective effects in vitro,[2][3] and has been proposed for use in the treatment of several neurodegenerative conditions including amyotrophic lateral sclerosis (ALS)[4] and Alzheimer's disease.[5]

Development of xaliproden for these two indications was discontinued in 2007 following analysis of Phase III data. While the drug did show an effect on hippocampal volume (suggesting perhaps a slowing of cell loss), there was insufficient evidence for efficacy in counteracting Alzheimer's related cognitive decline. Similarly while there were some indicators of efficacy in ALS, including a small but clinically noteworthy effect on some functional parameters, the overall benefit did not reach statistical significance when results across several Phase III trials were averaged. Xaliproden remains under investigation for treatment of peripheral neuropathy associated with chemotherapy.[6][7]

References

  1. ^ Appert-Collin A, Duong FH, Passilly Degrace P, Warter JM, Poindron P, Gies JP. MAPK activation via 5-hydroxytryptamine 1A receptor is involved in the neuroprotective effects of xaliproden. International Journal of Immunopathology and Pharmacology. 2005 Jan-Mar;18(1):21-31. PMID 15698508
  2. ^ Labie C, Lafon C, Marmouget C, Saubusse P, Fournier J, Keane PE, Le Fur G, Soubrié P. Effect of the neuroprotective compound SR57746A on nerve growth factor synthesis in cultured astrocytes from neonatal rat cortex. British Journal of Pharmacology. 1999 May;127(1):139-44. PMID 10369466
  3. ^ Duong FH, Warter JM, Poindron P, Passilly P. Effect of the nonpeptide neurotrophic compound SR 57746A on the phenotypic survival of purified mouse motoneurons. British Journal of Pharmacology. 1999 Dec;128(7):1385-92. PMID 10602316
  4. ^ Meininger V, Bensimon G, Bradley WR, Brooks B, Douillet P, Eisen AA, Lacomblez L, Leigh PN, Robberecht W. Efficacy and safety of xaliproden in amyotrophic lateral sclerosis: results of two phase III trials. Amyotrophic Lateral Sclerosis and Other Motor Neuron Disorders. 2004 Jun;5(2):107-17. PMID 15204012
  5. ^ Lemaire L, Fournier J, Ponthus C, Le Fur Y, Confort-Gouny S, Vion-Dury J, Keane P, Cozzone P (2002). "Magnetic resonance imaging of the neuroprotective effect of xaliproden in rats.". Invest Radiol 37 (6): 321–7. doi:10.1097/00004424-200206000-00003. PMID 12021588.  
  6. ^ Susman E. Xaliproden lessens oxaliplatin-mediated neuropathy. Lancet Oncology. 2006 Apr;7(4):288. PMID 16598880
  7. ^ Wolf S, Barton D, Kottschade L, Grothey A, Loprinzi C. Chemotherapy-induced peripheral neuropathy: prevention and treatment strategies. European Journal of Cancer. 2008 Jul;44(11):1507-15. PMID 18571399
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