Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus

Bae, Jaehyun; Park, Taegyun; Kim, Hye Young; Lee, Minyoung; Soo, Bong

doi:10.4093/dmj.2020.0272

Cited by 28 publications

(31 citation statements)

References 56 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…2 A previous retrospective study revealed that the combination of lobeglitazone and DPP4 inhibitor might be more potent than other lobeglitazone-combined regimens. 12 In this respect, our study might be an option when considering adding one more drug in common combination.…”

Section: Discussionmentioning

confidence: 96%

“…Technically, thiazolidinediones (TZDs) are the only insulin sensitizers among various antidiabetic agents. They activate peroxisome proliferator‐activated receptor gamma and simultaneously improve insulin resistance in adipose cells, upregulate glucose uptake and utilization by the muscles, and reduce hepatic glucose production 9‐12 . Considering the pathophysiology of T2DM, which includes insulin resistance and beta‐cell dysfunction, the frequency of TZD usage will probably increase 13 .…”

Section: Introductionmentioning

confidence: 99%

“…They activate peroxisome proliferator-activated receptor gamma and simultaneously improve insulin resistance in adipose cells, upregulate glucose uptake and utilization by the muscles, and reduce hepatic glucose production. [9][10][11][12] Considering the pathophysiology of T2DM, which includes insulin resistance and beta-cell dysfunction, the frequency of TZD usage will probably increase. 13 After the United States Food and Drug Administration approved pioglitazone and rosiglitazone in 1999, the adoption of TZDs has markedly increased.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study

Ryang

Kim

Bae

et al. 2022

Diabetes Obesity Metabolism

View full text Add to dashboard Cite

Aims To compare the efficacy and safety of adding low‐dose lobeglitazone (0.25 mg/day) or standard‐dose lobeglitazone (0.5 mg/day) to patients with type 2 diabetes mellitus (T2DM) with inadequate glucose control on metformin and dipeptidyl peptidase (DPP4) inhibitor therapy. Materials and Methods In this phase 4, multicentre, double‐blind, randomized controlled, non‐inferiority trial, patients with T2DM insufficiently controlled by metformin and DPP4 inhibitor combination therapy were randomized to receive either low‐dose or standard‐dose lobeglitazone. The primary endpoint was non‐inferiority of low‐dose lobeglitazone in terms of glycaemic control, expressed as the difference in mean glycated haemoglobin levels at week 24 relative to baseline values and compared with standard‐dose lobeglitazone, using 0.5% non‐inferiority margin. Results At week 24, the mean glycated haemoglobin levels were 6.87 ± 0.54% and 6.68 ± 0.46% in low‐dose and standard‐dose lobeglitazone groups, respectively (p = .031). The between‐group difference was 0.18% (95% confidence interval 0.017‐0.345), showing non‐inferiority of the low‐dose lobeglitazone. Mean body weight changes were significantly greater in the standard‐dose group (1.36 ± 2.23 kg) than in the low‐dose group (0.50 ± 1.85 kg) at week 24. The changes in HOMA‐IR, lipid profile and liver enzyme levels showed no significant difference between the groups. Overall treatment‐emergent adverse events (including weight gain, oedema and hypoglycaemia) occurred more frequently in the standard‐dose group. Conclusions Adding low‐dose lobeglitazone to metformin and DPP4 inhibitor combination resulted in a non‐inferior glucose‐lowering outcome and fewer adverse events compared with standard‐dose lobeglitazone. Therefore, low‐dose lobeglitazone might be one option for individualized strategy in patients with T2DM.

show abstract

Section: Discussionmentioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study

Ryang

Kim

Bae

et al. 2022

Diabetes Obesity Metabolism

View full text Add to dashboard Cite

show abstract

“…This contributes to the enhanced binding affinity of lobeglitazone for PPARγ; docking analysis suggests that the binding affinity of lobeglitazone is 12 times higher than those of rosiglitazone and pioglitazone Diabetes Metab J 2022 Forthcoming. Posted online 2022 https://e-dmj.org [34,38]. TZDs represent peripheral insulin sensitizers [1], but lobeglitazone showed beneficial effects on pancreatic β-cell survival and function in an animal study [2].…”

Section: Discussionmentioning

confidence: 99%

A Real-World Study of Long-Term Safety and Efficacy of Lobeglitazone in Korean Patients with Type 2 Diabetes Mellitus

Kim¹,

Kwon²,

Kim³

et al. 2022

Diabetes Metab J

View full text Add to dashboard Cite

Background: Thiazolidinediones (TZDs) have been associated with various safety concerns including weight gain, bladder cancer, and congestive heart failure (CHF). This study evaluated the efficacy and safety of lobeglitazone, a novel TZD in patients with type 2 diabetes mellitus (T2DM) in real practice. Methods: In this non-interventional, multi-center, retrospective, and observational study conducted at 15 tertiary or secondary referral hospitals in Korea, a total of 2,228 patients with T2DM who received lobeglitazone 0.5 mg for more than 1 year were enrolled. Results: Overall adverse events (AEs) occurred in 381 patients (17.10%) including edema in 1.97% (n=44). Cerebrovascular and cardiovascular diseases were identified in 0.81% (n=18) and 0.81% (n=18), respectively. One case of CHF was reported as an AE. Edema occurred in 1.97% (n=44) of patients. Hypoglycemia occurred in 2.47% (n=55) of patients. Fracture occurred in 1.17% (n=26) of all patients. Lobeglitazone significantly decreased HbA1c level, resulting in a mean treatment difference of -1.05%± page 2 of 11 Kim BY, et al. 2022 Forthcoming. Posted online 2022 https://e-dmj.org 1.35% (P<0.001), and decreased total cholesterol, triglyceride, and low-density lipoprotein cholesterol. However, it increased high-density lipoprotein cholesterol, regardless of statin administration. The patients who received lobeglitazone 0.5 mg showed an apparent reduction in glycosylated hemoglobin (HbA1c) from baseline during the first 6 months of treatment. The HbA1c levels remained stable between months 6 and 42. Conclusion: Lobeglitazone has long-term safety profile, good glycemic-lowering effect and long-term durability of glycemic control in real-world clinical settings.

show abstract

“…Lobeglitazone (LOBE) is a potential peroxisome-proliferator-activated receptor α/γ (PPARα/γ) agonist and a newly developed synthetic thiazolidinedione (TZD) class drug for restoration of insulin sensitivity in type 2 diabetes patients [14]. Although primary function of TZDs is anti-diabetic, TZDs are also reported to possess anti-inflammatory effects [15].…”

Section: Introductionmentioning

confidence: 99%

Lobeglitazone Exerts Anti-Inflammatory Effect in Lipopolysaccharide-Induced Bone-Marrow Derived Macrophages

Jeong

Kim

et al. 2021

Biomedicines

View full text Add to dashboard Cite

The purpose of this study is to elucidate the anti-inflammatory effect of lobeglitazone (LOBE) in lipopolysaccharide (LPS)-induced bone-marrow derived macrophages (BMDMs). We induced nitric oxide (NO) production and pro-inflammatory gene expression through LPS treatment in BMDMs. The changes of NO release and expression of pro-inflammatory mediators by LOBE were assessed via NO quantification assay and a real-time quantitative polymerase chain reaction (RT-qPCR), respectively. In addition, the regulatory effect of LOBE on activation of mitogen-activated protein kinase (MAPK) signaling pathway was investigated by measuring the phosphorylation state of extracellular regulatory protein (ERK) and c-Jun N-terminal kinase (JNK) proteins by Western blot. Our results show that LOBE significantly reduced LPS-induced NO production and pro-inflammatory gene expression of interleukin-1β (IL-1β), IL-6, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and monocyte chemoattractant protein-1 (MCP-1). Moreover, LOBE reduced phosphorylation levels of ERK and JNK of MAPK signaling pathway. In conclusion, LOBE exerts an anti-inflammatory effect in LPS-induced BMDMs by suppression of NO production and pro-inflammatory gene expression, and this effect is potentially through inhibition of the MARK signaling pathway.

show abstract

Lobeglitazone: A Novel Thiazolidinedione for the Management of Type 2 Diabetes Mellitus

Cited by 28 publications

References 56 publications

A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study

A double‐blind, Randomized controlled trial on glucose‐lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase‐4 inhibitor therapy: REFIND study

A Real-World Study of Long-Term Safety and Efficacy of Lobeglitazone in Korean Patients with Type 2 Diabetes Mellitus

Lobeglitazone Exerts Anti-Inflammatory Effect in Lipopolysaccharide-Induced Bone-Marrow Derived Macrophages

Contact Info

Product

Resources

About