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Protein Kinase C- ( PKC- ) Inhibition: A Promise not yet Fulfilled - PowerPoint PPT Presentation

Sep 29, 2023 •279 likes •415 views

Protein Kinase C- ( PKC- ) Inhibition: A Promise not yet Fulfilled Ruboxistaurin, an oral PKC- , was withdrawn on March 15, 2007 by Eli Lilly Dual Inhibition of Classical Protein Kinase C- and Protein Kinase C- Isoforms Protects

  1. Protein Kinase C- β ( PKC- β ) Inhibition: A Promise not yet Fulfilled Ruboxistaurin, an oral PKC- β, was withdrawn on March 15, 2007 by Eli Lilly

  2. Dual Inhibition of Classical Protein Kinase C- α and Protein Kinase C- β Isoforms Protects Against Diabetic Nephropathy Diabetes 2013;62:1010-1011

  3. ASCEND Trial: Endothelin Receptor Antagonist Avosentan Significantly Decreased Albuminuria Terminated due to increased CHF and deaths J Am Soc Nephrol 2010;21:527–535

  4. Addition of Atrasentan, an Endothelin Receptor Antagonist, to RAS Blockade Reduces Albuminuria in Diabetic Nephropathy Baseline UACR ~400 mg/g CR J Am Soc Nephrol 2011;22:763-772

  5. Atrasentan Restores Endothelial Glycocalyx Thickness Diabetes 2016;65:2429-2439

  6. Pirfenidone, an Inhibitor of TGF- β at 1200 mg/d, but NOT 2400 mg/d, Improves eGFR from Baseline Pirfenidone (Esbriet) approved to treat idiopathic pulmonary fibrosis J Am Soc Nephrol 2011;22:1144–1151

  7. Pentoxifylline-Lower Decline in eGFR and Greater UAE Reduction Baseline UAE ~1000 mg/day J Am Soc Nephrol 2015;26:220–229

  8. CCX140-B (CCR2 Antagonist) Lowers Albuminuria in Patients with Type 2 DM Monocyte chemoattractant protein-1 (MCP-1), also called C-C chemokine receptor 2 (CCR2) Baseline UAE 400 mg/day Lancet Diabetes & Endo 2015;3:687-696

  9. Pyridoxamine (Pyridorin), a Derivative of Vitamin B6, Inhibits the Formation of Advanced Glycation Endproducts I.V. form of Pyridorin for use in hospital-acquired acute kidney injury Nephron 2015;129:22–28

  10. Finerenone, a 3 rd Generation Nonsteroidal Mineralocorticoid Receptor Antagonists Lowers Albuminuria Baseline UACR ~200 mg/g CR JAMA 2015;314:884-894

  11. Patiromer (Veltassa)— Twice Daily Lowered Potassium Levels FDA Approved on October 22, 2015 but with a Black Box Warning N Engl J Med 2015;372:211-221

  12. Sodium Zirconium Cyclosilicate (ZS-9) 3X Daily X2 days ↓ Hyperkalemia AstraZeneca receives Complete Response Letter from FDA May 27, 2016 JAMA 2014;312:2223-2233

  13. Metformin Improves Whole-Body Glycocalyx Barrier Properties Cardiovasc Diabetol 2013;12:175

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