ruboxistaurin

inhibits protein kinase C beta; structure in first source

Also Known As:

13-((dimethylamino)methyl)-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo(e,k)pyrrolo(3,4-h)(1,4,13)oxadiazacyclohexadecene-1,3(2H)-dione; Arxxant; LY 333531; LY-333531; ruboxistaurin mesilate hydrate

Networked: 82 relevant articles (10 outcomes, 29 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Tuttle, Katherine R: 7 articles (04/2015 - 04/2005)
2.	Anderson, Pamela W: 5 articles (04/2015 - 11/2005)
3.	McGill, Janet B: 5 articles (04/2015 - 11/2005)
4.	Aiello, Lloyd Paul: 5 articles (11/2011 - 10/2005)
5.	Sheetz, Matthew J: 5 articles (11/2011 - 12/2006)
6.	Gilbert, Richard E: 5 articles (06/2009 - 08/2005)
7.	Kelly, Darren J: 5 articles (06/2009 - 08/2005)
8.	Bastyr, Edward J: 4 articles (04/2015 - 08/2005)
9.	Davis, Matthew D: 4 articles (11/2011 - 12/2006)
10.	Cox, Alison J: 4 articles (06/2009 - 08/2005)

Related Diseases

1.	Diabetic Retinopathy (Retinopathy, Diabetic) 01/01/2016 - "Although initial studies have indicated that the treatment of diabetic patients with ruboxistaurin, a specific inhibitor of PKCβ, may reduce visual loss in patients with diabetic retinopathy, the overall benefit seems to be small." 11/13/2008 - "Based on secondary analyses of clinical trials in patients with diabetic retinopathy or neuropathy, ruboxistaurin appears safe and may also prevent onset of DKD. " 11/07/2008 - "Data are from a randomized, placebo-controlled trial of ruboxistaurin for vision loss in patients with diabetic retinopathy. " 01/01/2007 - "Previously, results of the PKC-Diabetic Retinopathy Study (PKC-DRS) showed that ruboxistaurin at a dose of 32 mg/day has potential to reduce the risk of moderate vision loss especially in patients with diabetic macular oedema. " 01/01/2007 - "Data from a phase III, 3-year study of ruboxistaurin in patients with moderate to severe diabetic retinopathy showed that ruboxistaurin markedly reduced the risk of sustained vision loss compared with placebo. "
2.	Macular Edema 12/01/2010 - "Effect of ruboxistaurin on the visual acuity decline associated with long-standing diabetic macular edema." 01/01/2009 - "Effect of ruboxistaurin on the visual acuity decline associated with long-standing diabetic macular edema." 10/01/2005 - "Effect of ruboxistaurin on blood-retinal barrier permeability in relation to severity of leakage in diabetic macular edema." 12/01/2006 - "Initial laser treatment for macular edema was 26% less frequent in eyes of ruboxistaurin-treated patients (P = 0.008). " 12/01/2006 - "When clinically significant macular edema was >100 microm from the center of the macula at baseline, ruboxistaurin treatment was associated with less frequent progression of edema to within 100 microm (68% vs. 50%, P = 0.003). "
3.	Atherosclerosis 04/01/2009 - "Significant reduction in atherosclerosis of approximately 2-fold was observed in apoE(-/-) mice fed ruboxistaurin chow (PKCbeta inhibitor) vs. vehicle. " 11/01/2007 - "The aim of this in vitro study was to investigate the effect of ruboxistaurin on glucose-induced adhesion of monocytes to endothelial cells, representing one of the first pivotal steps in the course of atherogenesis. "
4.	Heart Failure 12/09/2011 - "These results provide additional evidence in a large animal model of disease that PKCα/β inhibition (with ruboxistaurin) represents a tenable and novel therapeutic approach for treating human heart failure." 07/17/2009 - "In conclusion, PKCalpha functions distinctly from PKCbeta and PKCgamma in regulating cardiac contractility and heart failure, and broad-acting PKC inhibitors such as ruboxistaurin could represent a novel therapeutic approach in treating human heart failure." 12/01/2017 - "These data suggest that ruboxistaurin represents a potential novel therapeutic for heart failure patients, as a moderate inotrope or therapeutic, which leads to beneficial ventricular remodeling." 12/09/2011 - "We demonstrate that ruboxistaurin administration to a pig model of myocardial infarction-induced heart failure was protective. " 12/09/2011 - "Inhibition of PKCα/β with ruboxistaurin antagonizes heart failure in pigs after myocardial infarction injury."
5.	Mitochondrial Diseases (Mitochondrial Disease) 09/15/2023 - "The administration of Rg1, MDL-28170, LY-333531 and NAC improved mitochondrial dysfunction, oxidative stress and VED, whereas the overexpression of calpain-1 amplified mitochondrial dysfunction, oxidative stress and VED and further upregulated the expression of PKC-β in HAECs exposed to HG. Overexpression of calpain-1 abrogated the protective effect of Rg1 against HG-induced oxidative stress and VED. "

Related Drugs and Biologics

1.	Protein Kinase C beta
2.	Protein Kinase C
3.	Mesylates (Mesylate)
4.	Protein Isoforms (Isoforms)
5.	Salts
6.	Apolipoproteins E (ApoE)
7.	nephrin
8.	calpain inhibitor III
9.	NAD (NADH)
10.	Topiramate (Topamax)

Related Therapies and Procedures

1.	Lasers (Laser)
2.	Therapeutics
3.	Oral Administration
4.	Stents