Naldemedine

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Naldemedine
Naldemedine.svg
Systematic (IUPAC) name
17-(cyclopropylmethyl)-6,7-didehydro-4,5α-epoxy-3,6,14-trihydroxy-N-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]morphinan-7-carboxamide
Clinical data
Legal status
Routes Oral
Identifiers
CAS number 916072-89-4
1345728-04-2 (tosylate)
ATC code None
PubChem CID 135626906
Chemical data
Formula C32H34N4O6 
Mol. mass 570.63556 g/mol

Naldemedine (INN, USAN; S-297,995) is a peripherally-selective μ-opioid receptor antagonist under development by Shionogi for the treatment of opioid-induced adverse effects including constipation, nausea, and vomiting.[1][2][3] Clinical studies have thus far found it to possess statistically significant effectiveness for these indications and to be generally well-tolerated with predominantly mild to moderate gastrointestinal side effects.[2] No effects indicative of central opioid withdrawal or impact on the analgesic or mydriatic effects of co-administered opioids have been observed.[1] As of July 2014, naldemedine is in phase III clinical trials in the United States and Japan.

See also[edit]

References[edit]

  1. ^ a b De Sarro, Giovambattista; Kelly S. Sprawls; Egilius L.H. Spierings; Dustin Tran (2012-03-07). "Drugs in Development for Opioid-Induced Constipation". In Catto-Smith G., Anthony. Constipation - Causes, Diagnosis and Treatment. p. 7. doi:10.5772/30377. ISBN 978-953-51-0237-3. Retrieved 12 May 2012. 
  2. ^ a b Shionogi (2009-03-27). "Research and Development at Shionogi (as of March 2009)" (PDF). Retrieved 2012-05-12. 
  3. ^ Nagase H, Fujii H (2011). "Opioids in preclinical and clinical trials". Topics in Current Chemistry 299: 29–62. doi:10.1007/128_2010_74. PMID 21630515.