Safety and efficacy of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 52 weeks: An open-label extension study

Kim, Sun Hwa; Kim, Sin Gon; Kim, Doo Man; Woo, Jeong Taek; Jang, Hak Chul; Chung, Choon Hee; Ko, Kyung Soo; Park, Jeong Hyun; Park, Yong Soo; Kim, Sang Jin; Choi, Dong Seop

doi:10.1016/j.diabres.2015.09.009

Cited by 24 publications

(34 citation statements)

References 10 publications

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“…Previous studies have shown that pioglitazone treatment increases body weight between 2.5 and 4.7 kg, depending on the study (23)(24)(25). In our study, lobeglitazone treatment showed a lower increase in the average body weight of 1.4 kg (from 76.5 ± 11.1 kg to 77.9 ± 11.8 kg [P = 0.001]), which is similar to the weight gain, ranging from 0.89 to 1.48 kg, that was observed in other clinical trials using 0.5 mg/day lobeglitazone (15)(16)(17).…”

Section: Discussionsupporting

confidence: 83%

“…Recently, a novel TZD called lobeglitazone was developed, and is currently being prescribed for T2D in Korea (14). The efficacy and safety of lobeglitazone in T2D has been well-investigated (15)(16)(17). To identify better treatment options for T2D patients with NAFLD, we investigated the effects of lobeglitazone on these patients by analyzing alterations in their CAP values using transient liver elastography, as well as in their glycemic, lipid, and liver profiles.…”

Section: Introductionmentioning

confidence: 99%

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Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness

Lee

Kim

et al. 2017

J Korean Med Sci

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Despite the rapidly increasing prevalence of non-alcoholic fatty liver disease (NAFLD) in type 2 diabetes (T2D), few treatment modalities are currently available. We investigated the hepatic effects of the novel thiazolidinedione (TZDs), lobeglitazone (Duvie) in T2D patients with NAFLD. We recruited drug-naïve or metformin-treated T2D patients with NAFLD to conduct a multicenter, prospective, open-label, exploratory clinical trial. Transient liver elastography (Fibroscan®; Echosens, Paris, France) with controlled attenuation parameter (CAP) was used to non-invasively quantify hepatic fat contents. Fifty patients with CAP values above 250 dB/m were treated once daily with 0.5 mg lobeglitazone for 24 weeks. The primary endpoint was a decline in CAP values, and secondary endpoints included changes in components of glycemic, lipid, and liver profiles. Lobeglitazone-treated patients showed significantly decreased CAP values (313.4 dB/m at baseline vs. 297.8 dB/m at 24 weeks; P = 0.016), regardless of glycemic control. Lobeglitazone improved HbA1C values (7.41% [57.5 mM] vs. 6.56% [48.2 mM]; P < 0.001), as well as the lipid and liver profiles of the treated patients. Moreover, multivariable linear regression analysis showed that hepatic fat reduction by lobeglitazone was independently associated with baseline values of CAP, liver stiffness, and liver enzymes, and metformin use. Lobeglitazone treatment reduced intrahepatic fat content, as assessed by transient liver elastography, and improved glycemic, liver, and lipid profiles in T2D patients with NAFLD. Further randomized controlled trials using liver histology as an end point are necessary to evaluate the efficacy of lobeglitazone for NAFLD treatment (Clinical trial No. NCT02285205).

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Section: Discussionsupporting

confidence: 83%

Section: Introductionmentioning

confidence: 99%

Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness

Lee

Kim

et al. 2017

J Korean Med Sci

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“…2,6 Even although this study and the previous studies with lobeglitazone were too short to evaluate the long-term AEs, there was no report regarding any incidence of bladder cancer, which stopped the use of pioglitazone. 6,7,11,15 This result might be explained by their different excretory routes, mainly through faeces. 15 Currently, the utility of TZDs tends to be underestimated because of the considerable focus on safety concerns.…”

Section: Discussionmentioning

confidence: 99%

Efficacy and safety of lobeglitazone versus sitagliptin as an add‐on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24 weeks

Kim

Yoon

et al. 2020

Diabetes Obesity Metabolism

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We aimed to evaluate the efficacy and safety profile of lobeglitazone compared with sitagliptin as an add‐on to metformin in patients with type 2 diabetes as well as other components of metabolic syndrome. Patients inadequately controlled by metformin were randomly assigned to lobeglitazone (0.5 mg, n = 121) or sitagliptin (100 mg, n = 126) for 24 weeks. The mean changes in HbA1c of the lobeglitazone and sitagliptin groups were −0.79% and −0.86%, respectively; the between‐group difference was 0.08% (95% confidence interval, −0.14% to 0.30%), showing non‐inferiority. The proportion of patients having two or more factors of other metabolic syndrome components decreased to a greater extent in the lobeglitazone group than in the sitagliptin group (−11.9% vs. −4.8%; P < .0174). Favourable changes in the lipid metabolism were also observed with lobeglitazone, which had a similar safety profile to sitagliptin. Lobeglitazone was comparable with sitagliptin as an add‐on to metformin in terms of efficacy and safety.

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“…In contrast to other TZDs, lobeglitazone is mainly excreted in the feces, reducing the concerns about the risk of bladder cancer in the mice [44] and rats [45]. In the study of lobeglitazone in patients with T2DM, lobeglitazone showed a favorable balance of efficacy and safety during the extension study [46]. In pharmacokinetic studies in healthy adults, lobeglitazone was well tolerated and did not significantly affect the pharmacokinetics of metformin or vice versa [47].…”

Section: Ppar Ligand Therapeutics In Diabetes Mellitusmentioning

confidence: 99%

The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development

Hong

Zhai

2018

IJMS

111

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Peroxisome proliferator-activated receptors (PPARs) are a well-known pharmacological target for the treatment of multiple diseases, including diabetes mellitus, dyslipidemia, cardiovascular diseases and even primary biliary cholangitis, gout, cancer, Alzheimer’s disease and ulcerative colitis. The three PPAR isoforms (α, β/δ and γ) have emerged as integrators of glucose and lipid metabolic signaling networks. Typically, PPARα is activated by fibrates, which are commonly used therapeutic agents in the treatment of dyslipidemia. The pharmacological activators of PPARγ include thiazolidinediones (TZDs), which are insulin sensitizers used in the treatment of type 2 diabetes mellitus (T2DM), despite some drawbacks. In this review, we summarize 84 types of PPAR synthetic ligands introduced to date for the treatment of metabolic and other diseases and provide a comprehensive analysis of the current applications and problems of these ligands in clinical drug discovery and development.

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Safety and efficacy of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 52 weeks: An open-label extension study

Cited by 24 publications

References 10 publications

Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness

Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness

Efficacy and safety of lobeglitazone versus sitagliptin as an add‐on to metformin in patients with type 2 diabetes with two or more components of metabolic syndrome over 24 weeks

The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development

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