Discovery of (S)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus

2012 ◽  
Vol 55 (3) ◽  
pp. 1318-1333 ◽  
Author(s):  
Jeffrey A. Pfefferkorn ◽  
Angel Guzman-Perez ◽  
John Litchfield ◽  
Robert Aiello ◽  
Judith L. Treadway ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Nicotinic Acid ◽  
Glucokinase Activator ◽  
Clinical Candidate

Dose-ranging study with the glucokinase activator AZD1656 in patients with type 2 diabetes mellitus on metformin

2013 ◽  
Vol 15 (8) ◽  
pp. 750-759 ◽  
Author(s):  
J. P. H. Wilding ◽  
M. Leonsson-Zachrisson ◽  
C. Wessman ◽  
E. Johnsson
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Glucokinase Activator ◽  
Dose Ranging

Safety, pharmacokinetics and pharmacodynamics of multiple-ascending doses of the novel glucokinase activator AZD1656 in patients with type 2 diabetes mellitus

2012 ◽  
Vol 14 (12) ◽  
pp. 1114-1122 ◽  
Author(s):  
L. A. Morrow ◽  
M. Leonsson-Zachrisson ◽  
H. Ericsson ◽  
M. Wollbratt ◽  
M. Knutsson ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
The Novel ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Glucokinase Activator

Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus

2013 ◽  
Vol 23 (2) ◽  
pp. 537-542 ◽  
Author(s):  
Kaapjoo Park ◽  
Byoung Moon Lee ◽  
Young Hwan Kim ◽  
Taedong Han ◽  
Wonhui Yi ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Glucokinase Activator

scholarly journals Piragliatin (RO4389620), a Novel Glucokinase Activator, Lowers Plasma Glucose Both in the Postabsorptive State and after a Glucose Challenge in Patients with Type 2 Diabetes Mellitus: A Mechanistic Study

2010 ◽  
Vol 95 (11) ◽  
pp. 5028-5036 ◽  
Author(s):  
Riccardo C. Bonadonna ◽  
Tim Heise ◽  
Christophe Arbet-Engels ◽  
Christoph Kapitza ◽  
Angelo Avogaro ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Plasma Glucose ◽  
Mechanistic Study ◽  
Glucokinase Activator ◽  
Glucose Challenge

scholarly journals Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Ping Wang ◽  
Huili Liu ◽  
Li Chen ◽  
Yingli Duan ◽  
Qunli Chen ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Insulin Resistance ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Diabetic Rats ◽  
Diabetic Group ◽  
Whole Body ◽  
Glucokinase Activator ◽  
Liver And Pancreas

Glucokinase (GK) plays a critical role in the control of whole-body glucose homeostasis. We investigated the possible effects of a novel glucokinase activator (GKA), HMS5552, to the GK in rats with type 2 diabetes mellitus (T2DM). Male Sprague-Dawley (SD) rats were divided into four groups: control group, diabetic group, low-dose (10 mg/kg) HMS5552-treated diabetic group (HMS-L), and high-dose (30 mg/kg) HMS5552-treated diabetic group (HMS-H). HMS5552 was administered intragastrically to the T2DM rats for one month. The levels of total cholesterol, triglyceride, fasting plasma insulin (FINS), and glucagon (FG) were determined, and an oral glucose tolerance test was performed. The expression patterns of proteins and genes associated with insulin resistance and GK activity were assayed. Compared with diabetic rats, the FINS level was significantly decreased in the HMS5552-treated diabetic rats. HMS5552 treatment significantly lowered the blood glucose levels and improved GK activity and insulin resistance. The immunohistochemistry, western blot, and semiquantitative RT-PCR results further demonstrated the effects of HMS5552 on the liver and pancreas. Our data suggest that the novel GKA, HMS5552, exerts antidiabetic effects on the liver and pancreas by improving GK activity and insulin resistance, which holds promise as a novel drug for the treatment of T2DM patients.

The glucokinase activator AZD6370 decreases fasting and postprandial glucose in type 2 diabetes mellitus patients with effects influenced by dosing regimen and food

2012 ◽  
Vol 98 (3) ◽  
pp. 436-444 ◽  
Author(s):  
Hans Ericsson ◽  
Folke Sjöberg ◽  
Maria Heijer ◽  
Hassan Dorani ◽  
Peter Johansson ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Postprandial Glucose ◽  
Dosing Regimen ◽  
Glucokinase Activator

Dose-ranging study with the glucokinase activator AZD1656 as monotherapy in Japanese patients with type 2 diabetes mellitus

2013 ◽  
Vol 15 (10) ◽  
pp. 923-930 ◽  
Author(s):  
A. Kiyosue ◽  
N. Hayashi ◽  
H. Komori ◽  
M. Leonsson-Zachrisson ◽  
E. Johnsson
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Japanese Patients ◽  
Glucokinase Activator ◽  
Dose Ranging
Sign in / Sign up

Export Citation Format

Share Document