Delving into the Latest Updates on Sodelglitazar with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Sodelglitazar (USAN)

+ [3]

Target

PPARα

Mechanism

PPARα agonists(Peroxisome proliferator-activated receptor α agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Diabetes Mellitus, Type 2DyslipidemiasMetabolic Syndrome

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC23H21F4NO3S2

InChIKeyZUGQWAYOWCBWGM-UHFFFAOYSA-N

CAS Registry447406-78-2

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

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D06647	Sodelglitazar	-	DB16332

R&D Status

10 top R&D records.

Login

to view more data

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	AU	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	CZ	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	CZ	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	CA	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	CO	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	CA	GSK Plc	01 Sep 2005
Diabetes Mellitus, Type 2	Phase 2	AU	GSK Plc	01 Sep 2005