Sodelglitazar, formerly known as GW 677954, is a thiazole
PPARδ receptor agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agon ...
developed by
GlaxoSmithKline
GSK plc (an acronym from its former name GlaxoSmithKline plc) is a British Multinational corporation, multinational Pharmaceutics, pharmaceutical and biotechnology company with headquarters in London. It was established in 2000 by a Mergers an ...
. While it is primarily active at the PPARδ receptor, it is considered a pan agonist with activity at
PPARα
Peroxisome proliferator-activated receptor alpha (PPAR-α), also known as NR1C1 (nuclear receptor subfamily 1, group C, member 1), is a nuclear receptor protein functioning as a transcription factor that in humans is encoded by the ''PPARA'' gen ...
and
PPARγ
Peroxisome proliferator-activated receptor gamma (PPAR-γ or PPARG), also known as the glitazone reverse insulin resistance receptor, or NR1C3 (nuclear receptor subfamily 1, group C, member 3) is a type II nuclear receptor functioning as a transc ...
receptors.
Safety
Phase 2 studies were terminated prior to completion due to safety findings in
rodent studies
Rodents have been employed in biomedical experimentation from the 1650s. Rodent studies up to the early 19th century were mainly physiological or toxicological. The first rodent behavioral study was carried out in 1822, a purely observational st ...
.
See also
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Elafibranor
Elafibranor, sold under the brand name Iqirvo, is a medication used for the treatment of primary biliary cholangitis.
Elafibranor is a dual PPARα/δ agonist. Elafibranor and its main active metabolite GFT1007 are peroxisome proliferator-acti ...
*
GW0742
GW0742 (also known as GW610742 and fitorine) is a PPARδ/β agonist that has been investigated for drug use by GlaxoSmithKline.
Pharmacology Pharmacodynamics
It is mixed PPAR-B agonist antagonist depending on its dosage. It has weak activity on ...
*
GW501516
GW501516 (also known as GW-501,516, GW1516, GSK-516, cardarine, and on the black market as endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It entered ...
*
MBX-8025
Seladelpar, sold under the brand name Livdelzi, is a medication used for the treatment of primary biliary cholangitis. It is used as the lysine dihydrate salt. It is a peroxisome proliferator-activated receptor delta (PPARδ) receptor agonist. ...
*
Peroxisome proliferator-activated receptor
In the field of molecular biology, the peroxisome proliferator–activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors regulating gene expression. PPARs play essential roles in regulating cel ...
References
PPAR agonists
Drugs developed by GSK plc
Experimental drugs
Trifluoromethyl compounds
Fluoroarenes
Thiazoles
Carboxylic acids
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