Chiglitazar: First Approval

Deeks, Emma D.

doi:10.1007/s40265-021-01648-1

Cited by 16 publications

(10 citation statements)

References 16 publications

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“…At the same time, acarbose showed beneficial effects on the composition of the gut microbiome, suggesting that the detected metabolic modifications of sulfonylureas might not be intermediated by their impacts on the gut microbiota ( 62 , 87 ). Recently, a few newly invented oral anti-glucose agents were discovered and used in clinical application, such as chiglitazar and imeglimin ( 148 , 149 ). Activating as a peroxisome proliferator-activated receptor pan-agonist for glucose control, chiglitazar was found to improve insulin sensitivity and lipid homeostasis and reduce circulating levels of inflammatory parameters ( 150 , 151 ).…”

Section: The Effects Of Oral Antidiabetic Drugs On Gut Microbiota And...mentioning

confidence: 99%

Effects of Oral Glucose-Lowering Agents on Gut Microbiota and Microbial Metabolites

et al. 2022

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The current research and existing facts indicate that type 2 diabetes mellitus (T2DM) is characterized by gut microbiota dysbiosis and disturbed microbial metabolites. Oral glucose-lowering drugs are reported with pleiotropic beneficial effects, including not only a decrease in glucose level but also weight loss, antihypertension, anti-inflammation, and cardiovascular protection, but the underlying mechanisms are still not clear. Evidence can be found showing that oral glucose-lowering drugs might modify the gut microbiome and thereby alter gastrointestinal metabolites to improve host health. Although the connections among gut microbial communities, microbial metabolites, and T2DM are complex, figuring out how antidiabetic agents shape the gut microbiome is vital for optimizing the treatment, meaningful for the instruction for probiotic therapy and gut microbiota transplantation in T2DM. In this review, we focused on the literatures in gut microbiota and its metabolite profile alterations beneficial from oral antidiabetic drugs, trying to provide implications for future study in the developing field of these drugs, such as combination therapies, pre- and probiotics intervention in T2DM, and subjects with pregestational diabetes and gestational diabetes mellitus.

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Section: The Effects Of Oral Antidiabetic Drugs On Gut Microbiota And...mentioning

confidence: 99%

Effects of Oral Glucose-Lowering Agents on Gut Microbiota and Microbial Metabolites

et al. 2022

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“…Despite the few cases of weight gain and edema, it was characterized by the American Union of Diabetes as a safe treatment for DT2 in 2019 and was later approved by China's authorities in 2021 as a new effective treatment for DT2 patients. [58][59][60][61] Lanifibranor (Scheme 11) is one more remarkable triple PPARα/γ/δ agonist. This molecule was designed by Boubia et al in an attempt to eliminate the adverse effects connected with PPARγ or dual PPARα/γ agonists.…”

Section: Triple Pparα/γ/δ Agonistsmentioning

confidence: 99%

“…Moving on to Phase 3, administration of chiglitazar to patients with DT2 caused a significant reduction in HbA 1c plasma levels, comparable to sitagliptin , while being well tolerated. Despite the few cases of weight gain and edema, it was characterized by the American Union of Diabetes as a safe treatment for DT2 in 2019 and was later approved by China's authorities in 2021 as a new effective treatment for DT2 patients [58–61] …”

Section: Diabetes Mellitusmentioning

confidence: 99%

Design of Improved Antidiabetic Drugs: A Journey from Single to Multitarget Agents

2022

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Multifactorial diseases exhibit a complex pathophysiology with several factors contributing to their pathogenesis and development. Examples of such disorders are neurodegenerative (e. g. Alzheimer's, Parkinson's) and cardiovascular diseases (e. g. atherosclerosis, metabolic syndrome, diabetes II). Traditional therapeutic approaches with single‐target drugs have been proven, in many cases, unsatisfactory for the treatment of multifactorial diseases such as diabetes II. The well‐established by now strategy of multitarget drugs is constantly gaining interest and momentum, as a more effective approach. The development of pharmacomolecules able to simultaneously modulate multiple relevant‐to‐the‐disease targets has already several successful examples in various fields and has, as such, inspired the design of multitarget antidiabetic agents; this review highlights the design aspect and efficacy of this approach for improved antidiabetics by presenting several examples of successful pharmacophore combinations in (multitarget) agents that modulate two or more molecular targets involved in diabetes II, resulting in a superior antihyperglycemic profile.

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“…Data reported in the literature suggest that carbazoles are able to modulate glucose metabolism, block adrenergic hyperactivation, prevent damage to β cells of the pancreas, inhibit inflammatory and oxidative mediators, control the cryptochrome or inhibit α-glucosidase (Table 2). Therefore, carbazole represents a versatile scaffold for the preparation of biologically active derivatives, useful in the treatment of diabetes [6,7,[27][28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44][45][46].…”

Section: Carbazole Derivatives In the Pathogenesis Of Diabetesmentioning

confidence: 99%

“…Chiglitazar (Bilessglu ® ) (22) (Figure 12) is a small molecule with agonist activity against PPARα, δ and γ, recently developed by Chipscreen Bioscience. In China, this drug was approved in October 2021 for the treatment of diabetes and is currently in phase II clinical trials for the treatment of non-alcoholic steatohepatitis [44]. In a very recent phase III study, [45] the efficacy and safety of chiglitazar (22) were investigated in patients with type 2 DM who were unable to control their blood sugar with diet and exercise alone.…”

Section: Chiglitazarmentioning

confidence: 99%

Carbazoles: Role and Functions in Fighting Diabetes

Grande

Ioele²,

Caruso³

et al. 2022

Applied Sciences

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Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing to their role in the pathogenesis and development of diabetes. Several studies have demonstrated the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation, prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we summarize the latest advances in the synthetic and natural carbazole-containing compounds involved in diabetes pathways.

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Chiglitazar: First Approval

Cited by 16 publications

References 16 publications

Effects of Oral Glucose-Lowering Agents on Gut Microbiota and Microbial Metabolites

Effects of Oral Glucose-Lowering Agents on Gut Microbiota and Microbial Metabolites

Design of Improved Antidiabetic Drugs: A Journey from Single to Multitarget Agents

Carbazoles: Role and Functions in Fighting Diabetes

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