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gemigliptin + dapagliflozin (LR 19051 / LR19051)

✓ Approved

LG Chem Ltd. · DPP4 · Small Molecule

What is gemigliptin + dapagliflozin?

gemigliptin + dapagliflozin is a small molecule developed by LG Chem Ltd.. It is approved for therapeutic indications via unknown.

Drug Profile

Brand NamesLR 19051, LR19051
CompanyLG Chem Ltd.
Drug ClassSmall Molecule
Molecular TargetDPP4, SLC5A2
RouteUnknown
StatusApproved
Sources: ClinicalTrials.gov, LG Chem Ltd.

Mechanism of Action

Molecular Targets

gemigliptin + dapagliflozin acts on 2 molecular targets:

DPP4dipeptidyl peptidase 4 (CD26, DPPIV)
SLC5A2solute carrier family 5 member 2 (SGLT2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

gemigliptin + dapagliflozin is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Metabolism and nutrition disordersType 2 diabetes mellitus✓ Approved

Related Research Articles

PubMedJournal of the American Heart Association2026-10-16

Dapagliflozin After Transcatheter Aortic Valve Implantation According to Frailty in DapaTAVI Trial.

Gonzalez-Manzanares Rafael R, Ojeda Soledad S, Amat-Santos Ignacio I, Ariza-Solé Albert A et al.

Frailty is common in patients with severe aortic stenosis undergoing transcatheter aortic valve implantation and portends worse outcomes. Whether the benefit of posttranscatheter aortic valve implantation dapagliflozin differs by frailty is uncertain. In this post hoc analysis, we investigated the efficacy of dapagliflozin according to frailty status in the DapaTAVI (Dapagliflozin in Patients Undergoing Transcatheter Aortic Valve Implantation) trial. Frailty was assessed through the Fatigue, Resistance, Ambulation, Illnesses, and Loss of Weight scale (robust=0, prefrail=1-2, frail=3-5). The primary outcome was the composite of all-cause death or worsening heart failure at 1 year. Among 1222 patients with baseline frailty assessment, 47.2% were frail, 40.3% prefrail, and 12.4% robust. Over 12 months, 215 patients (17.6%) experienced the primary end point. Patients who were prefrail and frail had higher risk than robust patients (adjusted hazard ratios [HRs], 1.88 [95% CI, 1.05-3.38] and 2.29 [1.29-4.07], respectively; P=0.004). Dapagliflozin was associated with a lower risk of the primary end point in patients who were frail (HR, 0.53 [95% CI, 0.36-0.77]) but not in those who were prefrail (HR, 1.01 [95% CI, 0.66-1.55]) or robust patients (HR, 1.26 [95% CI, 0.42-3.75]); P for interaction=0.021. There was no evidence that frailty modified the safety profile of dapagliflozin. Frailty was common and independently associated with worse outcomes after transcatheter aortic valve implantation. Dapagliflozin appeared to confer greater relative benefit in patients with frailty.

PMID 42885795
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PubMedBMC endocrine disorders2026-10-16

Effects of SGLT-2 inhibitors on thyroid-stimulating hormone and systemic immune-inflammation index in type 2 diabetes: a retrospective study.

Bayram Seyit Murat SM, Demirci Hüseyin H, Üçgül Enes E, Canlar Şule Ş et al.

This retrospective study examined whether long-term SGLT-2i use is associated with differences in thyroid-stimulating hormone (TSH) and the systemic immune-inflammation index (SII) in patients with type 2 diabetes mellitus (T2DM) without known thyroid disease. The neutrophil-to-lymphocyte ratio (NLR), renal function (eGFR), diabetes duration, and metformin use were also evaluated as potential covariates. This was a single-center, retrospective observational study. Adults with T2DM who had used empagliflozin or dapagliflozin for at least six months were compared with an age- and sex-matched control group of patients with T2DM not using SGLT-2i, drawn from the same outpatient clinics. Key exclusion criteria included known thyroid disease, known positivity for thyroid autoantibodies, active inflammatory or autoimmune processes, advanced organ failure, and immunomodulatory treatment. TSH, SII, and NLR were measured. Statistical analyses included intergroup comparisons, correlation, multivariate linear regression, post-hoc power calculation, and multicollinearity diagnostics (variance inflation factor, VIF). The study included 330 patients across the empagliflozin (n = 139), dapagliflozin (n = 85), and control (n = 106) groups. Median TSH (1.6, 1.8, and 1.9 µIU/mL; p = 0.338) and SII (481, 531, and 468.5; p = 0.509) did not differ significantly between groups. SII and NLR were significantly correlated (r = 0.467, p < 0.001). In multivariate regression, female sex (B = 0.161, p = 0.015) and eGFR (B=-0.0043, p = 0.037) were independent predictors of log-transformed TSH; SGLT-2i use, SII, NLR, age, metformin use, and diabetes duration were not. The study had 80% power to detect a Cohen's f of 0.17 or greater; observed effect sizes were substantially below this threshold (f = 0.02 for TSH, f ≈ 0.00 for SII). Long-term SGLT-2i use was not associated with significant changes in TSH or SII in patients with T2DM without known thyroid disease, and the achieved effect sizes suggest that any true effect, if present, is likely small. Renal function emerged as an independent correlate of TSH, suggesting that the relationship between the hypothalamic-pituitary-thyroid axis and renal physiology merits further attention in this population, independent of SGLT-2i exposure. Prospective, multicenter studies incorporating free thyroxine and triiodothyronine measurements are warranted to further clarify these relationships. This study is retrospective and does not involve a clinical trial registration.

PMID 42881387
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PubMedInternational journal of molecular sciences2026-10-16

The Influence of SGLT2 Inhibitors on the Immune System and Inflammatory Processes in Kidney Transplantation.

García-Sánchez Andrés A, Ortíz-Lazareno Pablo P, Pazarín-Villaseñor Leonardo L, Díaz-de la Cruz Elodia Nataly EN et al.

Kidney transplantation (KT) remains the optimal therapy for end-stage kidney disease (ESKD), yet long-term graft survival is limited by unremitting allograft dysfunction and non-immune treatment toxicities. Sterile inflammation primarily drives graft failure. This inflammatory process releases damage-associated molecular patterns (DAMPs). DAMPs activate pattern recognition receptors (PRRs), such as Toll-like receptors (TLRs) 2 and 4, from proximal tubule epithelial cells, endothelial compartments, and infiltrating myeloid lineages. PRR signaling and the release of pro-inflammatory cytokines (IL-1β, IL-18, TNF-α) promote pro-inflammatory M1 macrophage polarization and accelerate interstitial fibrosis and tubular atrophy (IFTA). While maintenance immunosuppression prevents adaptive rejection, it causes severe metabolic, cardiovascular, and oncologic complications, including post-transplant diabetes mellitus, hypertension, and malignancies. Sodium-glucose cotransporter 2 (SGLT2) inhibitors (dapagliflozin, empagliflozin, canagliflozin) have emerged as novel disease-modifying, immunomodulatory adjuncts that act independently of glycemic control. SGLT2 inhibition reactivates tubuloglomerular feedback to relieve intraglomerular hypertension, blunts hyperfiltration, and reduces tubular transport workload. This alleviates cortical hypoxia, curtails mitochondrial ROS production, and activates AMP-activated protein kinase (AMPK) to suppress NF-κB and NLRP3 inflammasome assembly. SGLT2 inhibitors downregulate TLR expression, drive a phenotypic shift toward reparative M2 macrophages, reduce proteinuria, and provide sustained volume decongestion without triggering compensatory activation of the renin-angiotensin-aldosterone system. By targeting both upstream bioenergetic strain and downstream fibrotic remodeling (YAP/TAZ axis), SGLT2 inhibitors complement standard immunosuppression to protect allograft architecture, reduce cardiovascular morbidity, and improve long-term transplant outcomes.

PMID 42883794
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PubMedOrganic & biomolecular chemistry2026-10-15

Nickel-catalyzed one-pot C-H alkylation of (hetero)arenes enabled by in situ electrophilic iodination and reductive coupling with alkyl pyridinium salts.

Zhang Yongming Y, Wu Fan F, Ni Feng F

Herein, we report a practical one-pot protocol for the formal C(sp2)-H alkylation of (hetero)arenes by combining in situ I2/Selectfluor-mediated electrophilic iodination with nickel-catalysed reductive cross-coupling using readily accessible alkyl pyridinium salts. The transformation exhibits a broad arene scope and tolerates various functional groups and a range of heterocycles. Importantly, late-stage functionalization of complex bioactive molecules, including dapagliflozin, aniracetam, clofibrate and fenofibrate derivatives, is demonstrated. This method utilized two abundant chemical feedstocks for forging C(sp2)-C(sp3) bonds, offering a versatile and operationally simple entry to alkylarenes.

PMID 42877948
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PubMedDiabetes research and clinical practice2026-10-14

Dapagliflozin and 54-week kidney function in kidney transplant recipients with post-transplant diabetes mellitus: a randomized controlled trial.

Li Jinghui J, Fu Zhirong Z, Xu Rongkun R, Zhuang Yanqian Y et al.

To evaluate dapagliflozin effects on kidney function and safety in kidney transplant recipients with post-transplant diabetes mellitus (PTDM). In this single-center, prospective, open-label randomized trial, 68 participants were assigned 1:1 to dapagliflozin 10 mg daily plus standard care or standard care alone. Week-54 observed-data analyses included 27 participants per group; an intention-to-treat multiple-imputation sensitivity analysis included all randomized participants. At week 54, the baseline-adjusted between-group eGFR difference was 6.81 mL/min/1.73 m2 (95 % CI, 1.68 to 11.94; P = 0.010) in the complete-case analysis and 6.05 mL/min/1.73 m2 (95 % CI, 0.99 to 11.11; P = 0.020) after multiple imputation. The estimate was attenuated after additional multivariable adjustment, with the 95 % CI including no difference. Serum magnesium declined less with dapagliflozin, whereas HbA1c and tacrolimus trough concentrations were similar. Observed adverse-event frequencies were similar between groups, although the trial was not powered to assess uncommon safety events. Dapagliflozin showed an exploratory week-54 eGFR signal, but the estimate was sensitive to covariate adjustment and missing-data assumptions. This small trial does not establish a definitive clinically meaningful kidney benefit.

PMID 42874781
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PubMedCurrent diabetes reviews2026-10-14

Gliflozin-Derived SGLT2 Inhibitors: Recent Advances and Future Perspectives in the Management of Type 2 Diabetes.

Prusty Biswanath B, Rout Sudhansu Sekhar SS, Saha Abhijit A

Gliflozin derivatives, a class of Sodium-Glucose Cotransporter (SGLT) inhibitors, have emerged as effective antidiabetic agents offering notable cardiovascular and renal protection. This class of compounds inhibits glucose reabsorption in the kidneys, thereby improving overall glycaemic control. This review provides a comprehensive overview of gliflozin derivatives, emphasizing their chemical characterization, safety, therapeutic efficacy, pharmacokinetic analysis, and potential future applications, focusing on clinical trials and new developments released between 2010 and 2026. Gliflozin derivatives slow the progression of chronic kidney disease and reduce the risk of heart failure. Some preliminary experimental evidence has reported the antibacterial activity of canagliflozin against MRSA. The Gliflozin derivatives dapagliflozin (IC50 =1.1nM), ertugliflozin (IC50 =0.9nM), sotagliflozin (IC50 =1.8nM), and bexagliflozin (IC50 =2.3nM), which has core motif, 1-chloro-2-(4-alkoxy benzyl) benzene as an aglycon unit and a glycon unit bind with SGLT2 receptor and lowered the HbA1c by 1.2%, 1.7%, 0.41% and 0.80%, respectively. Its selectivity, pharmacokinetics, and toxicity profiles are also optimal. Recent studies have demonstrated their involvement in conditions other than diabetes, including obesity, non-alcoholic fatty liver disease, Cardioprotective, Nephroprotective, Anti-inflammatory, and antihypertensive effects. Gliflozin derivatives represent a paradigm shift in the management of diabetes and have broad therapeutic potential. Future studies should emphasize creative structural changes to increase safety and efficacy.

PMID 42872647
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