GENEVA, Switzerland & ARCHAMPS, France I November 5, 2013 I Genkyotex, the leading developer of selective NOX enzyme inhibitors, announced today the initiation of a multinational Phase II clinical study of GKT137831 in patients with diabetic nephropathy. GKT137831 is a first in classinhibitor targeting NOX1 and NOX4 enzymes, both of which play a key role in the development of diabetic complications and chronic kidney disease in particular. In phase I studies in more than 100 subjects, GKT137831 was found to be safe and well tolerated when administered orally once and twice daily.
“There is a significant need for more effective therapies for diabetic nephropathy, particularly as the prevalence of this disease continues to rise. The central role of NOX enzymes in diabetic kidney disease suggests that GKT137831 may confer broad therapeutic benefits to patients,” explained Dr. Kumar Sharma, Professor of Medicine, Director, Institute of Metabolomic Medicine and Director, Center for Renal Translational Medicine, University of California, San Diego. “Studies to date in preclinical models of the disease have shown very promising results and we look forward to seeing data from diabetic patients.”
The placebo controlled, double-blind, randomized Phase II clinical study has been designed to evaluate the safety and efficacy of GKT137831 in 120 patients with Type 2 diabetes and residual albuminuria despite maximal inhibition of the renin angiotensin aldosterone system. The primary endpoint of the study is the change in the urine albumin-to-creatinine ratio (UACR) versus baseline. Secondary endpoints include changes in markers of glucose metabolism, adipose tissue dysfunction and inflammation, and in predictive markers of progression to end-stage renal disease.
“This is the first targeted NOX inhibitor to be trialled in patients and the study will provide extensive data about the role of NOX and NOX inhibition in this group of patients with nephropathy,’’ said Dr. Philippe Wiesel, Genkyotex’s Chief Medical Officer. “Investigational sites are now being opened in North America and the study will be rolled out to centres in Europe and Australia as well. We look forward to reporting on data in the first half of 2015.’’
An oral presentation entitled “Genetic Deletion And Pharmacological Inhibition Of The NADPH Oxidase NOX4 Provides Renoprotection In Diabetes-Induced Nephropathy” will be given on November 9 at 4:54 pm in Room 308 during the American Society of Nephrology’s Kidney Week 2013 Annual Meeting (November 7-10, Atlanta, GA). The presentation with be given by Dr. Jay Jha of the Baker IDI Heart & Diabetes Institute, Melbourne and will include data showing the positive effects of GKT137831 administration in models of diabetic nephropathy.
About NOX and its Role in Diabetic Nephropathy
NOX enzymes exist in seven isoforms and produce reactive oxygen species (ROS). ROS can cause tissue damage and modify biological pathways that are important in a number of pathologies, including metabolic, cardiovascular, pulmonary and neurological diseases. In the kidney, NOX4 is the most abundantly expressed isoform and even further upregulated in diabetic nephropathy. The causal role of NOX enzymes in diabetic complications is well recognised. NOX4 plays a key role in glomerular damage and kidney fibrosis, which lead to albuminuria and end-stage renal disease, respectively. NOX1 is also involved in retinal angiogenesis, atherosclerosis and other diabetic co-morbidities, making the inhibition of both the NOX1 and NOX4 enzymes by GKT137831, an attractive therapeutic option for patients with diabetes. This competitive therapeutic profile of GKT137831 has been validated in several animal models of diabetic complications.
About Genkyotex
Genkyotex is developing first in class, small molecule therapeutics that specifically and selectively inhibit the NOX family of enzymes. Using a unique screening platform, Genkyotex has identified novel NOX inhibitors with the potential to treat disease areas with a high clinical need and large market potential. The company’s lead product, GKT137831, is now entering Phase II clinical studies in patients with diabetic nephropathy and has shown promise in several other disease models, including atherosclerosis, idiopathic pulmonary fibrosis, liver fibrosis and models of angiogenisis. Genkyotex was founded in 2006 by scientists from Switzerland, the USA and Japan, with backing from Geneva incubator Eclosion. Leading global investors Edmond de Rothschild Investment Partners, Vesalius BioCapital and MP Healthcare Venture Management have joined Eclosion in providing significant investment to Genkyotex. Further information can be found at: www.genkyotex.com.
SOURCE: Genkyotex
Post Views: 131
GENEVA, Switzerland & ARCHAMPS, France I November 5, 2013 I Genkyotex, the leading developer of selective NOX enzyme inhibitors, announced today the initiation of a multinational Phase II clinical study of GKT137831 in patients with diabetic nephropathy. GKT137831 is a first in classinhibitor targeting NOX1 and NOX4 enzymes, both of which play a key role in the development of diabetic complications and chronic kidney disease in particular. In phase I studies in more than 100 subjects, GKT137831 was found to be safe and well tolerated when administered orally once and twice daily.
“There is a significant need for more effective therapies for diabetic nephropathy, particularly as the prevalence of this disease continues to rise. The central role of NOX enzymes in diabetic kidney disease suggests that GKT137831 may confer broad therapeutic benefits to patients,” explained Dr. Kumar Sharma, Professor of Medicine, Director, Institute of Metabolomic Medicine and Director, Center for Renal Translational Medicine, University of California, San Diego. “Studies to date in preclinical models of the disease have shown very promising results and we look forward to seeing data from diabetic patients.”
The placebo controlled, double-blind, randomized Phase II clinical study has been designed to evaluate the safety and efficacy of GKT137831 in 120 patients with Type 2 diabetes and residual albuminuria despite maximal inhibition of the renin angiotensin aldosterone system. The primary endpoint of the study is the change in the urine albumin-to-creatinine ratio (UACR) versus baseline. Secondary endpoints include changes in markers of glucose metabolism, adipose tissue dysfunction and inflammation, and in predictive markers of progression to end-stage renal disease.
“This is the first targeted NOX inhibitor to be trialled in patients and the study will provide extensive data about the role of NOX and NOX inhibition in this group of patients with nephropathy,’’ said Dr. Philippe Wiesel, Genkyotex’s Chief Medical Officer. “Investigational sites are now being opened in North America and the study will be rolled out to centres in Europe and Australia as well. We look forward to reporting on data in the first half of 2015.’’
An oral presentation entitled “Genetic Deletion And Pharmacological Inhibition Of The NADPH Oxidase NOX4 Provides Renoprotection In Diabetes-Induced Nephropathy” will be given on November 9 at 4:54 pm in Room 308 during the American Society of Nephrology’s Kidney Week 2013 Annual Meeting (November 7-10, Atlanta, GA). The presentation with be given by Dr. Jay Jha of the Baker IDI Heart & Diabetes Institute, Melbourne and will include data showing the positive effects of GKT137831 administration in models of diabetic nephropathy.
About NOX and its Role in Diabetic Nephropathy
NOX enzymes exist in seven isoforms and produce reactive oxygen species (ROS). ROS can cause tissue damage and modify biological pathways that are important in a number of pathologies, including metabolic, cardiovascular, pulmonary and neurological diseases. In the kidney, NOX4 is the most abundantly expressed isoform and even further upregulated in diabetic nephropathy. The causal role of NOX enzymes in diabetic complications is well recognised. NOX4 plays a key role in glomerular damage and kidney fibrosis, which lead to albuminuria and end-stage renal disease, respectively. NOX1 is also involved in retinal angiogenesis, atherosclerosis and other diabetic co-morbidities, making the inhibition of both the NOX1 and NOX4 enzymes by GKT137831, an attractive therapeutic option for patients with diabetes. This competitive therapeutic profile of GKT137831 has been validated in several animal models of diabetic complications.
About Genkyotex
Genkyotex is developing first in class, small molecule therapeutics that specifically and selectively inhibit the NOX family of enzymes. Using a unique screening platform, Genkyotex has identified novel NOX inhibitors with the potential to treat disease areas with a high clinical need and large market potential. The company’s lead product, GKT137831, is now entering Phase II clinical studies in patients with diabetic nephropathy and has shown promise in several other disease models, including atherosclerosis, idiopathic pulmonary fibrosis, liver fibrosis and models of angiogenisis. Genkyotex was founded in 2006 by scientists from Switzerland, the USA and Japan, with backing from Geneva incubator Eclosion. Leading global investors Edmond de Rothschild Investment Partners, Vesalius BioCapital and MP Healthcare Venture Management have joined Eclosion in providing significant investment to Genkyotex. Further information can be found at: www.genkyotex.com.
SOURCE: Genkyotex
Post Views: 131
