Sugarnon (evogliptin) / Dong-A - LARVOL DELTA

Evogliptin prevents ceramide-induced pyroptosis during calcification via modulation of NLRP3/GSDM-D mediated pathway in Vascular Smooth Muscle Cells. (PubMed, PLoS One) - "Furthermore, MCC950 (NLRP3 inhibitor), disulfiram (GSDM-D inhibitor) and evogliptin significantly downregulated osteogenic and pyroptotic markers including LDH release in both Pi-induced only and CER + Pi-treated VSMCs. Also, the cleavage efficiency of GSDM-D was high in Pi and CER + Pi groups which was reduced with prior treatment of evogliptin. Hence, our data demonstrate that evogliptin alleviates VC by blocking phenotypic transition and associated pyroptosis via modulation of NLRP3/GSDM-D mediated pathway in CER-induced VSMCs."

Journal • Cardiovascular • Inflammation • BMP2 • IL18 • IL1B • NLRP3 • RUNX2

Novel Drug Molecules for Atherosclerosis from Ginkgo biloba, an Endangered Himalayan Herb, Via Pharmacoinformatics Approaches. (PubMed, Curr Pharm Biotechnol) - "The findings highlight the multi-target therapeutic potential of Isoginkgetin in mitigating the initiation and progression of atherosclerosis."

Journal • Atherosclerosis • Cardiovascular • Inflammation • Metabolic Disorders • CYP19A1 • PACERR • PTGS2

Combined Treatment with Evogliptin and Temozolomide Alters miRNA Expression but Shows Limited Additive Effect on Glioma. (PubMed, Int J Mol Sci) - "The co-administration of evogliptin and temozolomide resulted in distinct miRNA profile changes. Nevertheless, both in vitro and in vivo, the added cytotoxicity from the combination was minimal."

Journal • Brain Cancer • Glioma • Oncology • Solid Tumor • DPP4

Comparative efficacy and safety of Evogliptin in type 2 diabetes patients above and below 65 years. (PubMed, Diabetes Obes Metab) - No abstract available

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Enhanced Efficacy and Safety of Evogliptin in Older Adults—A Comparative Study in Type 2 Diabetes Patients Aged above and below 65 Years (ADA 2025) - "Evogliptin effectively improves glycemic control, especially HbA1c levels, with minimal adverse effects in elderly T2DM patients following extended treatment. These findings underscore the importance of personalized diabetes management strategies, tailored to patient age and treatment duration, to maximize therapeutic benefits."

Clinical • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Effect of Bone Metabolism and the Efficacy of Evogliptin and Dapagliflozin for Blood Sugar in the Menopause Female Patients with Type 2 Diabetes—A Multicenter Randomized Exploratory Clinical Trial (ADA 2025) - "In postmenopausal patients with T2DM, Evogliptin demonstrated a more favorable safety profile regarding BMD compared to Dapagliflozin. Dapagliflozin resulted in small but significant reductions in BMD or T-score at non-vertebral bone, due at least in part to weight loss. These findings provide evidence for selecting appropriate antidiabetic medications in postmenopausal women with osteoporosis."

Clinical • Diabetes • Metabolic Disorders • Osteoporosis • Type 2 Diabetes Mellitus

A Study to Evaluate the Efficacy and Safety of DA-1229 (Evogliptin) in Patient's Calcific Aortic Valve Disease With Mild to Moderate Aortic Stenosis (EVOID-AS) (clinicaltrials.gov) - P2/3 | N=580 | Recruiting | Sponsor: REDNVIA Co., Ltd. | N=867 ➔ 580 | Active, not recruiting ➔ Recruiting

Enrollment change • Enrollment open • Cardiovascular

Determination of absolute bioavailability, absorption, metabolism, and excretion of evogliptin in healthy male subjects using a microtracer method. (PubMed, J Pharm Sci) - "The concomitant oral dosing followed by microtracer IV dosing and the microtracer oral dosing enabled a comprehensive description of evogliptin's absorption, metabolism, and excretion in humans. Evogliptin was safe and well tolerated in healthy subjects."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

A Study to Evaluate the Efficacy and Safety of DA-1229 (Evogliptin) in Patient's Calcific Aortic Valve Disease with Mild to Moderate Aortic Stenosis (EVOID-AS) (clinicaltrials.gov) - P2/3 | N=867 | Active, not recruiting | Sponsor: REDNVIA Co., Ltd. | Recruiting ➔ Active, not recruiting

Enrollment closed • IGF1

Population pharmacokinetic and pharmacodynamic model of evogliptin: Severe uremia increases the bioavailability of evogliptin. (PubMed, CPT Pharmacometrics Syst Pharmacol) - "The developed PK/PD model accurately predicted exposure and the resulting DPP-4 activity of evogliptin in renal impairment. The findings of this study suggest that renal impairment and associated biochemical changes may impact the bioavailability of CYP3A4-metabolized drugs."

Journal • PK/PD data • Chronic Kidney Disease • Nephrology • Renal Disease • CYP3A4

Effect of Evogliptin on the Progression of Aortic Valvular Calcification. (PubMed, J Am Coll Cardiol) - P2 | "This exploratory study did not demonstrate the protective effect of evogliptin on AV calcification. Favorable 18F-NaF PET results and possible suppression of aortic valve calcification with longer medication use in the evogliptin groups suggest the need for larger confirmatory trials. (A Multicenter, Double-blind, Placebo-controlled, Stratified-randomized, Parallel, Therapeutic Exploratory Clinical Study to Evaluate the Efficacy and Safety of DA-1229 in Patients With Calcific Aortic Valve Disease; NCT04055883)."

Clinical • Journal

Analytical quality by design-based stability-indicating high performance liquid chromatography method for the estimation of evogliptin tartrate in bulk and tablet dosage form. (PubMed, Biomed Chromatogr) - "The drug was sensitive to acidic, basic, oxidative, thermal, and photodegradation resolving six degradation products. Thus, the developed AQbD-based stability-indicating HPLC method is applicable in analyzing evogliptin in bulk, tablet dosage form and stability samples."

Journal

Efficacy and safety of dapagliflozin add-on to evogliptin plus metformin therapy in patients with type 2 diabetes: A randomized, double-blind, placebo-controlled study. (PubMed, Diabetes Obes Metab) - "Dapagliflozin add-on to evogliptin plus metformin improved glycaemic control and was well tolerated by the target patients."

Clinical • Journal • Diabetes • Metabolic Disorders • Renal Disease • Type 2 Diabetes Mellitus

Cardiovascular safety of evogliptin dual and triple therapy in patients with type 2 diabetes: a nationwide cohort study. (PubMed, BMJ Open) - "These findings suggest that dual or triple therapies of evogliptin for the management of type 2 diabetes in routine clinical practice present no cardiovascular harms, but could alternatively offer cardiovascular benefits in this patient population."

Journal • Cardiovascular • Congestive Heart Failure • Diabetes • Heart Failure • Metabolic Disorders • Myocardial Infarction • Type 2 Diabetes Mellitus

Evaluation of the Ejection Pressure for Tracking Internal Cracks during Compaction in Bilayer Tablet Formulations Using Experimental and Finite Element Methods. (PubMed, Pharmaceuticals (Basel)) - "This study aimed to evaluate the ejection pressure and the correlation of the findings with the occurrence of internal cracks within bilayer tablets (BLTs) consisting of metformin HCl (MF) and evogliptin tartrate (EG). These findings indicate that the mechanisms of internal cracking and delamination were successfully confirmed by FEM simulation. Moreover, measuring ejection pressure before BLT manufacturing can prevent invisible tablet cracks without damaging the tablets."

Journal • CNS Disorders

GLYCEMIC EFFECTS OF DIPEPTYL‐PEPTIDASE INHIBITOR ADDITION TO TYPE 1 DIABETES TREATMENT IN PERSONS SUBMITTED TO BARIATRIC SURGERY USING SENSOR‐AUGMENTED INSULIN PUMP OR HYBRID CLOSED‐LOOP SYSTEM (ATTD 2024) - "To improve the glucose variability possible associated to the gastric bypass it was initiated DPP4i (evogliptin)... The increase in prevalence of obesity in T1D puts bariatric surgery as an alternative,although data is scarce. Unfortunately weight loss do not seems to impact glycemic control in T1DM. The change in glucose kinetics related to RYGB with faster delivery of glucose to the jejunum causing marked hyperglycemic post-meal with subsequent rapid decreases in glycaemia may impose extra challenge to a HCLS."

Bariatric surgery • Surgery • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 1 Diabetes Mellitus • Type 2 Diabetes Mellitus

Efficacy and Safety of Evogliptin Add-on Therapy to Dapagliflozin/Metformin Combinations in Patients with Poorly Controlled Type 2 Diabetes Mellitus: A 24-Week Multicenter Randomized Placebo-Controlled Parallel-Design Phase-3 Trial with a 28-Week Extension. (PubMed, Diabetes Metab J) - P3 | "Long-term triple combination with evogliptin added to DAPA/MET showed superior HbA1c reduction and glycemic control compared to placebo at 52 weeks and was well tolerated."

Journal • P3 data • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

The Effect of Compression Pressure on the First Layer Surface Roughness and Delamination of Metformin and Evogliptin Bilayer and Trilayer Tablets. (PubMed, Pharmaceuticals (Basel)) - "Accordingly, the decrease in the roughness of the first layer reduced the inter-penetration at the interface, as observed via energy dispersive spectrometer (EDS)-equipped scanning electron microscopy, decreasing the interfacial bonding strength and causing delamination of the MF/EG multi-layer tablets. These findings indicate the significance of roughness control in the actual preparation of multi-layer tablets and the usefulness of profilometer- and EDS-based surface analyses for interpreting the delamination of multi-layer tablets."

Journal

The Effect of Evogliptin Tartrate on Controlling Inflammatory Pain. (PubMed, Biomedicines) - " Evogliptin tartrate mirrored the anti-inflammatory pain relief of indomethacin. We aim to broaden its use as an anti-inflammatory drug or pain relief drug."

Journal • Inflammation • Pain • IL1B • TNFA

Effect of evogliptin and temozolomide combination therapy for the treatment of glioblastoma, in vitro and in vivo (SNO 2023) - "The combination of evogliptin and TMZ had a moderate effect on the treatment of GBM in vitro and in vivo. miR-4440 and miR-6780b-5p could be associated with inhibiting the proliferation of GBM cells by targeting DPP4."

Combination therapy • Preclinical • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Oncology • Solid Tumor • DPP4 • MIR1246 • MIR126 • MIR149 • MIR23A • MIR433 • MIR671

Thalidomide and a Dipeptidyl Peptidase 4 Inhibitor in a Rat Model of Experimental Autoimmune Myocarditis. (PubMed, Korean Circ J) - "Although thalidomide and the DPP4 inhibitor had an immunomodulatory effect and are used against inflammatory diseases, they did not ameliorate myocardial inflammation and fibrosis in this rat model of EAM."

Journal • Preclinical • Cardiovascular • Fibrosis • Immunology • Inflammation • CD4

Stability-Indicating Densitometric Analysis of Evogliptin Tartrate in Bulk and Tablet Dosage Form. (PubMed, J AOAC Int) - "The proposed method has a promising application commercially for identification, routine quantitative determination, and monitoring of stability of the evogliptin tartrate in bulk and tablet dosage forms to guarantee its safety, efficacy, and quality. Moreover, the developed method will also help in formulation development and in determining the appropriate storage conditions."

Journal • Diabetes • Metabolic Disorders

Effect of Dipeptidyl-4 Inhibitors in Reducing Stroke Severity, From HIRA Database (clinicaltrials.gov) - P=N/A | N=22119 | Not yet recruiting | Sponsor: Ajou University School of Medicine | Initiation date: Apr 2023 ➔ Aug 2023

Trial initiation date • Cardiovascular • CNS Disorders

Efficacy and Safety of Dapagliflozin Add-on Therapy to Evogliptin plus Metformin Combinations in Inadequately Controlled Patients with Type 2 Diabetes—A 24-Week, Randomized, Double-blind, Placebo-Controlled, Parallel-Design, Phase 3 Trial (ADA 2023) - "Triple combination with dapagliflozin add-on to evogliptin plus metformin improved glycemic control and is well tolerated in patients with type 2 diabetes who are not adequately controlled with evogliptin and metformin combination."

Clinical • P3 data • Diabetes • Hypoglycemia • Metabolic Disorders • Type 2 Diabetes Mellitus

Pharmacokinetic and Pharmacodynamic Drug-Drug Interactions between Evogliptin and Empagliflozin or Dapagliflozin in Healthy Male Volunteers. (PubMed, Clin Transl Sci) - "Administration of EV+EP or EV+DP had no significant effects on the PK profiles of each drug. All treatments were well-tolerated."

Journal • PK/PD data • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus