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{{Short description|Chemical compound}} |
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{{Drugbox |
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{{Drugbox |
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| verifiedrevid = 333634406 |
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| IUPAC_name = (9''S'')-9--6,7,10,11-tetrahydro-9''H'',18''H''-5,21:12,17-di(metheno)dibenzopyrrolooxadiazacyclohexadecine-18,20-dione |
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| verifiedrevid = 477855864 |
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| image = Ruboxistaurin.svg |
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| IUPAC_name = (9''S'')-9--6,7,10,11-tetrahydro-9''H'',18''H''-5,21:12,17-di(metheno)dibenzopyrrolooxadiazacyclohexadecine-18,20-dione |
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| CAS_number = 169939-94-0 |
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| image = Ruboxistaurin.svg |
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| ATC_prefix = none |
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| image2 = Ruboxistaurin 3D ball.png |
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| ATC_suffix = |
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| alt2 = Ball-and-stick model of the ruboxistaurin molecule |
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| PubChem = 153999 |
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<!--Clinical data--> |
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| ChemSpiderID = 135727 |
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| tradename = |
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| SMILES = O=C6NC(=O)C=5c1cn(c2ccccc12)CCO(CN(C)C)CCn4c3ccccc3c(c4)C=56 |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| 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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| pregnancy_US = <!-- A / B / C / D / X --> |
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| StdInChIKey = ZCBUQCWBWNUWSU-SFHVURJKSA-N |
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| pregnancy_category = |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> |
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| legal_US = Not FDA approved |
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| legal_status = |
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| routes_of_administration = |
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<!--Pharmacokinetic data--> |
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| bioavailability = |
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| protein_bound = |
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| metabolism = |
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| elimination_half-life = |
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| excretion = |
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<!--Identifiers--> |
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| IUPHAR_ligand = 5263 |
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| CAS_number_Ref = {{cascite|changed|??}} |
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| CAS_number = 169939-94-0 |
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| ATC_prefix = none |
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| ATC_suffix = |
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| PubChem = 153999 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 135727 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 721809WQCP |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL = 91829 |
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| ChEMBL = 91829 |
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| DrugBank = |
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| C = 28 |H = 28 |N = 4 |O = 3 |
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| molecular_weight = 468.546 ]/] |
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| bioavailability = |
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| metabolism = |
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| elimination_half-life = |
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| excretion = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category= |
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| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 --> |
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| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C --> |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = |
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| routes_of_administration = |
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}} |
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'''Ruboxistaurin''' (proposed brand name '''Arxxant''') is an investigational drug for diabetic peripheral retinopathy. It is currently being investigated by ]. |
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<!--Chemical data--> |
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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> |
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| C=28 | H=28 | N=4 | O=3 |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| 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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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = ZCBUQCWBWNUWSU-SFHVURJKSA-N |
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|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}} |
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'''Ruboxistaurin''' (proposed brand name '''Arxxant''') is an investigational drug for ] being investigated by ]. It is a member of the ] family. |
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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> |
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==Mechanism of action== |
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==Mechanism of action== |
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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> |
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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> |
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==References== |
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==References== |
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==External links== |
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==External links== |
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{{pharma-stub}} |
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{{gastrointestinal-drug-stub}} |
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