Merimepodib
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| Non-proprietary name | Merimepodib | |||||||||||||||
| other names |
N -3- (3- [3-Methoxy-4- (oxazol-5-yl) phenyl] ureido) benzylcarbamic acid ( S ) -tetrahydrofuran-3-yl ester ( IUPAC ) |
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| Molecular formula | C 23 H 24 N 4 O 6 | |||||||||||||||
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| Drug information | ||||||||||||||||
| Drug class |
Inosine monophosphate dehydrogenase inhibitor with antiviral effect |
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| properties | ||||||||||||||||
| Molar mass | 452.51 g · mol -1 | |||||||||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||
Merimepodib is an experimental drug, the effectiveness of which was claimed in clinical studies as an additional agent to the then existing peginterferon α / ribavirin therapy in the treatment of hepatitis C in the 2000s .
Merimepodib selectively inhibits cellular inosine monophosphate dehydrogenase (IMPDH). It has no specific antiviral effect and no viral protein as a target, but a certain effect in combination with ribavirin on cell cultures containing HCV replicon . In a larger study with 286 patients, it showed no effect or additional benefit in treatment-resistant patients. Since the introduction of the highly effective, direct antiviral agent (DAA ) drugs for the treatment of hepatitis C, its use has become obsolete.
Chemical information
The ( S ) -configured enantiomer is used in pharmaceuticals .
patent
The patent is held by Vertex Pharmaceuticals Inc., Cambridge MA. The patent number of the synthesis is US5807876.
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ Marcellin P., ea: Phase 2 study of the combination of merimepodib with peginterferon-alpha2b, and ribavirin in nonresponders to previous therapy for chronic hepatitis C. In: J Hepatol . 2007 Oct; 47 (4): 476-483, PMID 17629590 .
- ↑ VK Rusti et al .: Merimepodib, pegylated interferon, and ribavirin in genotype 1 chronic hepatitis C pegylated interferon and ribavirin nonresponders. Hepatology (2009) 50 (6): pp. 1719-1726 PMID 19852040
- ↑ www.patents.com: Inhibitors of IMPDH enzyme - ID: US5807876.
literature
synthesis
- Stamos, Bethiel: In: PCT Int. Appl . 2001., p. 63 pp.
pharmacology
- Decker, Heiser, Chaturvedi, Faust, Ku, Moseley, Nimmesgern :. In: Drugs under Experimental and Clinical Research . 27./3., 2001, pp. 89-95
- Markland et al .: In: Antimicrobial Agents and Chemotherapy . 44./4., Pp. 859-866.
- Jain et al .: In J. Pharm. Sci. 90./5., 2001, pp. 625-637
