A Randomized, Double-blind, Parallel, Placebo-Controlled, Study to Evaluate the Safety and Tolerability of Oral GW677954 Capsules (15 mg) in Combination With Insulin in Subjects With Type 2 Diabetes Mellitus

Many drugs used for the treatment of Type 2 Diabetes Mellitus cause the body to retain water. This study will assess whether or not GW677954 causes the body to retain fluid.

Start Date01 Sep 2006

Sponsor / Collaborator

GSK Plc

NCT00264667 / CompletedPhase 2

A Randomised,Double-blind, Parallel Group, Placebo-controlled, Multicentre Study to Evaluate the Safety, Tolerability and Efficacy of Oral GW677954 Capsules 2.5mg, 5mg, 10mg and 20mg a Day for 24 Weeks in Overweight Dyslipidaemic Subjects

Study in patients with dyslipidaemia.

Start Date01 Dec 2005

Sponsor / Collaborator

GSK Plc

EUCTR2005-001558-26-ES / Not yet recruitingPhase 2

A RANDOMISED, DOUBLE-BLIND, PARALLEL GROUP, PLACEBO-CONTROLLED, MULTICENTRE STUDY TO EVALUATE THE SAFETY, TOLERABILITY AND EFFICACY OF ORAL GW677954 CAPSULES 2.5mg, 5mg, 10mg AND 20mg A DAY FOR WEEKS IN OVERWEIGHT DYSLIPIDAEMIC SUBJECTS

Start Date11 Oct 2005

Sponsor / Collaborator

GSK Plc

100 Clinical Results associated with Sodelglitazar

100 Translational Medicine associated with Sodelglitazar

100 Patents (Medical) associated with Sodelglitazar

Literatures (Medical) associated with Sodelglitazar

01 Oct 2011·Protein & Peptide LettersQ4 · BIOLOGY

Docking and Molecular Dynamics Simulations of Peroxisome Proliferator Activated Receptors Interacting with Pan Agonist Sodelglitazar

Q4 · BIOLOGY

Article

Author: Wang, Run-Ling ; Wang, Shu-Qing ; Liu, Xu-Yuan ; Tang, Li-Da ; Xu, Wei-Ren ; Chou, Kuo-Chen

PPAR (peroxisome proliferator-activated receptor) pan agonists play a critical role in treating metabolic diseases, especially the Type-2 diabetes mellitus (T2DM). GlaxoSmithKline's sodelglitazar (GW677954) is one of the potent PPAR pan agonists, which is currently being investigated in Phase II clinical trials for the treatment of T2DM and its complications. The present study was aimed at investigation into the effect of sodelglitazar at the binding pockets of PPARs. The Schrodinger Suite program (2009) was used for the molecular docking, while the GROMACS program used for the molecular dynamics (MD) simulations. The results thus obtained showed that sodelglitazar being docked well in the active site of PPARs. It was revealed by the MD simulations that the structures of the receptors remained quite stable during the simulations and that the important AF-2 helix showed less flexibility after binding with sodelglitazar. Also, it was observed that sodelglitazar could periodically form hydrogen bonds with the AF-2 helix of PPARs to stabilize the AF-2 helix in an active conformation. Our findings have confirmed that GlaxoSmithKline's sodelglitazar can activate the PPARs, which is quite consistent with the previous biological studies.

100 Deals associated with Sodelglitazar

External Link

KEGG	Wiki	ATC	Drug Bank
D06647	Sodelglitazar	-	DB16332

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 2	PE	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	MX	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	US	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	MX	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	US	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	LV	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	CO	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	PE	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	LV	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	CO	GSK Plc	01 Sep 2005

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