LY 333531 mesylate - CAS 192050-59-2
Category: Inhibitor
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LY 333531 mesylate is an orally-available protein kinase C β (PKC-β) specific inhibitor used for the treatment of diabetic nephropathy and diabetic macular edema.
Brife Description:
PKC-β inhibitor
LY 333531 mesylate; LY333531 mesylate; LY-333531 mesylate; Ruboxistaurin mesylate; (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione mesylate
the treatment of diabetic nephropathy and diabetic macular edema
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1.PKC-B inhibition: a new therapeutic approach for diabetic complications?
Avignon A;Sultan A Diabetes Metab. 2006 Jun;32(3):205-13.
PKC comprises a superfamily of isoenzymes that is activated in response to various stimuli. Hyperglycaemia induces the activation of different PKC isoforms. However, the PKC-B isoform appears to be preferentially activated by high glucose levels and has been shown to be associated with diabetic vascular complications. In vitro and in vivo animal studies have shown that ruboxistaurin mesylate, a novel selective inhibitor of PKC-B ameliorates the biochemical and functional consequences of PKC activation and may have the potential to reduce the burden of vascular complications associated with diabetes. Results of the first phase-II and phase-III trials evaluating the efficacy of this compound on diabetic microvascular complications have been published recently. They confirm that this compound may favorably influence the evolution of diabetic microvascular complications.
2.Treatment of symptomatic diabetic peripheral neuropathy with the protein kinase C beta-inhibitor ruboxistaurin mesylate during a 1-year, randomized, placebo-controlled, double-blind clinical trial.
Vinik AI;Bril V;Kempler P;Litchy WJ;Tesfaye S;Price KL;Bastyr EJ 3rd;MBBQ Study Group Clin Ther. 2005 Aug;27(8):1164-80.
OBJECTIVE: ;The aim of this study was to assess the effects of ruboxistaurin (RBX) mesylate on nerve function and sensory symptoms in patients with diabetes mellitus (DM) and diabetic peripheral neuropathy (DPN).;METHODS: ;Patients were enrolled in a multinational, randomized, Phase II, double-blind, placebo-controlled parallel-group trial comparing 32 mg/d or 64 mg/d RBX with placebo for 1 year. DPN was identified by abnormal measurable vibration detection threshold (VDT) and verified by abnormal neurologic examination and nerve electrophysiology measures. Baseline patient characteristics (eg, sex, type of DM, age, body mass index, glycosylated hemoglobin, and duration of DM and DPN) were measured. The primary end point was the change in VDT. Secondary end point measures included effects of RBX versus placebo on Neuropathy Total Symptom Score-6 (NTSS-6), neurologic examination, electrophysiologic nerve conduction studies, Neuropathy Impairment Score, Clinical Global Impressions, and safety. A post-hoc analysis was performed on patients with less severe DPN (sural sensory nerve action potential > or =0.5 microV and NTSS-6 total score >6).;RESULTS: ;Two hundred five patients were assessed: 66 were assigned to the RBX 32 mg/d group, 71 to the RBX 64 mg/d group, and 68 to the placebo group.
3.Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications.
Joy SV;Scates AC;Bearelly S;Dar M;Taulien CA;Goebel JA;Cooney MJ Ann Pharmacother. 2005 Oct;39(10):1693-9. Epub 2005 Sep 13.
OBJECTIVE: ;To review current clinical data regarding the pharmacologic actions of ruboxistaurin (LY333531) mesylate, an inhibitor of protein kinase C (PKC) beta, and its role to potentially reduce the development and/or the progression of diabetic microvascular complications.;DATA SOURCES: ;Primary literature was obtained via a MEDLINE search (1966-August 2004) and through review of pertinent abstracts and presentations at major medical meetings.;STUDY SELECTION AND DATA EXTRACTION: ;Literature relevant to PKC physiology, the pharmacokinetics of ruboxistaurin, and data evaluating the use of ruboxistaurin in treating diabetic microvascular complications in human and relevant animal models was reviewed.;DATA SYNTHESIS: ;PKC is part of a group of intracellular signaling molecules activated in response to various specific hormonal, neuronal, and growth factor stimuli. Hyperglycemia leads to PKC beta 1 and 2 isoform activation, which experimentally has been shown to contribute to the development and progression of diabetic microvascular complications (retinopathy, nephropathy, neuropathy) through various biochemical mechanisms. Animal and/or human studies using ruboxistaurin mesylate, a novel, highly selective inhibitor of PKC beta, have shown delay in the progression and, in some cases, reversal of diabetic retinopathy, nephropathy, and neuropathy.
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CAS 192050-59-2 LY 333531 mesylate

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