GW-501516 GlaxoSmithKline/Ligand.

¹Johnson & Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA. PPelton@prdus.jnj.com

Current Opinion in Investigational Drugs (London, England : 2000)

|April 22, 2006

Summary

GlaxoSmithKline and Ligand are developing GW-501516, a novel drug targeting dyslipidemia. Ongoing Phase II trials are evaluating its potential as a peroxisome proliferator-activator receptor-delta agonist.

Area of Science:

Pharmacology
Metabolic Diseases
Drug Development

Background:

Dyslipidemia is a significant risk factor for cardiovascular disease.
Current treatments for dyslipidemia have limitations and side effects.
Peroxisome proliferator-activated receptor delta (PPAR-δ) agonists represent a novel therapeutic target.

Purpose of the Study:

To evaluate the safety and efficacy of GW-501516, a PPAR-δ agonist.
To assess the potential of GW-501516 in treating dyslipidemia.

Main Methods:

GW-501516 is a peroxisome proliferator-activator receptor-delta agonist.
Phase II clinical trials are currently underway.
The trials are designed to assess the drug's therapeutic potential.

Main Results:

Clinical trial data is still being collected.
Preliminary findings are anticipated upon trial completion.

Conclusions:

GW-501516 shows promise for dyslipidemia treatment.
Further clinical evaluation is required to confirm efficacy and safety.

Related Experiment Videos

GW-501516 GlaxoSmithKline/Ligand.

Related Concept Videos

Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein inhibitor.

Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists.

Improvement of dyslipidemia, insulin sensitivity, and energy balance by a peroxisome proliferator-activated receptor alpha agonist.

Synthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors alpha/delta dual agonists.

Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta.

Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.

Reporting disease control rates or clinical benefit rates in early clinical trials of anticancer agents: useful endpoint or hype?

Abating progressive tissue injury and preserving function after CNS trauma: The role of inflammation modulatory therapies.

Teriflunomide, an inhibitor of dihydroorotate dehydrogenase for the potential oral treatment of multiple sclerosis.

Tralokinumab, an anti-IL-13 mAb for the potential treatment of asthma and COPD.

Vedolizumab, a humanized mAb against the α4β7 integrin for the potential treatment of ulcerative colitis and Crohn's disease.

Pitrakinra, a dual IL-4/IL-13 antagonist for the potential treatment of asthma and eczema.

Exploring the Distinct Regulatory Actions and Molecular Pathways of Coptisine Through Network Pharmacology: Insights Into Its Influence on Platelet Activation and Thrombus Development.

Effect of Betahistine on Daytime Sedation and Metabolic Parameters in Patients with Schizophrenia on Second-generation Antipsychotics.

Adult dual and polytobacco use in the United States: Findings from the 2021-2023 National Survey on Drug Use and Health.

Dipeptidyl Peptidase-4 (DPP-4) Inhibitors Versus Glucagon-Like Peptide-1 (GLP-1) Receptor Agonists Following Orthopedic Shoulder Surgery: A Comparative Analysis.

Dipeptidyl Peptidase-4 (DPP-4) Inhibitors Are Associated With Reduced Early but Increased Chronic Postoperative Opioid Use After Shoulder Surgery.

Simvastatin modulates sleep-wake behavior and locomotor activity in a dose-dependent manner in <i>Drosophila</i>.

Related Experiment Videos

GW-501516 GlaxoSmithKline/Ligand.

Area of Science:

Background:

Purpose of the Study:

Main Methods:

Main Results:

Conclusions:

Related Concept Videos

Related Articles