TGR5 receptor agonists are primarily investigated for their role in metabolic and inflammatory diseases. These compounds activate the TGR5 (also known as GPBAR1) bile acid receptor, which is involved in regulating glucose homeostasis, energy expenditure, and insulin sensitivity. As such, they show promise in the treatment of type 2 diabetes by enhancing glucose-dependent insulin secretion and improving glucose tolerance. Another key application is in obesity management. Activation of TGR5 increases the expression of type 2 iodothyronine deiodinase in brown adipose tissue, leading to higher thermogenesis and energy expenditure, which promotes weight loss. TGR5 agonists also exhibit anti-inflammatory effects, particularly in immune cells like macrophages, making them candidates for treating chronic inflammatory conditions, including non-alcoholic steatohepatitis (NASH) and inflammatory bowel disease (IBD). Additionally, these agonists influence gallbladder filling and gut motility, which can impact the development of therapies for biliary and gastrointestinal disorders. Due to their broad systemic effects, TGR5 agonists are being explored in multi-factorial metabolic syndrome components, offering a potential for oral therapeutics with dual or multi-target benefits.