Ruboxistaurin

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-[(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
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H28N4O3
Molar mass468.557 g·mol−1
3D model (JSmol)
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 checkY
  • Key:ZCBUQCWBWNUWSU-SFHVURJKSA-N checkY
 ☒NcheckY (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.

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] 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

  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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