"目錄號(hào): HY-15209

Others-

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

NCT00832481

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

Phase 1

NCT01780051

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

Phase 1

NCT00819741

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

February 2009

Phase 4

NCT02040246

RenJi Hospital

Diabetes Mellitus, Type 2

February 2009

Phase 4

NCT00745433

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

January 2008

NCT00959101

Novo Nordisk A/S

Diabetes-Healthy

August 2009

Phase 1

NCT01355718

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

August 2011

NCT02305901

Boehringer Ingelheim

Healthy

December 2014

Phase 1

NCT01489644

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

June 2006

Phase 1

NCT01077570

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

March 2010

NCT01498913

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

August 30, 2001

NCT01536366

Bial - Portela C S.A.

Parkinson Disease

June 2009

Phase 1

NCT00709917

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

March 2007

NCT01490658

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

June 2006

Phase 1

NCT01022762

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

November 2009

Phase 4

NCT00336310

National Cheng-Kung University Hospital

Diabetes Mellitus, Type 2

July 2006

Phase 4

NCT00231192

Children's Hospital of Philadelphia

Diabetes

October 2005

NCT01605773

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

November 8, 2001

Phase 4

NCT01498900

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

November 2006

NCT00491725

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

September 2005

Phase 4

NCT01465152

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

March 6, 2002

Phase 4

NCT00118950

Steno Diabetes Center

Diabetes Mellitus, Type 2

March 2001

Phase 4

NCT00399711

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

November 2006

Phase 3

NCT00568984

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

November 21, 2002

Phase 4

NCT01562561

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

June 1, 2001

Phase 3

NCT01720290

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

July 25, 2002

Phase 4

NCT01698931

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

April 26, 2002

Phase 4

NCT01709305

Merck Sharp & Dohme Corp.

Type 2 Diabetes Mellitus

November 8, 2012

Phase 4

NCT00568074

Novo Nordisk A/S

Diabetes-Diabetes Mellitus, Type 2

December 16, 2003

Phase 4

NCT00118963

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 - H?pitaux 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

NCT03028103

Epizyme, Inc.

Diffuse Large B Cell Lymphoma-Primary Mediastinal Lymphoma-Mantle Cell Lymphoma

March 27, 2017

Phase 1

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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 .