Naldemedine
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Systematic (IUPAC) name | |
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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 | Investigational New Drug |
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 |
SMILES
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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.<ref name="Sprawls1997" /[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 May 2012, naldemedine is in phase IIb clinical trials in the United States and Japan.[4]
See also
References
- ↑ 1.0 1.1 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.
- ↑ 2.0 2.1 Shionogi (2009-03-27). "Research and Development at Shionogi (as of March 2009)" (PDF). Retrieved 2012-05-12.
- ↑ Nagase H, Fujii H (2011). "Opioids in preclinical and clinical trials". Topics in Current Chemistry 299: 29–62. PMID 21630515.
- ↑ Shionogi (May 2012). "Pipeline (as of May 2012)" (PDF). Retrieved 2012-05-12.
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