Long-Term Safety and Efficacy of Sitagliptin for Type 2 Diabetes Mellitus in Japan: Results of a Multicentre, Open-Label, Observational Post-Marketing Surveillance Study

Yoshikawa, Kiwamu; Tsuchiya, Akira; Kido, Teruhiko; Ota, Tomohiro; Ikeda, Keiko; Iwakura, Mika; Maeda, Yoshikazu; Maekawa, Shinichiroh

doi:10.1007/s12325-020-01293-2

Cited by 8 publications

(10 citation statements)

References 28 publications

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“…In terms of effectiveness, the current study confirmed the glucose‐lowering effects of linagliptin use in Korean patients with T2D in a real‐world setting. The mean changes in HbA1c were similar to the results of the Japanese PMS studies, 9,10 a pooled analysis of data from Asian patients, 16 and PMS studies of other DPP‐4 inhibitors 13–15 . Our subgroup analysis also revealed that blood glucose levels were effectively reduced in all linagliptin‐treated patients categorized by various clinical factors.…”

Section: Discussionsupporting

confidence: 81%

“…The mean changes in HbA1c were similar to the results of the Japanese PMS studies, 9,10 a pooled analysis of data from Asian patients, 16 and PMS studies of other DPP-4 inhibitors. [13][14][15] Our subgroup analysis also revealed that blood glucose levels were effectively reduced in all linagliptin-treated patients categorized by various clinical factors. However, the glucose-lowering effects were more pronounced in patients with a shorter duration of T2D, lower BMI values, higher baseline HbA1c, no history of diabetic complications, no history of dyslipidaemia, and in those not using sulphonylureas at all.…”

Section: Discussionmentioning

confidence: 53%

“…However, in those previous studies, gastrointestinal disorder was also one of the most frequent ADRs. Furthermore, in the PMS studies of other DPP‐4 inhibitors such as sitagliptin, vildagliptin and teneligliptin, hypoglycaemia and gastrointestinal disorders were the major ADRs 13–15 …”

Section: Discussionmentioning

confidence: 99%

“…Furthermore, in the PMS studies of other DPP-4 inhibitors such as sitagliptin, vildagliptin and teneligliptin, hypoglycaemia and gastrointestinal disorders were the major ADRs. [13][14][15] We assumed that the shorter observation period in the current PMS study (24 weeks) was a reason for the comparatively low incidence of ADRs, and the different composition of the ADRs. When we analysed patients treated with linagliptin monotherapy separately, there was no significant difference in the incidence of ADRs compared with the combination group, which was consistent with previous PMS studies 9,10 (data not shown).…”

Section: Discussionmentioning

confidence: 99%

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Safety and effectiveness of linagliptin in Korean patients with type 2 diabetes: A postmarketing surveillance study

Bae

Song

Park

et al. 2021

Diabetes Obesity Metabolism

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We designed a postmarketing surveillance study of linagliptin for patients with type 2 diabetes (T2D) in Korea. This prospective, observational, multicentre study investigated the safety and glycaemic effectiveness of linagliptin as monotherapy or combination therapy with other antidiabetic drugs in routine clinical practice. Endpoints were the incidence of adverse drug reactions (ADRs) and the change in HbA1c. Overall, 3119 and 2171 patients were included in the safety and effectiveness analysis sets, respectively. A total of 56 patients (1.8%) experienced ADRs. The most common ADR was gastrointestinal disorders (0.7%), followed by metabolism and nutrition disorders (0.5%). ADRs of special interest, including pancreatic diseases, cardiac diseases and hypoglycaemia, occurred in 12 patients, 11 of whom had hypoglycaemia, while one had a skin lesion. Mean HbA1c change during the study period was −0.8%.Lower body mass index, shorter diabetes duration and higher baseline HbA1c were independently associated with a better effectiveness, while the presence of diabetic complications, dyslipidaemia and the use of sulphonylureas were associated with a poor response. In conclusion, linagliptin showed an excellent safety profile and glycaemic effectiveness in Korean patients with T2D.

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Section: Discussionsupporting

confidence: 81%

Section: Discussionmentioning

confidence: 53%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Safety and effectiveness of linagliptin in Korean patients with type 2 diabetes: A postmarketing surveillance study

Bae

Song

Park

et al. 2021

Diabetes Obesity Metabolism

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“…For example, in an observational post-marketing surveillance study, long-term sitagliptin use was not associated with additional safety concerns in type 2 diabetic patients. 80 Even if there were to be an increase in the systemic exposure of sitagliptin by twofold, it would be unlikely to result in any clinically relevant adverse event. 2,28 Even higher doses such as 800 mg single dose and 600 mg multiple doses have been shown to be tolerated well.…”

Section: Surrogate Techniques For In Vivo Bioequivalence (Be) Testingmentioning

confidence: 99%

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Sitagliptin Phosphate Monohydrate

Charoo¹,

Abdallah

Bakheit

et al. 2022

Journal of Pharmaceutical Sciences

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Evaluation of the anti-diabetic drug sitagliptin as a novel attenuate to SARS-CoV-2 evidence-based in silico: molecular docking and molecular dynamics

et al. 2022

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The current outbreak of COVID-19 cases worldwide has been responsible for a significant number of deaths, especially in hospitalized patients suffering from comorbidities, such as obesity, diabetes, hypertension. The disease not only has prompted an interest in the pathophysiology, but also it has propelled a massive race to find new anti-SARS-CoV-2 drugs. In this scenario, known drugs commonly used to treat other diseases have been suggested as alternative or complementary therapeutics. Herein we propose the use of sitagliptin, an inhibitor of dipeptidyl peptidase-4 (DPP 4 ) used to treat type-II diabetes, as an agent to block and inhibit the activity of two proteases, 3CL pro and PL pro , related to the processing of SARS-CoV-2 structural proteins. Inhibition of these proteases may possibly reduce the viral load and infection on the host by hampering the synthesis of new viruses, thus promoting a better outcome. In silico assays consisting in the modeling of the ligand sitagliptin and evaluation of its capacity to interact with 3CL pro and PL pro through the prediction of the ligand bioactivity, molecular docking, overlapping of crystal structures, and molecular dynamic simulations were conducted. The experiments indicate that sitagliptin can interact and bind to both targets. However, this interaction seems to be stronger and more stable to 3CL pro (ΔG = −7.8 kcal mol −1 ), when compared to PL pro (ΔG = −7.5 kcal mol −1 ). This study suggests that sitagliptin may be suitable to treat COVID-19 patients, beyond its common use as an anti-diabetic medication. In vivo studies may further support this hypothesis.

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Long-Term Safety and Efficacy of Sitagliptin for Type 2 Diabetes Mellitus in Japan: Results of a Multicentre, Open-Label, Observational Post-Marketing Surveillance Study

Cited by 8 publications

References 28 publications

Safety and effectiveness of linagliptin in Korean patients with type 2 diabetes: A postmarketing surveillance study

Safety and effectiveness of linagliptin in Korean patients with type 2 diabetes: A postmarketing surveillance study

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Sitagliptin Phosphate Monohydrate

Evaluation of the anti-diabetic drug sitagliptin as a novel attenuate to SARS-CoV-2 evidence-based in silico: molecular docking and molecular dynamics

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