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Enavogliflozin (DWP-16001)

Cat No.:V74235 Purity: ≥98%
Enavogliflozin (DWP-16001), an antidiabetic active molecule, is an orally bioactive, first-in-class, selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.
Enavogliflozin (DWP-16001)
Enavogliflozin (DWP-16001) Chemical Structure CAS No.: 1415472-28-4
Product category: SGLT
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Enavogliflozin (DWP-16001), an antidiabetic active molecule, is an orally bioactive, first-in-class, selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.
Enavogliflozin (DWP-16001, CAS#: 1415472-28-4) is a first-in-class, orally active, and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor being developed as a best-in-class antidiabetic agent. By selectively inhibiting SGLT-2 in the proximal renal tubules, it reduces glucose reabsorption and promotes urinary glucose excretion, thereby lowering blood glucose levels in a insulin-independent manner. Enavogliflozin is currently under clinical investigation for the treatment of type 2 diabetes mellitus.
Biological Activity I Assay Protocols (From Reference)
Targets
SGLT2
SGLT-2 (sodium-glucose cotransporter-2). Enavogliflozin is a potent and selective inhibitor of SGLT-2, the primary transporter responsible for glucose reabsorption in the kidney. By selectively blocking SGLT-2, the compound reduces renal glucose reabsorption, leading to increased urinary glucose excretion and subsequent lowering of plasma glucose levels. This mechanism is insulin-independent, making it an attractive therapeutic approach for type 2 diabetes management.
ln Vitro
The antidiabetic medication enavogliflozin (DWP-16001) is an oral, potent, highly selective, and best-in-class sodium-glucose cotransporter-2 (SGLT-2) inhibitor[1][2][3].
Enavogliflozin demonstrates potent inhibitory activity against SGLT-2, as a first-in-class and best-in-class SGLT-2 inhibitor. While specific IC50 values are not detailed in the available literature, the compound's selectivity for SGLT-2 over SGLT-1 is a key feature of its pharmacological profile. By selectively targeting SGLT-2, it effectively reduces glucose reabsorption in the kidney without significantly affecting intestinal glucose absorption mediated by SGLT-1.
ln Vivo
In vivo, Enavogliflozin has demonstrated antidiabetic efficacy in preclinical models of type 2 diabetes. As an orally active compound, it is administered via the oral route, and its glucose-lowering effects are mediated through increased urinary glucose excretion. The compound is currently under clinical development for the treatment of type 2 diabetes mellitus, with clinical trials ongoing to evaluate its efficacy and safety.
Enzyme Assay
In vitro enzyme activity assays for Enavogliflozin typically involve measuring its ability to inhibit SGLT-2-mediated glucose uptake. These assays are performed using cells that express recombinant human SGLT-2, and the compound's inhibitory potency is determined by measuring the reduction in radiolabeled glucose or methyl-α-D-glucopyranoside uptake in the presence of increasing concentrations of the compound. Selectivity over SGLT-1 is confirmed using similar assays with SGLT-1-expressing cells.
Cell Assay
Cellular assays for Enavogliflozin involve the use of cell lines that express SGLT-2, such as human embryonic kidney (HEK) cells stably transfected with the human SGLT-2 gene. These cells are incubated with the compound in the presence of radiolabeled glucose or a fluorescent glucose analog, and the inhibition of glucose uptake is measured to determine the compound's potency and selectivity. This approach confirms the compound's ability to functionally inhibit SGLT-2-mediated glucose transport in a cellular context.
Animal Protocol
In vivo efficacy of Enavogliflozin has been evaluated in preclinical animal models of type 2 diabetes, such as db/db mice or streptozotocin-induced diabetic rats. The compound is administered orally, and blood glucose levels are monitored over time to assess its glucose-lowering effects. Urinary glucose excretion is also measured to confirm the mechanism of action. The compound has demonstrated antidiabetic efficacy in these models and is currently under clinical investigation.
ADME/Pharmacokinetics
Enavogliflozin has a molecular formula of C24H27ClO6 and a molecular weight of 446.92. It is orally active, indicating good oral bioavailability. The compound is supplied with a purity of ≥99%. As a small-molecule SGLT-2 inhibitor, its pharmacokinetic properties support once-daily oral dosing for the management of type 2 diabetes. The compound is currently in clinical development, and further pharmacokinetic data will be established from ongoing clinical trials.
Toxicity/Toxicokinetics
No specific toxicity data for Enavogliflozin is detailed in the available literature. As a SGLT-2 inhibitor, its safety profile would be expected to be similar to other members of this drug class, which are generally well-tolerated with common adverse effects including urinary tract infections, genital mycotic infections, and volume depletion-related events. Standard preclinical and clinical toxicology studies have been conducted as part of its clinical development program.
References

[1]. Daewoong speeds up developing antidiabetic Enavogliflozin.

[2]. These are the results of clinical trials of the diabetes drug Enavogliflozin and Metformin.

[3]. Global Diabetes Pipeline Landscape Report 2020 Featuring Daewoong's Enavogliflozin & Janssen Biotech's Golimumab Among Others - ResearchAndMarkets.com.

Additional Infomation
Enalapril is being studied in the clinical trial NCT06399835 (Effects of Enalapril vs. Pioglitazone on Glucose and Atherosclerosis). It is a novel sodium-glucose cotransporter 2 inhibitor; currently undergoing clinical development for the treatment of type 2 diabetes. See also: Canagliflozin (related drugs); Tolpagliflozin (related drugs).
Enavogliflozin (also known as DWP-16001) is a first-in-class, orally active, and selective SGLT-2 inhibitor being developed as a best-in-class antidiabetic agent. It has the molecular formula C24H27ClO6 and a molecular weight of 446.92. The compound is currently under clinical investigation for the treatment of type 2 diabetes mellitus, with clinical trial NCT06399835 evaluating Enavogliflozin versus Pioglitazone on glucose and atherosclerosis. It is a research compound not yet approved for clinical use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H27CLO6
Molecular Weight
446.92
Exact Mass
446.149
CAS #
1415472-28-4
PubChem CID
71076840
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
666.1±55.0 °C at 760 mmHg
Flash Point
356.7±31.5 °C
Vapour Pressure
0.0±2.1 mmHg at 25°C
Index of Refraction
1.666
LogP
4.9
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
5
Heavy Atom Count
31
Complexity
609
Defined Atom Stereocenter Count
5
SMILES
C1CC1C2=CC=C(C=C2)CC3=CC(=C4CCOC4=C3Cl)[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O
InChi Key
KORCWPOBTZTAFI-YVTYUBGGSA-N
InChi Code
InChI=1S/C24H27ClO6/c25-19-15(9-12-1-3-13(4-2-12)14-5-6-14)10-17(16-7-8-30-23(16)19)24-22(29)21(28)20(27)18(11-26)31-24/h1-4,10,14,18,20-22,24,26-29H,5-9,11H2/t18-,20-,21+,22-,24+/m1/s1
Chemical Name
(2S,3R,4R,5S,6R)-2-[7-chloro-6-[(4-cyclopropylphenyl)methyl]-2,3-dihydro-1-benzofuran-4-yl]-6-(hydroxymethyl)oxane-3,4,5-triol
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (223.75 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2375 mL 11.1877 mL 22.3754 mL
5 mM 0.4475 mL 2.2375 mL 4.4751 mL
10 mM 0.2238 mL 1.1188 mL 2.2375 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
Title:Enavogliflozin vs. Pioglitazone on Glucose and Atherosclerosis
Status:Recruiting
updateDate:2026-05-05
Ctid:NCT06399835

Link: https://clinicaltrials.gov/ct2/show/NCT06399835

Conditions:Type 2 Diabetes
Interventions:Pioglitazone
Phase:Phase 4
Title:Drug-Drug Interaction Study to Evaluate the Effect of DWC202511 or DWC202512 With DWP16001 in Healthy Adults
Status:Completed
updateDate:2026-02-11
Ctid:NCT07213310

Link: https://clinicaltrials.gov/ct2/show/NCT07213310

Conditions:Healthy
Interventions:DWC202512
Phase:Phase 1
Title:Enavogliflozin Outcome Trial in Functional Tricuspid Regurgitation
Status:Active, not recruiting
updateDate:2025-12-29
Ctid:NCT06027307

Link: https://clinicaltrials.gov/ct2/show/NCT06027307

Conditions:Tricuspid Regurgitation|Heart Failure With Preserved Ejection Fraction
Interventions:Placebo
Phase:Phase 3
View More

Title:ENAVOgliflozin Outcome Trial in Patients With Severe Aortic Stenosis After Transcatheter Aortic Valve Replacement
Status:Recruiting
updateDate:2025-12-15
Ctid:NCT05672836

Link: https://clinicaltrials.gov/ct2/show/NCT05672836

Conditions:Aortic Valve Stenosis|Heart Failure
Interventions:Standard-of-Care
Phase:Phase 4
Title:Enavogliflozin for the Management of Patients With Amyloid CardiomyopaThy
Status:Not yet recruiting
updateDate:2025-11-21
Ctid:NCT07240844

Link: https://clinicaltrials.gov/ct2/show/NCT07240844

Conditions:Amyloid Cardiomyopathy
Interventions:Placebo
Phase:Phase 4
Title:To Evaluate the Efficacy and Safety of Envlo Tablet or Envlomet SR Tablet in Patients With Type II Diabetes Mellitus
Status:Active, not recruiting
updateDate:2025-09-02
Ctid:NCT05926414

Link: https://clinicaltrials.gov/ct2/show/NCT05926414

Conditions:Diabetes Mellitus, Type 2
Interventions:Enavogliflozin
Phase:
Title:Registry Study to Determine the Effectiveness and Safety of Weight Loss With Enavogliflozin in Patients With Type 2 Diabetes Mellitus
Status:Active, not recruiting
updateDate:2025-09-02
Ctid:NCT06427083

Link: https://clinicaltrials.gov/ct2/show/NCT06427083

Conditions:Type 2 Diabetes Mellitus
Interventions:Envolomet SR Tablet
Phase:
Title:Effects of Enavogliflozin on Coronary Microvascular and Cardiac Function in Obesity
Status:Recruiting
updateDate:2025-09-02
Ctid:NCT06782139

Link: https://clinicaltrials.gov/ct2/show/NCT06782139

Conditions:Obesity and Type 2 Diabetes
Interventions:Placebo
Phase:Phase 4
Title:Evaluation of Enavogliflozin's Efficacy and Safety in Type II Diabetes With Hypertension or Dyslipidemia
Status:Recruiting
updateDate:2025-01-23
Ctid:NCT06647888

Link: https://clinicaltrials.gov/ct2/show/NCT06647888

Conditions:Diabetes Mellitus, Type 2
Interventions:Envlomet SR Tablet
Phase:
Title:ENavogliflozin DElivering Alleviation of Ventricular Diastolic Dysfunction in nonObstRuctive Hypertrophic CardioMyopathy
Status:Recruiting
updateDate:2024-11-08
Ctid:NCT06580717

Link: https://clinicaltrials.gov/ct2/show/NCT06580717

Conditions:Nonobstructive Hypertrophic Cardiomyopathy
Interventions:enavogliflozin Placebo
Phase:Phase 4
Title:Phase 1 Study of Drug-Drug Interactions Between DWP16001, DWC202407, and DWC202408 in Healthy Adults
Status:Not yet recruiting
updateDate:2024-10-16
Ctid:NCT06644404

Link: https://clinicaltrials.gov/ct2/show/NCT06644404

Conditions:Healthy
Interventions:DWC202408 2mg
Phase:Phase 1
Title:A Prospective Trial of Enavogliflozin to Evaluate Cardio-renal Outcome in Type 2 Diabetes Mellitus Patients
Status:Recruiting
updateDate:2024-10-15
Ctid:NCT06642623

Link: https://clinicaltrials.gov/ct2/show/NCT06642623

Conditions:Diabetes Mellitus, Type 2|Cardiovascular Diseases|Kidney Diseases
Interventions:Dapagliflozin or Empagliflozin
Phase:Phase 4
Title:Evaluate the Efficacy and Safety of DWP16001 in Type 2 Diabetic Nephropathy with Moderate Renal Impairment Patients
Status:Not yet recruiting
updateDate:2024-09-20
Ctid:NCT06606093

Link: https://clinicaltrials.gov/ct2/show/NCT06606093

Conditions:Type 2 Diabetic Nephropathy
Interventions:DWP16001 0.3mg
Phase:Phase 3
Title:Effect of Enavogliflozin on Recurrence of Atrial Fibrillation After Catheter Ablation
Status:Not yet recruiting
updateDate:2024-07-30
Ctid:NCT06528262

Link: https://clinicaltrials.gov/ct2/show/NCT06528262

Conditions:Atrial Fibrillation
Interventions:Placebo
Phase:Phase 4
Title:A Study to Investigate the Effect of DWP16001 as add-on Therapy to Drug A in Patients With Type 2 Diabetes Mellitus
Status:Unknown status
updateDate:2024-04-08
Ctid:NCT05466643

Link: https://clinicaltrials.gov/ct2/show/NCT05466643

Conditions:Type 2 Diabetes Mellitus
Interventions:DWP16001 Placebo
Phase:Phase 3
Title:To Compare the Safety and PK/PD Characteristics of Subjects With Between Hepatic Impairment and Normal Hepatic Function
Status:Unknown status
updateDate:2024-04-08
Ctid:NCT05747664

Link: https://clinicaltrials.gov/ct2/show/NCT05747664

Conditions:Diabetes Mellitus, Type 2
Interventions:DWP16001
Phase:Phase 1
Title:The Efficacy and Safety of DWP16001 in Combination With Metformin in T2DM Patients Inadequately Controlled on Metformin
Status:Unknown status
updateDate:2024-04-04
Ctid:NCT05505994

Link: https://clinicaltrials.gov/ct2/show/NCT05505994

Conditions:Diabetes Mellitus|Diabetes Mellitus, Type 2|Glucose Metabolism Disorders|Metabolic Disease|Endocrine System Diseases
Interventions:Dapagliflozin Placebo
Phase:Phase 3
Title:Study to Evaluate the Long Term Safety and Efficacy of DWP16001 in Patients With Type 2 Diabetes Mellitus
Status:Unknown status
updateDate:2023-11-21
Ctid:NCT06141980

Link: https://clinicaltrials.gov/ct2/show/NCT06141980

Conditions:T2DM (Type 2 Diabetes Mellitus)
Interventions:DWP16001 0.3 mg
Phase:Phase 3
Title:To Evaluate the Effect of Food on the Safety and PK Characteristics of DWP16001 in Healthy Adult Volunteers
Status:Unknown status
updateDate:2023-04-04
Ctid:NCT05797922

Link: https://clinicaltrials.gov/ct2/show/NCT05797922

Conditions:Healthy
Interventions:DWP16001
Phase:Phase 1
Title:To Compare the Pharmacokinetic Characteristics of the Fixed-dose Combination Compared to the Loose Combination
Status:Unknown status
updateDate:2023-02-21
Ctid:NCT05737771

Link: https://clinicaltrials.gov/ct2/show/NCT05737771

Conditions:FDC|Diabetes Mellitus, Type 2
Interventions:DWP16001
Phase:Phase 1
Title:The Efficacy and Safety of DWP16001 Compared to Placebo in the Treatment of Type 2 Diabetes Mellitus.
Status:Completed
updateDate:2022-10-25
Ctid:NCT04632862

Link: https://clinicaltrials.gov/ct2/show/NCT04632862

Conditions:T2DM (Type 2 Diabetes Mellitus)
Interventions:DWP16001
Phase:Phase 3
Title:Evaluate the Long Term Safety and Efficacy of DWP16001 add-on to Metformin in Patients With T2DM Inadequately Controlled on Metformin
Status:Completed
updateDate:2022-10-25
Ctid:NCT05376969

Link: https://clinicaltrials.gov/ct2/show/NCT05376969

Conditions:T2DM (Type 2 Diabetes Mellitus)
Interventions:DWP16001
Phase:Phase 3
Title:Drug-Drug Interaction of DWP16001 in Combination With DWC202204 and DWC202205 in Healthy Male Adults
Status:Unknown status
updateDate:2022-08-15
Ctid:NCT05500898

Link: https://clinicaltrials.gov/ct2/show/NCT05500898

Conditions:Healthy
Interventions:DWP16001+DWC202204+DWC202205
Phase:Phase 1
Title:A Crossover Study of DWJ1525 to Evaluate the Safety and Pharmacokinetic Properties in Healthy Volunteers
Status:Completed
updateDate:2022-07-11
Ctid:NCT05192395

Link: https://clinicaltrials.gov/ct2/show/NCT05192395

Conditions:Healthy
Interventions:DWC202101
Phase:Phase 1
Title:The Drug Interaction of DWP16001 and DWC202010 After Oral Administration in Healthy Adults
Status:Unknown status
updateDate:2022-04-11
Ctid:NCT05321732

Link: https://clinicaltrials.gov/ct2/show/NCT05321732

Conditions:Healthy Volunteers
Interventions:DWP202010
Phase:Phase 1
Title:Study to Evaluate the Safety and PK Properties of DWP16001 in Healthy Subjects With Various Ethnicities
Status:Unknown status
updateDate:2022-01-26
Ctid:NCT05207176

Link: https://clinicaltrials.gov/ct2/show/NCT05207176

Conditions:Healthy
Interventions:DWP16001
Phase:Phase 1
Title:Study to Evaluate Drug-Drug Interaction of DWP16001 in Combination With DWC202001 and DWC202002 in Healthy Male Adults
Status:Unknown status
updateDate:2020-04-27
Ctid:NCT04343547

Link: https://clinicaltrials.gov/ct2/show/NCT04343547

Conditions:Healthy
Interventions:DWP16001+DWC202001+DWC202002
Phase:Phase 1
Title:Study to Evaluate Drug-Drug Interaction of DWP16001 in Combination With Metformin in Healthy Male Adults (Phase 1 Study)
Status:Completed
updateDate:2020-01-13
Ctid:NCT04064073

Link: https://clinicaltrials.gov/ct2/show/NCT04064073

Conditions:Healthy
Interventions:DWP16001+Metformin IR
Phase:Phase 1
Title:Type 2 Diabetes Patients With Renal Impairment
Status:Unknown status
updateDate:2020-01-09
Ctid:NCT04221399

Link: https://clinicaltrials.gov/ct2/show/NCT04221399

Conditions:Type2 Diabetes
Interventions:DWP16001
Phase:Phase 1
Title:Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of DWP16001 After Oral Administration in Healthy Male Volunteers
Status:Completed
updateDate:2019-08-21
Ctid:NCT03364985

Link: https://clinicaltrials.gov/ct2/show/NCT03364985

Conditions:Healthy
Interventions:Dapagliflozin
Phase:Phase 1
Title:Study to Evaluate the Efficacy and Safety of DWP16001 in Patients With Type 2 Diabetes Mellitus
Status:Unknown status
updateDate:2019-07-18
Ctid:NCT04014023

Link: https://clinicaltrials.gov/ct2/show/NCT04014023

Conditions:T2DM (Type 2 Diabetes Mellitus)
Interventions:Placebo
Phase:Phase 2

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