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In addition, there is continuing research and development of new dual α/δ and γ/δ PPAR agonists for additional therapeutic indications, as well as "pan" agonists acting on all three isoforms. [7] [8] The anti-hypertension drug telmisartan is known to have PPAR γ/δ dual partial agonist activity in vivo. It also activates PPAR-α in vitro. [9]
This category lists drugs that act as agonists on peroxisome proliferator-activated receptors (PPARs). Subcategories This category has the following 2 subcategories, out of 2 total.
PPAR -alpha and -gamma pathways. 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 the expression of genes . [ 1 ]
Expression of PPAR-α is highest in tissues that oxidize fatty acids at a rapid rate. In rodents, highest mRNA expression levels of PPAR-alpha are found in liver and brown adipose tissue, followed by heart and kidney. [12] Lower PPAR-alpha expression levels are found in small and large intestine, skeletal muscle and adrenal gland.
Fibrates, known as derivatives of fibric acids, are peroxisome proliferator-activated receptor alpha (PPAR-α) agonists primarily used for lowering TG levels and management of atherogenic dyslipidemia. [30] [31] [32] Typical drugs of the class include fenofibrate, bezafibrate, ciprofibrate and gemfibrozil.
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It is a first in class drug which acts as a dual PPAR agonist at the subtypes α (alpha) and γ (gamma) of the peroxisome proliferator-activated receptor (PPAR). Agonist action on PPARα lowers high blood triglycerides, and agonist action on PPARγ improves insulin resistance and consequently lowers blood sugar. [2]
Elafibranor is a dual PPARα/δ agonist. [7] [8] Elafibranor and its main active metabolite GFT1007 are peroxisome proliferator-activated receptor (PPAR) agonists, both of which activate PPAR-alpha, PPAR-gamma, and PPAR-delta in vitro. [1] In June 2024, the US Food and Drug Administration (FDA) granted accelerated approval to elafibranor. [1 ...