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gemigliptin + dapagliflozin (LR 19051 / LR19051)

✓ Approved

LG Chem Ltd. · DPP4 · 小分子

什么是 gemigliptin + dapagliflozin?

gemigliptin + dapagliflozin 是一种小分子,由LG Chem Ltd.研发。该药已获批,用于治疗相关适应症,给药途径:Unknown。

药物档案

商品名LR 19051, LR19051
公司LG Chem Ltd.
药物类别小分子
分子靶点DPP4, SLC5A2
给药途径Unknown
状态Approved

作用机制

分子靶点

gemigliptin + dapagliflozin 作用于 2 个分子靶点:

DPP4dipeptidyl peptidase 4 (CD26, DPPIV)
SLC5A2solute carrier family 5 member 2 (SGLT2)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

gemigliptin + dapagliflozin 针对 1 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Metabolism and nutrition disordersType 2 diabetes mellitus✓ Approved

相关研究文献

PubMedRenal failure2026-09-07

Circadian reprogramming of inflammation and metabolism in chronic kidney disease.

Li Xiao-Qian XQ, Cheng Lei L, Chen Tian-Fen TF, Ma Yi-Nuo YN et al.

Chronic kidney disease (CKD) is driven by inflammation, fibrosis, and metabolic dysfunction. While circadian rhythm dysregulation is well documented in chronic disorders, its specific impact on CKD pathogenesis remains elusive. We performed four-hour interval time-series RNA sequencing on renal tissues from control and CKD mice. We used the JTK_CYCLE algorithm to identify rhythmic genes and categorize them as lost, acquired, or sustained in CKD; we subsequently performed focused bioinformatic analyses. The renal circadian profile was substantially altered; acquired rhythmicity emerged as the dominant pattern, and core clock gene expression was disrupted. Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis revealed that upregulated acquired-rhythmic genes in CKD were enriched in immune-inflammatory pathways; the expression of these genes peaked at Zeitgeber time (ZT) 12-16, consistent with a higher level of renal macrophage infiltration at ZT16 than at ZT0. Conversely, genes associated with nutrient and energy metabolism pathways were downregulated but acquired rhythmicity in CKD. Dapagliflozin improved renal function and restored the circadian expression rhythms of NR1D1 and p-BMAL1. CKD profoundly remodels the renal circadian transcriptome, driving immune-inflammatory and metabolic pathways into maladaptive rhythmicity. Furthermore, dapagliflozin can partially restore the expression of renal core clock genes.

PMID 42703061
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PubMedClinical cardiology2026-09-06

Prospective Evaluation of Quality-of-Life Improvement After Dapagliflozin Initiation in a Greek Population With HFrEF: The EVOLUTION-HF 12-Month Results.

Potoupni Victoria V, Boulmpou Aristi A, Maragkoudakis Spyridon S, Briasoulis Alexandros A et al.

Heart failure with reduced ejection fraction (HFrEF), defined by a left ventricular ejection fraction ≤ 40%, remains a major global health challenge, associated with substantial morbidity, mortality, and impaired quality of life (QoL), particularly in patients with higher NYHA class. Sodium-glucose cotransporter-2 (SGLT2) inhibitors have emerged as a cornerstone therapy for HFrEF, significantly reducing hospitalizations and mortality regardless of glycemic status, sex, race, or comorbidities. EVOLUTION-HF was an observational, multi-center, longitudinal cohort study involving 257 consecutive patients diagnosed with HFrEF who initiated dapagliflozin in a routine clinical setting in Greece. The primary objectives were to characterize baseline demographic and clinical features of patients newly initiated on dapagliflozin for HFrEF and to evaluate dapagliflozin treatment patterns, including discontinuation timing, reasons for discontinuation, and concomitant heart failure and glucose-lowering therapies over time. The secondary objectives are to describe patient-reported outcomes using the KCCQ-23 and to assess adherence to dapagliflozin among patients with HFrEF. A total of 257 patients were enrolled and the follow-up period lasted for 12 months. Significant improvements among all KCCQ-23 scores were observed from baseline to 12-months post dapagliflozin initiation, revealing that the initiation and optimization of guideline-directed medical therapy in routine clinical practice provides improvement to quality of life over time. Dapagliflozin was safe and well-tolerated throughout the observation period. Although benefits are observed in most patients, individuals aged > 65 years, with prior myocardial infarction, or recent hospitalizations show a diminished response, underscoring the need for tailored management and closer follow-up in these higher-risk groups.

PMID 42701883
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PubMedClinics (Sao Paulo, Brazil)2026-09-06

Dapagliflozin as an adjunct to insulin improves glycemic control, weight, and lipid profile with a superior safety profile in type 2 diabetes: a randomized trial.

Sun Lili L, Liu Guiling G, Liang Baozhong B, You Houmei H

To investigate the efficacy and safety of dapagliflozin-insulin combination in patients with Type 2 Diabetes Mellitus (T2DM). In this 3-month, randomized controlled trial, 86 T2DM patients were allocated to either insulin monotherapy (Group A) or dapagliflozin-insulin combination (Group B). Primary endpoints included glycemic control (Fasting Blood Glucose [FBG], 2-hour Postprandial Blood Glucose [2hPBG], Hemoglobin A1c [HbA1c]), lipid profile (Total Cholesterol [TC], Triglycerides [TG], Low-Density Lipoprotein Cholesterol [LDL-C], High-Density Lipoprotein Cholesterol [HDL-C]), anthropometrics (Body Mass Index [BMI], Body Weight [BW]), blood pressure (Systolic Blood Pressure [SBP], Diastolic Blood Pressure [DBP]), and adverse events. After treatment, the combination therapy (Group B) demonstrated significantly greater improvements than insulin alone (Group A). Reductions in Group B versus Group A were: HbA1c (24.9%vs. 10.3%), FBG (23.6%vs. 5.6%), 2hPBG (25.1%vs. 13.7%), TC (35.1%vs. 16.9%), TG (15.9%vs. 11.0%), LDL-C (15.7%vs. 6.5%), SBP (7.3%vs. 3.2%), DBP (12.6%vs. 7.8%), BMI (9.8%vs. 4.3%), and BW (5.4%vs. 3.3%); while HDL-C increased more in Group B (16.3%vs. 9.9%). Group B demonstrated superior benefits in glycemic control, lipid profile, anthropometrics parameters and blood pressure reductions. All post-treatment between-group comparisons were statistically significant (p < 0.05). Critically, the incidence of adverse events was 71.4% lower in Group B, a statistically significant difference (p = 0.007). Dapagliflozin as an adjunct to insulin provides superior multi-faceted metabolic benefits encompassing glycemic control, weight reduction, lipid improvement, and blood pressure lowering, coupled with a more favorable safety profile, supporting its inclusion in standard insulin regimens for T2DM.

PMID 42700538
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PubMedThe American journal of case reports2026-09-06

Primary Care Recognition of Rabson-Mendenhall Syndrome Despite Absence of Classical Diabetic Symptoms.

Al Eisa Abdullah A, Aldayhani Atheer Humoud AH

BACKGROUND Rabson-Mendenhall syndrome (RMS) is an extremely rare autosomal recessive disorder caused by pathogenic variants in the insulin receptor gene, leading to severe insulin resistance and compensatory hyperinsulinemia. Classical features include acanthosis nigricans, non-obese or underweight body habitus, hirsutism, dental abnormalities, dysmorphic features, and variable growth abnormalities. Early recognition may be difficult when the initial presentation is dominated by non-specific symptoms rather than classical metabolic complaints. CASE REPORT A 10-year-old Saudi girl presented to a family medicine clinic with intermittent bilateral leg pain and excessive hunger, without polyuria or polydipsia. Examination revealed extensive acanthosis nigricans, moderate hirsutism, deep voice, high-arched palate, and dental enamel defects. Laboratory evaluation showed severe hyperinsulinemia with insulin level of 3522.5 µU/mL, elevated HbA1c of 8.4% (68 mmol/mol), and biochemical hyperandrogenism. Although RMS is classically associated with growth restriction, the patient was tall for age and had a family history of tall stature, requiring cautious interpretation of growth-related findings. Whole-exome sequencing confirmed a homozygous pathogenic insulin receptor variant (c.433C>T, p.Arg145Cys), establishing the diagnosis of RMS. Treatment included vitamin D supplementation, metformin, basal-bolus insulin therapy, dapagliflozin, home glucose monitoring, diabetes education, dietary counseling, and multidisciplinary follow-up. Glycemic control remained suboptimal despite treatment intensification, reflecting the severe receptor-level insulin resistance associated with RMS. CONCLUSIONS In this patient, marked acanthosis nigricans, severe hyperinsulinemia, hyperglycemia, and hyperandrogenic features supported evaluation for a genetic insulin resistance syndrome despite the absence of classical diabetic symptoms.

PMID 42700438
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PubMedJournal of cardiovascular pharmacology2026-09-04

Effective Protection Against Alcohol-Related Cardiac Damage: Dapagliflozin.

Demirtas Cumaali C, Kılıç Şahhan Ş, Babaoğlu Mert M, Asal Süha S et al.

Chronic alcohol consumption causes serious damage to the liver and cardiovascular system and leads to neoplastic lesions in various organs such as the esophagus, liver, and breast. In our study, we evaluated the protective effects of standard and high doses of dapagliflozin against alcohol-related cardiac damage by utilizing its anti-inflammatory, anti-fibrotic, and anti-cardiac remodeling effects with biochemical and pathological parameters. Twenty male and twenty female Sprague-Dawley rats were used in the experiments. The animals were randomly divided into 5 groups, with 4 males and 4 females in each group. The experimental groups (ALCOHOL, ALCOHOL+DAP, and ALCOHOL+hDAP groups) were given 20% ethyl alcohol intraperitoneally (i.p.) once daily for 28 days. Dapagliflozin (DAP, ALCOHOL+DAP, and ALCOHOL+hDAP groups) and saline solution (CONT and ALCOHOL groups) were administered orally via gavage (o.g.). In the hearts of animals exposed to alcohol, cardiomyocyte hypertrophy, irregular myofiber arrangement, widespread or focal infiltration of inflammatory cells such as neutrophils and lymphocytes, and marked cytoplasmic vacuolization were observed. Treatment with high-dose dapagliflozin alleviated these structural changes. Alcohol caused significant proximal tubular damage. High-dose dapagliflozin resulted in a greater reduction in alcohol-induced renal damage. Although standard dose dapagliflozin improved alcohol-induced impaired Caspas-3, Cytokeratin 18-M30, Cytokeratin 18-M65, TAS, TOS, OSI, MDA, IL-1β, TNF-α, HsCRP, Endothelin-1, IMA, total thiol, native thiol, and disulfide levels, high dose dapagliflozin provided significant improvements (p<0.001). This study suggests that high-dose dapagliflozin (3 mg/kg) may have the potential to regulate mitochondrial function and thiol/disulfide balance in alcohol-related heart damage by inhibiting fibrosis, hypertrophy, apoptosis, inflammation, and oxidative stress through various mechanisms.

PMID 42696673
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PubMedBioscience reports2026-09-04

SGLT2 inhibitor ameliorates hypertension by regulating the CYP4A/20-HETE pathway in the kidney.

Zhou Zhitong Z, Hang Weijian W, Zhao Rui R, Jiang Jiangang J et al.

Sodium-Glucose Transport Protein 2 inhibitors (SGLT2i), initially developed as antidiabetic agents and now established as foundational therapies for heart failure, have also shown antihypertensive effects in clinical trials involving patients with diabetes and heart failure. However, the underlying mechanisms remain incompletely understood. Given the diverse roles of arachidonic acid (AA) and its metabolites in blood pressure regulation, we investigated the antihypertensive effects of SGLT2i in hypertensive patients and an animal model, and explored whether modulation of AA metabolism contributes to these effects. We first confirmed the antihypertensive effects of SGLT2i in a retrospective cohort study and spontaneously hypertensive rats (SHRs). Targeted metabolomic analysis of plasma and tissues from SHRs identified 20-hydroxyeicosatetraenoic acid (20-HETE) originating from the renal cortex as a key metabolite modulated by SGLT2i. Among the enzymes responsible for 20-HETE production, CYP4A but not CYP4F was found to be downregulated by dapagliflozin at both mRNA and protein levels. Immunofluorescence colocalization further localized this effect to proximal tubular epithelial cells, where SGLT2i reduced CYP4A expression and subsequent 20-HETE production, leading to attenuated renal inflammation, fibrosis and blood pressure elevation. Together, these findings not only confirm the antihypertensive effects of SGLT2i but also delineate a novel antihypertensive mechanism by which lower blood pressure, demonstrating that modulation of arachidonic acid metabolism contributes partially to blood pressure-lowering effects.

PMID 42695342
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