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词条 Ruboxistaurin
释义

  1. Mechanism of action

  2. References

  3. External links

{{Drugbox
| Verifiedfields = changed
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| verifiedrevid = 477855864
| IUPAC_name = (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-di(metheno)dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20-dione
| image = Ruboxistaurin.svg
| image2 = Ruboxistaurin 3D ball.png
| alt2 = Ball-and-stick model of the ruboxistaurin molecule
| tradename =
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| protein_bound =
| metabolism =
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| IUPHAR_ligand = 5263
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 169939-94-0
| ATC_prefix = none
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| PubChem = 153999
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
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| ChemSpiderID = 135727
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 721809WQCP
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 91829
| C=28 | H=28 | N=4 | O=3
| molecular_weight = 468.546 g/mol
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C28H28N4O3/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34)/t18-/m0/s1
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Ruboxistaurin (proposed brand name Arxxant) is an investigational drug for diabetic retinopathy being investigated by Eli Lilly and Company. It is a member of the bisindolylmaleimide family.

On February 2006, Lilly submitted a New Drug Application for ruboxistaurin, and on August 18, 2006, Lilly received an approvable letter from the US FDA for ruboxistaurin,[1] with a request for an additional clinical trial, which would take 5 years to complete.[2]

{{update|date=February 2017}}

Mechanism of action

Ruboxistaurin is an inhibitor of protein kinase C-beta.[3]

References

1. ^{{cite web |url=https://www.drugs.com/nda/arxxant_060818.html |title=Drugs.com, Eli Lilly and Company Announces Approvable Letter Issued by FDA for Arxxant |accessdate=2008-02-15 |work= }}
2. ^{{cite web |url=https://www.drugs.com/nda/arxxant_060929.html |title=Drugs.com, Lilly Announces FDA Requirement of Additional Clinical Trial Before Ruboxistaurin Could Be Approved for Treatment of Diabetic Retinopathy |accessdate=2008-02-15 |work= }}
3. ^{{cite journal |vauthors=Clarke M, Dodson PM |title=PKC inhibition and diabetic microvascular complications |journal=Best Pract Res Clin Endocrinol Metab |volume=21 |issue=4 |pages=573–86 |date=December 2007 |pmid=18054736 |doi=10.1016/j.beem.2007.09.007}}

External links

  • [https://web.archive.org/web/20011217132655/http://investor.lilly.com/pipeline.cfm Eli Lilly and Company Product Pipeline]
{{gastrointestinal-drug-stub}}

2 : Eli Lilly and Company|Bisindolylmaleimides

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