scholarly journals Emerging role of GLP-1 receptor agonists in the treatment of obesity

2010 ◽  
Vol Volume 3 ◽  
pp. 263-273 ◽  
Author(s):  
Lisa M. Neff
2017 ◽  
Vol 31 (11) ◽  
pp. 1403-1418 ◽  
Author(s):  
Guy A Higgins ◽  
Fiona D Zeeb ◽  
Paul J Fletcher

The selective 5-HT2C receptor agonist lorcaserin entered clinical obesity trials with the prevalent view that satiety was a primary mechanism of action. Subsequent Phase II and III trials demonstrated efficacy in terms of weight loss, although the overall effect size (~3% placebo-corrected change) is considered modest. Lorcaserin has been approved by the FDA for the treatment of obesity with lifestyle modification, but since its introduction in 2013 its sales are in decline, probably due to its overall modest effect. However, in some individuals, lorcaserin has a much more clinically significant effect (i.e. >10% placebo-corrected change), although what common features, if any, define these high responders is presently unknown. In the present article we highlight the evidence that alternative mechanisms to satiety may contribute to the anti-obesity effect of lorcaserin, namely effects on constructs of primary and conditioned reward and impulsivity. This may better inform the clinical evaluation of lorcaserin (and any future 5-HT2C receptor agonists) to subgroups of obese subjects characterized by overeating due to maladaptive impulsivity and reward mechanisms. One such population might be individuals diagnosed with binge eating disorder.


Author(s):  
Giuseppe Lassandro ◽  
Valentina Palladino ◽  
Giovanni Carlo Del Vecchioa ◽  
Viviana Valeria Palmieri ◽  
Paola Carmela Corallo ◽  
...  

Background and Objective: Immune thrombocytopenia (ITP) is a common bleeding disorder in childhood. The management of ITP in children is controversial, requiring personalized assessment of patients and therapeutic choices. Thrombopoietin receptor agonists (TPO-RAs), eltrombopag and romiplostim, have been shown to be safety and effective for the treatment of pediatric ITP. The aim of our research is defining the role of thrombopoietin receptor agonists in the management of pediatric ITP. Method: This review focuses on the use of TPO-RAs in pediatric ITP, in randomized trials and in clinical routine, highlighting their key role in management of the disease. Results: Eltrombopag and romiplostim appear effective treatment options for children with ITP. Several clinical studies have assessed that the use of TPO-RAs increases platelet count, decreases bleeding symptoms and improves health-related quality of life. Moreover, TPO-RAs are well tolerated with minor side effects. Conclusion: Although TPO-RAs long term efficacy and safety still require further investigations, their use is gradually expanding in clinical practice of children with ITP.


2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Yawei Wang ◽  
Binlin Tang ◽  
Lei Long ◽  
Peng Luo ◽  
Wei Xiang ◽  
...  

AbstractPro-inflammatory activation of adipose tissue macrophages (ATMs) is causally linked to obesity and obesity-associated disorders. A number of studies have demonstrated the crucial role of mitochondrial metabolism in macrophage activation. However, there is a lack of pharmaceutical agents to target the mitochondrial metabolism of ATMs for the treatment of obesity-related diseases. Here, we characterize a near-infrared fluorophore (IR-61) that preferentially accumulates in the mitochondria of ATMs and has a therapeutic effect on diet-induced obesity as well as obesity-associated insulin resistance and fatty liver. IR-61 inhibits the classical activation of ATMs by increasing mitochondrial complex levels and oxidative phosphorylation via the ROS/Akt/Acly pathway. Taken together, our findings indicate that specific enhancement of ATMs oxidative phosphorylation improves chronic inflammation and obesity-related disorders. IR-61 might be an anti-inflammatory agent useful for the treatment of obesity-related diseases by targeting the mitochondria of ATMs.


Author(s):  
Johanna Helmstädter ◽  
Karin Keppeler ◽  
Leonie Küster ◽  
Thomas Münzel ◽  
Andreas Daiber ◽  
...  
Keyword(s):  

Antioxidants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 102
Author(s):  
Federico Pietrocola ◽  
José Manuel Bravo-San Pedro

Reactive oxygen species (ROS) operate as key regulators of cellular homeostasis within a physiological range of concentrations, yet they turn into cytotoxic entities when their levels exceed a threshold limit. Accordingly, ROS are an important etiological cue for obesity, which in turn represents a major risk factor for multiple diseases, including diabetes, cardiovascular disorders, non-alcoholic fatty liver disease, and cancer. Therefore, the implementation of novel therapeutic strategies to improve the obese phenotype by targeting oxidative stress is of great interest for the scientific community. To this end, it is of high importance to shed light on the mechanisms through which cells curtail ROS production or limit their toxic effects, in order to harness them in anti-obesity therapy. In this review, we specifically discuss the role of autophagy in redox biology, focusing on its implication in the pathogenesis of obesity. Because autophagy is specifically triggered in response to redox imbalance as a quintessential cytoprotective mechanism, maneuvers based on the activation of autophagy hold promises of efficacy for the prevention and treatment of obesity and obesity-related morbidities.


2010 ◽  
Vol 151 (19) ◽  
pp. 763-773 ◽  
Author(s):  
Andrea Balázs

A túlsúly és az elhízás bizonyítottan a jövő egyik legjelentősebb egészségügyi problémája. A fejlett országokban a túlsúlyos és elhízott emberek aránya ötévente megduplázódik. Egy európai vizsgálat adatai szerint minden második felnőtt túlsúlyos, és a becslések szerint 2000 és 2030 között az elhízottak száma megduplázódhat. Ahogy növekszik világszerte az elhízottak és a cukorbetegek száma, úgy nő az érdeklődés a természetes alapú készítmények iránt. Az elhízás terápiájában több száz gyógynövény ismert, de a forgalmazott és alkalmazott teakeverékeket szájhagyomány vagy más információforrás alapján alkalmazzák. A nagyszámú növény botanikailag rendkívül sokféle, számos rendszertani egységből kerül ki, így az sem meglepő, hogy a hatóanyagok kémiailag szintén sokfélék. A különböző hatóanyagok más-más hatásmechanizmuson keresztül fejtik ki hatásukat. Az elhízás, a diabetes kezelésére engedélyezett növényi gyógyszerkészítmény még nincs forgalomban, így a lakosság vagy engedély nélküli, vagy ismeretlen minőségű, vagy más célra engedélyezett termékeket fogyaszt. Ez a helyzet sok országra jellemző, ami visszaélésekre ad lehetőséget, valamint a betegek számára sem ad kellő biztonságot a gyógynövények alkalmazásában.


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