Ruboxistaurin Chemical formula
Synonyms: LY-333531; LY-341684 (ruboxistaurin mesilate); Ruboxistaurina; Ruboxistaurine; Ruboxistaurinum. (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,19H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4h][1,4,13]oxadiazacyclohexadecene-18,20-dione.
Cyrillic synonym: Рубоксистаурин.

Chemical information

Chemical formula: C28H28N4O3 = 468.5.
CAS — 169939-94-0 (ruboxistaurin); 169939-93-9 mesilate).


Ruboxistaurin is an oral inhibitor of the β-isoform of the enzyme protein kinase C, which is thought to play a role in the development of diabetic microvascular complications. It is under investigation as an adjunct in the treatment of diabetic retinopathy.
1. Joy SV, et al. Ruboxistaurin, a protein kinase C β inhibitor, as an emerging treatment for diabetes microvascular complications. Ann Pharmacother 2005; 39: 1693–9
2. Vinik A. The protein kinase C-
β inhibitor, ruboxistaurin, for the
treatment of diabetic microvascular complications. Expert Opin Invest Drugs 2005; 14: 1547–59
3. The PKC-DRS Study Group. The effect of ruboxistaurin on visual loss in patients with moderately severe to very severe nonproliferative diabetic retinopathy: initial results of the Protein Kinase C
β Inhibitor Diabetic Retinopathy Study (PKC-DRS)
multicenter randomized clinical trial. Diabetes 2005; 54: 2188–97.
Published November 28, 2018.