Ruboxistaurin

Ruboxistaurin
Clinical data
ATC code	none;
Legal status
Legal status	US: Not FDA approved;
Identifiers
	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;
CAS Number	169939-94-0 ;
PubChem CID	153999;
IUPHAR/BPS	5263;
ChemSpider	135727 ;
UNII	721809WQCP;
ChEMBL	ChEMBL91829 ;
CompTox Dashboard (EPA)	DTXSID00168775 ;
Chemical and physical data
Formula	C28H28N4O3
Molar mass	468.557 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN(C[C@]1([H])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 ;
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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.

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,^[1] with a request for an additional clinical trial, which would take 5 years to complete.^[2] Lilly has not made any further request for approval and ruboxistaurin is not approved by the FDA for any medical use.^[3]

Mechanism of action

Ruboxistaurin is an inhibitor of protein kinase C-beta.^[4]

References

^ "Drugs.com, Eli Lilly and Company Announces Approvable Letter Issued by FDA for Arxxant". Retrieved 2008-02-15.
^ "Drugs.com, Lilly Announces FDA Requirement of Additional Clinical Trial Before Ruboxistaurin Could Be Approved for Treatment of Diabetic Retinopathy". Retrieved 2008-02-15.
^ "Arxxant Approval Status". drugs.com.
^ 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

Eli Lilly and Company Product Pipeline

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[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.

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