PSI-6130: Difference between revisions

PSI-6130
Clinical data
ATC code	none;
Identifiers
	IUPAC name 4-Amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyrimidin-2(1H)-one;
CAS Number	817204-33-4;
UNII	05J68784G1;
CompTox Dashboard (EPA)	DTXSID10231287 ;
Chemical and physical data
Formula	C10H14FN3O4
Molar mass	259.23 g/mol g·mol−1
	(verify)

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Revision as of 21:55, 21 September 2011

PSI-6130 is an experimental treatment for hepatitis C. PSI-6130 is a member of a class of antiviral drugs known as nucleoside polymerase inhibitors that was created by chemist Jeremy L. Clark.^[1] Specifically, PSI-6130 inhibits the hepatitis C virus NS5B RNA dependant RNA polymerase.^[2]

PSI-6130 is currently being developed by Hoffmann–La Roche as a 3',5'-diisobutyrl ester prodrug, R7128.^[3] R7128 is part of the combination of all-oral agents clinical trial known as INFORM-1.^[4]^{[unreliable source?]}

References

^ Clark, J.; et al. (2005). "Design, synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'C-methylcytidine, a potent inhibitor of hepatitis C virus replication". Journal of Medicinal Chemistry. 48 (17): 5504. doi:10.1021/jm0502788. PMID 16107149. {{cite journal}}: Explicit use of et al. in: |author= (help)
^ Lieven J Stuyver, Tamara R McBrayer, Phillip M Tharnish, Jeremy Clark, Laurent Hollecker; et al. (2006). "Inhibition of hepatitis C replicon RNA synthesis by beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: a specific inhibitor of hepatitis C virus replication". Antiviral Chemistry & Chemotherapy. 17 (2): 79–87. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
^ Cole, P.; Castaner, R.; Bolos, J. (2009). "R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection". Drugs of the Future. 34 (4): 282–290.{{cite journal}}: CS1 maint: multiple names: authors list (link)
^ "INFORM-1 (R7227 and R7128) study".

[1] Clark, J.; et al. (2005). "Design, synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'C-methylcytidine, a potent inhibitor of hepatitis C virus replication". Journal of Medicinal Chemistry. 48 (17): 5504. doi:10.1021/jm0502788. PMID 16107149. {{cite journal}}: Explicit use of et al. in: |author= (help)

[2] Lieven J Stuyver, Tamara R McBrayer, Phillip M Tharnish, Jeremy Clark, Laurent Hollecker; et al. (2006). "Inhibition of hepatitis C replicon RNA synthesis by beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: a specific inhibitor of hepatitis C virus replication". Antiviral Chemistry & Chemotherapy. 17 (2): 79–87. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)

[3] Cole, P.; Castaner, R.; Bolos, J. (2009). "R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection". Drugs of the Future. 34 (4): 282–290.{{cite journal}}: CS1 maint: multiple names: authors list (link)

[4] "INFORM-1 (R7227 and R7128) study".

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 '''PSI-6130''' is an experimental treatment for [[hepatitis C]]. PSI-6130 is a member of a class of [[antiviral drug]]s known as [[nucleoside polymerase]] [[enzyme inhibitor|inhibitors]] that was created by chemist Jeremy L. Clark.<ref>{{cite journal | journal = Journal of Medicinal Chemistry | year = 2005 | volume = 48 | issue = 17 | pages = 5504 | pmid = 16107149 | title = Design, synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'C-methylcytidine, a potent inhibitor of hepatitis C virus replication | author = Clark, J., et. al. | url = http://pubs.acs.org/doi/abs/10.1021/jm0502788?prevSearch=%255Bauthor%253A%2Bjeremy%2Bl.%2Bclark%255D&searchHistoryKey= | doi = 10.1021/jm0502788}}</ref>  Specifically, PSI-6130 inhibits the hepatitis C virus NS5B RNA dependant RNA polymerase.<ref>{{cite journal | journal = Antiviral Chemistry & Chemotherapy | year = 2006 | volume = 17 | issue = 2 | pages = 79–87 | title = Inhibition of hepatitis C replicon RNA synthesis by beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: a specific inhibitor of hepatitis C virus replication | author = Lieven J Stuyver, Tamara R McBrayer, Phillip M Tharnish, Jeremy Clark, Laurent Hollecker, et. al. | url = http://www.intmedpress.com/serveFile.cfm?sUID=01f7cbfd-f36a-4ff5-ba6e-3eab3035fa55 }}</ref>
-PSI-6130 is currently being developed by [[Hoffmann–La Roche]] as a 3',5'-diisobutyrl ester prodrug, R7128.<ref>{{cite journal |author=Cole, P.; Castaner, R.; Bolos, J. |title=R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection  |journal=Drugs of the Future |volume=34 |issue=4 |pages=282–290 |year=2009 |url=http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=1367744&p_IsPs=N}}</ref>  R7128 is part of the combination of all-oral agents clinical trial known as INFORM-1.<ref>{{cite web | title = INFORM-1 (R7227 and R7128) study | url = http://www.medhelp.org/posts/Hepatitis-C/INFORM-1-R7227-and-R7128-study/show/935635}}</ref>{{Verify credibility|date=September 2010}}
+PSI-6130 is currently being developed by [[Hoffmann–La Roche]] as a 3',5'-diisobutyrl ester prodrug, R7128.<ref>{{cite journal |author=Cole, P.; Castaner, R.; Bolos, J. |title=R-7128: RNA-directed RNA polymerase (NS5B) inhibitor treatment of hepatitis C virus infection  |journal=Drugs of the Future |volume=34 |issue=4 |pages=282–290 |year=2009 |url=http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=1367744&p_IsPs=N}}</ref>  R7128 is part of the combination of all-oral agents clinical trial known as INFORM-1.<ref>{{cite web | title = INFORM-1 (R7227 and R7128) study | url = http://www.roche-trials.com/trialDetailsGet.action?studyNumber=PP22205}}</ref>{{Verify credibility|date=September 2010}}
 ==References==