2018
DOI: 10.1016/j.bmcl.2017.11.006
|View full text |Cite
|
Sign up to set email alerts
|

Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1
1

Citation Types

0
13
0

Year Published

2018
2018
2024
2024

Publication Types

Select...
7
1

Relationship

0
8

Authors

Journals

citations
Cited by 10 publications
(13 citation statements)
references
References 15 publications
0
13
0
Order By: Relevance
“…The clinical development of PPARβ/δ agonists has been unsuccessful to date, and GW501516 remains a banned metabolic modulator by the World Anti-Doping Agency. Pharmaco-equivalents with better safety profiles, however, are still heavily researched [ 135 , 136 ].…”
Section: Regulation Of Ppars During Physical Exercisementioning
confidence: 99%
“…The clinical development of PPARβ/δ agonists has been unsuccessful to date, and GW501516 remains a banned metabolic modulator by the World Anti-Doping Agency. Pharmaco-equivalents with better safety profiles, however, are still heavily researched [ 135 , 136 ].…”
Section: Regulation Of Ppars During Physical Exercisementioning
confidence: 99%
“…Yet, in the present study, Cardarine was shown to reduce oxidative stress and attenuate obesity, which otherwise may activate inflammatory pathways and promote tumorigenesis (Reuter et al, 2010). Compound 1 examined by Lagu et al is a more selective PPAR-δ agonist than GW501516 that appears to exhibit an improved safety profile (Lagu et al, 2018). Thus, further research on GW501516 and similar PPAR-δ agonists are required as some benefits may outweigh impeding risks, especially in the context of metabolic syndrome-like conditions.…”
Section: Journal Ofmentioning
confidence: 62%
“…This is also due to the lack of literature. Given the toxicity of GW501516 in animal models, 4 it is obvious that no controlled study will be implemented to address the previously mentioned issues, which have emerged for interpreting the hair findings. This is simply ethically not acceptable.…”
Section: Resultsmentioning
confidence: 99%
“…Rapidly, 3 GlaxoSmithKline and Ligand developed GW‐501516, an agonist for the potential treatment of dyslipemia. The drug reached phase II clinical trials but was discontinued in 2007 due to induction of intestinal adenoma in rats, and other highly selective PPAR‐δ with an improved safety profile were proposed 4 …”
Section: Introductionmentioning
confidence: 99%