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Revision as of 19:18, 20 October 2011 editCheMoBot (talk | contribs)Bots141,565 edits Updating {{drugbox}} (changes to verified fields - updated 'ChEBI_Ref', 'KEGG_Ref', 'CAS_number_Ref') per Chem/Drugbox validation (report errors or bugs)← Previous edit Latest revision as of 19:34, 20 December 2023 edit undoJJMC89 bot III (talk | contribs)Bots, Administrators3,688,880 editsm Moving Category:Eli Lilly and Company brands to Category:Drugs developed by Eli Lilly and Company per Misplaced Pages:Categories for discussion/Log/2023 December 9#Category:AstraZeneca brands 
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{{Short description|Chemical compound}}
{{Drugbox {{Drugbox
| Verifiedfields = changed | Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 431680053 | verifiedrevid = 477855864
| IUPAC_name = (9''S'')-9--6,7,10,11-tetrahydro-9''H'',18''H''-5,21:12,17-di(metheno)dibenzopyrrolooxadiazacyclohexadecine-18,20-dione | IUPAC_name = (9''S'')-9--6,7,10,11-tetrahydro-9''H'',18''H''-5,21:12,17-di(metheno)dibenzopyrrolooxadiazacyclohexadecine-18,20-dione
| image = Ruboxistaurin.svg | image = Ruboxistaurin.svg
| image2 = Ruboxistaurin 3D ball.png

| alt2 = Ball-and-stick model of the ruboxistaurin molecule
<!--Clinical data--> <!--Clinical data-->
| tradename = | tradename =
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> | legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> | legal_UK = <!-- GSL / P / POM / CD / Class A, B, C -->
| legal_US = Not FDA approved
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status = | legal_status =
| routes_of_administration = | routes_of_administration =


<!--Pharmacokinetic data--> <!--Pharmacokinetic data-->
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| metabolism = | metabolism =
| elimination_half-life = | elimination_half-life =
| excretion = | excretion =


<!--Identifiers--> <!--Identifiers-->
| IUPHAR_ligand = 5263
| CAS_number_Ref = {{cascite|correct|??}} | CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 169939-94-0 | CAS_number = 169939-94-0
| ATC_prefix = none | ATC_prefix = none
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 135727 | ChemSpiderID = 135727
| UNII_Ref = {{fdacite|changed|FDA}} | UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 721809WQCP | UNII = 721809WQCP
| ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL_Ref = {{ebicite|correct|EBI}}
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<!--Chemical data--> <!--Chemical data-->
| C=28 | H=28 | N=4 | O=3 | C=28 | H=28 | N=4 | O=3
| molecular_weight = 468.546 ]/]
| StdInChI_Ref = {{stdinchicite|correct|chemspider}} | 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 | 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = ZCBUQCWBWNUWSU-SFHVURJKSA-N | StdInChIKey = ZCBUQCWBWNUWSU-SFHVURJKSA-N
|drug_name=|alt=|caption=|type=|MedlinePlus=|licence_EU=|licence_US=|SMILES=CN(C1()CCN2C=C(C(C(O)=NC3=O)=C3C(C4=CC=CC=C45)=CN5CCO1)C6=CC=CC=C62)C}}
}}
'''Ruboxistaurin''' (proposed brand name '''Arxxant''') is an investigational drug for diabetic peripheral retinopathy. It is currently being investigated by ]. '''Ruboxistaurin''' (proposed brand name '''Arxxant''') is an investigational drug for ] being investigated by ]. It is a member of the ] family.


On February, 2006, Lilly submitted a New Drug Application for ruboxistaurin, and on August 18, 2006, Lilly received an "approvable" letter from the ] ] for ruboxistaurin,<ref>{{cite web |url=http://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 |format= |work= }}</ref> with a request for an additional clinical trial, which would take 5 years to complete.<ref>{{cite web |url=http://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 |format= |work= }}</ref> In February 2006, Lilly submitted a ] for ruboxistaurin, and on August 18, 2006, Lilly received an ] from the ] for ruboxistaurin,<ref>{{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 }}</ref> with a request for an additional ], which would take 5 years to complete.<ref>{{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 }}</ref> Lilly has not made any further request for approval and ruboxistaurin is not approved by the FDA for any medical use.<ref>{{Cite web | title= Arxxant Approval Status | url = https://www.drugs.com/history/arxxant.html | publisher = ] }}</ref>


==Mechanism of action== ==Mechanism of action==
Ruboxistaurin is an inhibitor of ]-beta.<ref>{{cite journal |author=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 |year=2007 |month=December |pmid=18054736 |doi=10.1016/j.beem.2007.09.007}}</ref> Ruboxistaurin is an inhibitor of ]-beta.<ref>{{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}}</ref>


==References== ==References==
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==External links== ==External links==
* *



] ]
] ]
] ]




Latest revision as of 19:34, 20 December 2023

Chemical compound Pharmaceutical compound
Ruboxistaurin
Ball-and-stick model of the ruboxistaurin molecule
Clinical data
ATC code
  • none
Legal status
Legal status
  • US: Not FDA approved
Identifiers
IUPAC name
  • (9S)-9--6,7,10,11-tetrahydro-9H,18H-5,21:12,17-di(metheno)dibenzopyrrolooxadiazacyclohexadecine-18,20-dione
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H28N4O3
Molar mass468.557 g·mol
3D model (JSmol)
SMILES
  • CN(C1()CCN2C=C(C(C(O)=NC3=O)=C3C(C4=CC=CC=C45)=CN5CCO1)C6=CC=CC=C62)C
InChI
  • InChI=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
  • Key:ZCBUQCWBWNUWSU-SFHVURJKSA-N
  (what is this?)  (verify)

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.

In 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, with a request for an additional clinical trial, which would take 5 years to complete. Lilly has not made any further request for approval and ruboxistaurin is not approved by the FDA for any medical use.

Mechanism of action

Ruboxistaurin is an inhibitor of protein kinase C-beta.

References

  1. "Drugs.com, Eli Lilly and Company Announces Approvable Letter Issued by FDA for Arxxant". Retrieved 2008-02-15.
  2. "Drugs.com, Lilly Announces FDA Requirement of Additional Clinical Trial Before Ruboxistaurin Could Be Approved for Treatment of Diabetic Retinopathy". Retrieved 2008-02-15.
  3. "Arxxant Approval Status". drugs.com.
  4. Clarke M, Dodson PM (December 2007). "PKC inhibition and diabetic microvascular complications". Best Pract Res Clin Endocrinol Metab. 21 (4): 573–86. doi:10.1016/j.beem.2007.09.007. PMID 18054736.

External links


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