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Indantadol

Indantadol
Indantadol.svg
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
ChemSpider
UNII
Chemical and physical data
FormulaC11H14N2O
Molar mass190.24 g/mol g·mol−1
3D model (JSmol)

Indantadol (CHF-3381, V-3381) is a drug which was formerly being investigated as an anticonvulsant and neuroprotective and is now under development for the treatment of neuropathic pain and chronic cough in Europe by Vernalis and Chiesi.[1][2][3][4][5][6][7][8] It acts as a competitive, reversible, and non-selective monoamine oxidase inhibitor,[5][6][9] and as a low affinity, non-competitive NMDA receptor antagonist.[1][2][10] A pilot study of indantadol for chronic cough was initiated in October 2009 and in April 2010 it failed to achieve significant efficacy in neuropathic pain in phase IIb clinical trials.[7][8][11][12]

See also

References

  1. ^ a b Villetti G, Bregola G, Bassani F, et al. (June 2001). "Preclinical evaluation of CHF3381 as a novel antiepileptic agent". Neuropharmacology. 40 (7): 866–78. doi:10.1016/S0028-3908(01)00026-0. PMID 11378157.
  2. ^ a b Gandolfi O, Bonfante V, Voltattorni M, et al. (September 2001). "Anticonvulsant preclinical profile of CHF 3381: dopaminergic and glutamatergic mechanisms". Pharmacology Biochemistry and Behavior. 70 (1): 157–66. doi:10.1016/S0091-3057(01)00591-3. PMID 11566153.
  3. ^ Zucchini S, Buzzi A, Bergamaschi M, Pietra C, Villetti G, Simonato M (November 2002). "Neuroprotective activity of CHF3381, a putative N-methyl-D-aspartate receptor antagonist". NeuroReport. 13 (16): 2071–4. doi:10.1097/00001756-200211150-00016. PMID 12438928.
  4. ^ Villetti G, Bergamaschi M, Bassani F, et al. (August 2003). "Antinociceptive activity of the N-methyl-D-aspartate receptor antagonist N-(2-Indanyl)-glycinamide hydrochloride (CHF3381) in experimental models of inflammatory and neuropathic pain". The Journal of Pharmacology and Experimental Therapeutics. 306 (2): 804–14. doi:10.1124/jpet.103.050039. PMID 12750440.
  5. ^ a b "CHF 3381". Drugs in R&D. 5 (1): 28–30. 2004. doi:10.2165/00126839-200405010-00005. PMID 14725488.
  6. ^ a b Mattia C, Coluzzi F (September 2007). "Indantadol, a novel NMDA antagonist and nonselective MAO inhibitor for the potential treatment of neuropathic pain". IDrugs : The Investigational Drugs Journal. 10 (9): 636–44. PMID 17786847.
  7. ^ a b "IN-STEP Phase IIb study results".
  8. ^ a b "Vernalis initiates Pilot Study of V3381 in patients with chronic cough".
  9. ^ Mathiesen O, Imbimbo BP, Hilsted KL, Fabbri L, Dahl JB (August 2006). "CHF3381, a N-methyl-D-aspartate receptor antagonist and monoamine oxidase-A inhibitor, attenuates secondary hyperalgesia in a human pain model". The Journal of Pain. 7 (8): 565–74. doi:10.1016/j.jpain.2006.02.004. PMID 16885013.
  10. ^ Barbieri M, Bregola G, Buzzi A, et al. (August 2003). "Mechanisms of action of CHF3381 in the forebrain". British Journal of Pharmacology. 139 (7): 1333–41. doi:10.1038/sj.bjp.0705381. PMC 1573965. PMID 12890713.
  11. ^ "V3381CC".
  12. ^ "Vernalis completes recruitment in V3381 Phase II IN-STEP study for neuropathic pain".