"目录号: HY-15209
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Repaglinide(AG-EE 623ZW)是氨基甲酰甲基苯甲酸（CMBA）衍生物，可作用于II型糖尿病。
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生物活性
Description
Repaglinide(AG-EE 623ZW) is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes. IC50 value:Target: Repaglinide is very rapidly absorbed (tmax less than 1 hour) with a t1/2 of less than one hour. Furthermore, repaglinide is inactivated in the liver and more than 90 % excreted via the bile. Repaglinide (1 mg/kg p.o.) was effective (P < 0.001) as an insulin-releasing agent in a rat model (low-dose streptozotocin) of type 2 diabetes.
Clinical Trial
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Chinese PLA General Hospital
Type 2 Diabetes
January 2009
NCT02128321
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Repaglinide-Pharmacokinetics of Caffeine-Healthy Subjects
January 2014
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Dalim BioTech Co., Ltd.
Diabetes Mellitus, Type 2
March 2013
Phase 1
NCT01797198
Astellas Pharma Europe B.V.-Astellas Pharma Inc
Drug-Drug Interaction (DDI)-Healthy Subjects
April 2012
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Novo Nordisk A/S
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RenJi Hospital
Diabetes Mellitus, Type 2
February 2009
Phase 4
NCT00745433
Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
January 2008
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Novo Nordisk A/S
Diabetes-Healthy
August 2009
Phase 1
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
August 2011
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Boehringer Ingelheim
Healthy
December 2014
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
June 2006
Phase 1
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
March 2010
NCT01498913
Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
August 30, 2001
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Bial - Portela C S.A.
Parkinson Disease
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Phase 1
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
March 2007
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
June 2006
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
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National Cheng-Kung University Hospital
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July 2006
Phase 4
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Children's Hospital of Philadelphia
Diabetes
October 2005
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
November 8, 2001
Phase 4
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
August 2004
NCT00763412
Arbelaez, Ana Maria-Washington University School of Medicine-National Institutes of Health (NIH)-Novo Nordisk A/S-National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Cystic Fibrosis Related Diabetes-Pancreatic Insufficiency
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
September 2005
Phase 4
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Steno Diabetes Center
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
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Phase 3
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
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Phase 4
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Diabetes-Diabetes Mellitus, Type 2
June 1, 2001
Phase 3
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
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Phase 4
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Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
April 26, 2002
Phase 4
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Merck Sharp & Dohme Corp.
Type 2 Diabetes Mellitus
November 8, 2012
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Diabetes-Diabetes Mellitus, Type 2
December 16, 2003
Phase 4
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Steno Diabetes Center
Diabetes Mellitus, Type 2
January 2003
Phase 4
NCT00799448
Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
September 16, 2003
Phase 4
NCT01720303
Novo Nordisk A/S
Diabetes-Diabetes Mellitus, Type 2
September 19, 2002
Phase 4
NCT00662714
Mukoviszidose Institut gGmbH-Novo Nordisk A/S-Mucoviscidose-ABCF2-Assistance Publique - Hôpitaux de Paris
Cystic Fibrosis-Diabetes Mellitus
September 2001
Phase 3
NCT01140438
Norwegian University of Science and Technology
Diabetes
March 2009
NCT00072904
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)-Cystic Fibrosis Foundation Therapeutics-Novo Nordisk A/S
Cystic Fibrosis-Diabetes Mellitus
June 2001
Phase 3
NCT02694263
University of Leicester-University Hospital Birmingham
Diabetes Mellitus, Type 2
July 2016
Phase 4
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Epizyme, Inc.
Diffuse Large B Cell Lymphoma-Primary Mediastinal Lymphoma-Mantle Cell Lymphoma
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References
[1].Marbury T, Huang WC, Strange P, Lebovitz H et al. Repaglinide versus glyburide: a one-year comparison trial. Diabetes Research and Clinical Practice .1999, 43(3):155-166.
[2].David R. Owens . Repaglinide-prandial glucose regulator: a new class of oral antidiabetic drugs . Diabetic Medicine 1998,15 : S28-S36.
[3].J Fuhlendorff, P Rorsman, H Kofod. Stimulation of insulin release by repaglinide and glibenclamide involves both common and distinct processes. Diabetes. 1998. 47 (3): 345-351 .
[4].R Moses, R Slobodniuk, S Boyages. Effect of repaglinide addition to metformin monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care . 22 (1 ) : 119-124 .
[5].Julio Rosenstock, MD, David R. Hassman, DO, Robert D. Madder, DO. Diabetes Care June 2004 vol. 27 no. 6 1265-1270
[6].Shiling Hu1, Shuya Wang1, Barbara Fanelli1. Pancreatic β-Cell KATP Channel Activity and Membrane-Binding Studies with Nateglinide: A Comparison with Sulfonylureas and Repaglinide . JPET , 2000,293 (2 ): 444-452 .