remogliflozin etabonate + vildagliptin (Remozen V / Remo V)

✓ Approved

Glenmark Pharmaceuticals Limited · DPP4 · 小分子

什么是 remogliflozin etabonate + vildagliptin？

remogliflozin etabonate + vildagliptin 是一种小分子，由Glenmark Pharmaceuticals Limited研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名	Remozen V, Remo V
公司	Glenmark Pharmaceuticals Limited
药物类别	小分子
分子靶点	DPP4, SLC5A2
给药途径	Oral (PO)
状态	Approved

来源： ClinicalTrials.gov, Glenmark Pharmaceuticals Limited

作用机制

分子靶点

remogliflozin etabonate + vildagliptin 作用于 2 个分子靶点：

DPP4	dipeptidyl peptidase 4 (CD26, DPPIV)
SLC5A2	solute 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

remogliflozin etabonate + vildagliptin 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 disorders	Type 2 diabetes mellitus	✓ Approved

相关研究文献

PubMedCureus2026-08-02

Probable Vildagliptin-Associated Acute Pancreatitis in a Patient With Well-Controlled Type 2 Diabetes Mellitus: A Case Report.

Aung Kyaw Zin KZ, Saw Naw Eh Law NEL

Drug-induced acute pancreatitis (DIAP) is rare, accounting for approximately 0.1%-5% of all cases, and the association between dipeptidyl peptidase-4 (DPP-4) inhibitors and pancreatitis remains controversial despite postmarketing safety signals. We report the case of a 46-year-old man with well-controlled type 2 diabetes mellitus who presented with severe epigastric pain radiating to the back after six months of therapy with vildagliptin and metformin. Laboratory evaluation showed markedly elevated serum amylase (1,220 U/L) and lipase (2,334 U/L), exceeding three times the upper limit of normal, while contrast-enhanced CT demonstrated acute interstitial edematous pancreatitis without evidence of necrosis. A systematic evaluation excluded common etiologies, including gallstones, alcohol use, hypertriglyceridemia, hypercalcemia, pancreaticobiliary obstruction, and structural abnormalities. Vildagliptin was promptly discontinued, and the patient received supportive management, with complete clinical recovery. The temporal association, exclusion of alternative causes, and improvement following drug withdrawal (positive dechallenge), together with a Naranjo Adverse Drug Reaction Probability Scale score of 7, support a probable drug-related association, with vildagliptin considered the most likely causative agent. Clinicians should remain aware of this rare but potential adverse effect when evaluating patients receiving DPP-4 inhibitors who present with acute pancreatitis after exclusion of more common causes.

PMID 42539684

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PubMedbioRxiv : the preprint server for biology2026-07-29

Effect of Immunosuppressive Drugs on Glucose-Stimulated Insulin Secretion: Concentration-Response Studies in Dynamic Perifusion Assays.

Chuang Sung-Ting ST, Watts Brandon B, Alcazar Oscar O, Buchwald Peter P

Immunosuppressive drugs, which are required to maintain graft function in transplant recipients, are associated with many unavoidable side effects including posttransplant diabetes mellitus (PTDM) that involves both peripheral insulin resistance and impairment of insulin secretion. To characterize in detail the concentration-dependency of the effect of well-known immunosuppressive drugs on glucose-stimulated insulin secretion (GSIS), we performed dynamic perifusion studies with human pancreatic islets. The effect on the time-profile of GSIS has been assessed over a wide concentration range for several clinically relevant immunomodulatory therapies, including small-molecule drugs (cyclosporine, sirolimus, tacrolimus, prednisolone acetate, and loteprednol etabonate) and biologics (abatacept and anti-CD40L), plus a prospective β-cell proliferation-inducing agent (harmine). While biologics showed no significant detrimental effects after one-day treatment even at relatively high concentrations (5 μM), all small-molecule drugs inhibited insulin secretion in a concentration-dependent manner, although glucocorticoids showed a distinct response pattern. Calcineurin and mTOR inhibitors preserved GSIS within their therapeutic ranges but progressively distorted its time-profile at higher concentrations and completely suppressed secretion at the highest levels. Cyclosporine exhibited the least, only about 35-fold, separation between its therapeutic target (C targ) and half-maximal GSIS inhibitory (IC50) concentrations. Glucocorticoids did not alter the shape of the time-profile but inhibited overall insulin secretion even at therapeutic levels. Their inhibitory effect only increased slowly with concentration and did not follow a classic sigmoid pattern that has unity Hill slope. These findings establish quantitative benchmarks for immunosuppressant-induced β-cell toxicity and provide a framework for optimizing immunosuppressive regimens to reduce the risk of PTDM.

PMID 42523260

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PubMedJournal of clinical medicine2026-07-15

Evaluating Lacrimal Punctum Size as a Clinical Indicator of Dry Eye Disease Severity in a Real-World Lebanese Cohort.

Tlaiss Yehya Y, Warrak John J, Warrak Elias E

Background/Objectives: To investigate the relationship between lacrimal punctum size and the severity of dry eye disease (DED) in a clinically refractory, real-world patient cohort from a tertiary ophthalmology center in Lebanon. Methods: A retrospective observational study was conducted at Advanced Eye Care Center, Beirut, Lebanon (2016-2024). A total of 312 eyes from 156 patients with moderate-to-severe DED unresponsive to topical artificial tears, loteprednol etabonate, and cyclosporine (0.05% ophthalmic emulsion) were included. All eyes subsequently underwent lower lacrimal punctum plug insertion as part of clinical management. Lacrimal punctal diameter was estimated by the largest silicone plug (0.5 mm, 0.6 mm, or 0.7 mm) inserted nonforcefully into the lower punctum under slit-lamp visualization. Tear film stability was assessed by Tear Break-Up Time (TBUT). Group differences were analyzed using the Kruskal-Wallis H test with post hoc Mann-Whitney U tests (Bonferroni correction), and Spearman's rank correlation was calculated to quantify the monotonic association. Results: Eyes were distributed across punctal diameter categories as follows: 0.5 mm (n = 15, 4.8%), 0.6 mm (n = 204, 65.4%), and 0.7 mm (n = 93, 29.8%). Median TBUT values were 5.55 s [IQR 5.51-5.77], 5.06 s [IQR 4.80-5.37], and 4.51 s [IQR 4.23-4.71] for the 0.5 mm, 0.6 mm, and 0.7 mm groups, respectively. Kruskal-Wallis analysis confirmed significant inter-group differences (H = 140.1, p < 0.001). All post hoc pairwise comparisons remained significant after Bonferroni correction (p < 0.001). Spearman's rank correlation demonstrated a significant negative association between lacrimal punctal diameter and TBUT (ρ = -0.70, p < 0.000001). All analyses were conducted at the eye level and do not account for within-patient correlation (bilateral design, 156 patients); p-values should be interpreted accordingly. Conclusions: In this treatment-refractory cohort, larger lacrimal punctal diameter was significantly associated with greater tear film instability. These findings suggest that lacrimal punctal diameter estimation during therapeutic plug insertion may serve as a practical, cost-free adjunct to standard DED evaluation. Prospective multimodal studies are needed to validate punctal diameter as an independent clinical indicator of DED severity.

PMID 42452448

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PubMedBMC pregnancy and childbirth2026-07-14

Comparison of the permeability of DPP-4 inhibitors-sitagliptin, vildagliptin, linagliptin, and alogliptin-in placental barrier cell models and exploration of their transport mechanisms by LC-MS/MS.

Bai Mengru M, Shen Qian Q, Wu Yong Y, Chen Mingyang M et al.

Uncontrolled hyperglycemia in pregnancy poses risks to both mother and fetus, but treatment options are limited. Sitagliptin, vildagliptin, linagliptin, and alogliptin are dipeptidyl peptidase-4 (DPP-4) inhibitors effective in type 2 diabetes. However, data on their placental transfer and safety in pregnant women is lacking. Therefore, this study compared the permeability of these drugs in multiple placental cell models, including BeWo, HTR-8/SVneo, and primary human trophoblast cells, and attempted to explore their transport mechanisms. A cost-effective liquid chromatography-tandem mass spectrometry method was developed and validated to quantify the four DPP-4 inhibitors. The accumulation of these drugs in placental cell models was compared, and the BeWo Transwell transport assay was conducted to assess transport rates. Transporter inhibitors, siRNA knockdown, and transporter overexpression cell models were used to explore the transmembrane transport mechanism of these drugs. Linagliptin had the highest accumulation in placental cells, followed by alogliptin, sitagliptin, and vildagliptin. The apparent permeability coefficient of linagliptin, alogliptin and sitagliptin was similar in BeWo cells, while vildagliptin was the lowest. The accumulation of linagliptin, alogliptin, sitagliptin and vildagliptin in BeWo cells at 37 °C were significantly higher than those at 4 °C, indicating the presence of carrier-mediated uptake. However, studies using transporter inhibitors, siRNA knockdown, and transporter overexpression cell models showed that equilibrative nucleoside transporters (ENTs), concentrative nucleoside transporters (CNTs), and organic anion transporter (OAT) 4 do not facilitate the placental transfer of linagliptin, alogliptin, sitagliptin, and vildagliptin. Vildagliptin had the lowest accumulation and permeability in placental cells among the four DPP-4 inhibitors. There might be carrier-mediated transmembrane transport of linagliptin, alogliptin, sitagliptin and vildagliptin, but ENTs, CNTs and OAT4 were not involved in. This study provides a basis for future research on their safety during pregnancy.

PMID 42443801

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PubMedChemistry & biodiversity2026-06-30

Structure-Based De Novo Design of Novel Dual DPP IV and PTP 1B Inhibitors (DDPI's).

Singh Yogesh Y, Thareja Suresh S

Inhibition of DPP IV and PTP 1B constitutes a legitimate approach in modulating glucose homeostasis, thereby representing a viable therapeutic strategy for managing T2DM. This study employed a novel structure-based de novo design approach for developing dual DPP IV and PTP 1B inhibitors (DDPI's) with synergistic anti-hyperglycemic potential to effectively manage T2DM. By leveraging high-resolution protein structures, a specialized ligand library was designed employing a de novo approach to perform virtual screening. Molecular docking studies revealed four promising lead candidates, that is, YS-3, YS-5, YS-14, and YS-15 (>-138.26 kcal/mol in DPP IV while >-150.29 kcal/mol in PTP1B), with higher binding affinities as compared to clinical standard inhibitors, Vildagliptin (-103.46 kcal/mol; DPP IV) and Ertiprotafib (-141.91 kcal/mol; PTP 1B). Further, molecular dynamics (MD) and MM-GBSA analyses were performed to comprehend the thermodynamic stability of these leads. Analysis of 100 ns trajectories, integrating depth-based PCA, FEL, and DSSP, enabled identification of key intermolecular contacts responsible for the dual inhibitory behavior. DFT-based electronic profiling and ADMET predictions confirmed the biological viability and drug-like properties. These findings provide a robust structural blueprint for DDPI's with improved affinity, along with a better understanding of the inhibitory mechanisms.

PMID 42378400

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PubMedScientific reports2026-06-26

Simple and cost-effective UV spectrophotometric platforms integrating advanced green and blue metrics for concurrent analysis of dapagliflozin and vildagliptin in diabetes therapy.

Darweish Eman E, Hashem Hisham A HA, Nasr Rawan R, Bahgat Eman A EA

The co-administration of dapagliflozin (DPF) and vildagliptin (VLT) in tablet dosage forms is a clinically established strategy for managing of type 2 diabetes mellitus and has demonstrated favorable therapeutic outcomes. Nevertheless, the simultaneous quantitative determination of both drugs remains challenging because of the severe overlap in their UV absorption spectra, with λmax values at 224 nm for DPF and 214 nm for VLT. In this study, novel eco-friendly UV spectrophotometric methods were developed and validated for the accurate determination of DPF and VLT in their combined pharmaceutical formulations. The proposed methods include Fourier deconvolution, mean centering, dual wavelength, and induced dual wavelength techniques, which allow precise, reliable, and sensitive analysis without the need for prior separation. These approaches are simple, minimize noise in ratio spectra, and require limited mathematical manipulation, thereby reducing analysis time. DPF and VLT showed linear responses over concentration ranges of 2-24 µg/mL and 10-100 µg/mL, respectively. The limits of detection ranged from 0.00486 to 0.7979 µg/mL for DPF and from 0.0185 to 0.8690 µg/mL for VLT. Method greenness was evaluated using Eco-scale, GAPI, MoGAPI, CaFRI, and blueness assessment, while CACI was applied to assess overall analytical performance. Statistical comparison between the methods showed no significant differences.

PMID 42350572

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remogliflozin etabonate + vildagliptin (Remozen V / Remo V)

什么是 remogliflozin etabonate + vildagliptin？

药物档案

作用机制

分子靶点

治疗适应症

相关研究文献

Probable Vildagliptin-Associated Acute Pancreatitis in a Patient With Well-Controlled Type 2 Diabetes Mellitus: A Case Report.

Effect of Immunosuppressive Drugs on Glucose-Stimulated Insulin Secretion: Concentration-Response Studies in Dynamic Perifusion Assays.

Evaluating Lacrimal Punctum Size as a Clinical Indicator of Dry Eye Disease Severity in a Real-World Lebanese Cohort.

Comparison of the permeability of DPP-4 inhibitors-sitagliptin, vildagliptin, linagliptin, and alogliptin-in placental barrier cell models and exploration of their transport mechanisms by LC-MS/MS.

Structure-Based De Novo Design of Novel Dual DPP IV and PTP 1B Inhibitors (DDPI's).

Simple and cost-effective UV spectrophotometric platforms integrating advanced green and blue metrics for concurrent analysis of dapagliflozin and vildagliptin in diabetes therapy.

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