vanoglipel (DA-1241) / Dong-A - LARVOL DELTA

LC-MS/MS Assay for Quantification of DA-1241, a Novel GPR119 Agonist, in Animal and Human Plasma: Application to Preclinical Pharmacokinetic Studies. (PubMed, J Mass Spectrom) - "The method met all the other validation criteria for matrix effect, recovery, and stability. The established method was successfully implemented on plasma protein binding assessments and preclinical pharmacokinetic studies of DA-1241 after a single oral administration in mice, rats, and dogs."

Journal • PK/PD data • Preclinical • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis

Anticipated Clinical Milestones (PRNewswire) - "DA-1726 in Obesity: Data from the 8-week 48 mg MAD cohort to explore the non-titrated maximum tolerated dose is expected by year-end 2025....Vanoglipel (DA-1241) in MASH: The Company is currently working to schedule an end-of-Phase 2 meeting with the FDA during the first half of 2026."

FDA event • P1 data • Metabolic Dysfunction-Associated Steatohepatitis • Obesity

MetaVia Announces Poster Presentation on Vanoglipel (DA-1241) at the AASLD Liver Meeting (PRNewswire)

P2a data • Metabolic Dysfunction-Associated Steatohepatitis

DA-1241, A GPR119 AGONIST, DEMONSTRATES HEPATOPROTECTIVE EFFECTS THROUGH IMPROVING INFLAMMATION AND METABOLISM IN THE LIVER: A 16-WEEK RANDOMIZED PLACEBO-CONTROLLED TRIAL IN PRESUMED METABOLIC DYSFUNCTION-ASSOCIATED STEATOHEPATITIS (MASH) PATIENTS (AASLD 2025) - P2 | "DA-1241 is the first oral GPR119 agonist to demonstrate both hepatoprotective and glucose-regulating effects in presumed MASH patients. These findings support its further development as a potential monotherapy or combination therapy for MASH and metabolic disorders."

Clinical • Fibrosis • Hepatology • Immunology • Inflammation • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • CCL2 • KRT18 • TIMP1

Additive Hepatoprotective Effects of DA-1241, a GPR119 Agonist, in Combination with Efruxifermin in a Diet-Induced Obese and Biopsy-Confirmed Mouse Model of MASH (ADA 2025) - "For the first time, we suggest a beneficial combination effect of DA-1241 and EFX in MASH treatment, highlighting the therapeutic potential of combining GPR119 agonists and FGF21 analogues, likely by further inhibiting steatosis, fibrosis, and inflammation."

Biopsy • Combination therapy • Late-breaking abstract • Preclinical • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Obesity • COL1A1 • CXCL10 • FGF21 • HHIP • TNFA

MetaVia Presents Pre-Clinical Data on DA-1241 Demonstrating Additive Hepatoprotective Effects in Combination With Efruxifermin at the ADA's 85th Scientific Session (PRNewswire) - "MetaVia Inc...announced the presentation of pre-clinical data on DA-1241, a novel G-Protein-Coupled Receptor 119 (GPR119) agonist, demonstrating additive hepatoprotective effects in combination with Efruxifermin, a fibroblast growth factor 21 (FGF21) analogue, in a metabolic dysfunction-associated steatohepatitis (MASH) mouse model....DA-1241 was found to be weight-neutral over the 12-week treatment period, while EFX monotherapy induced a statistically significant 17% reduction in body weight compared to vehicle (p < 0.05). No additional weight loss was observed with the combination therapy, indicating that further benefits induced by the combination were independent of weight loss. Both DA-1241 and EFX monotherapies led to improvements in liver function markers, including reductions in plasma transaminases and hepatic cholesterol levels."

Preclinical • Metabolic Dysfunction-Associated Steatohepatitis

MetaVia Announces Poster Presentation on DA-1241 at the ADA's 85th Scientific Sessions (PRNewswire) - "MetaVia Inc...today announced that an abstract highlighting pre-clinical data on DA-1241, a novel G-Protein-Coupled Receptor 119 (GPR119) agonist, has been accepted for a poster presentation at the American Diabetes Association's 85th Scientific Sessions, taking place June 20-23, 2025 at the McCormick Place Convention Center in Chicago, Illinois."

Preclinical • Metabolic Dysfunction-Associated Steatohepatitis • Obesity

DA-1241, a GPR119 agonist, ameliorates fatty liver through the upregulation of TFEB-mediated autophagy (ECO 2025) - "DA1241 treatment failed to produce favorable metabolic effects, including reduced hepatic triglyceride levels, in liver-specific TFEB knockout mice. Thus, DA1241 attenuates hepatic steatosis through TFEB-mediated autophagy induction."

Addiction (Opioid and Alcohol) • Diabetes • Dyslipidemia • Hepatology • Inflammation • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Type 2 Diabetes Mellitus • TFEB

DA-1241, a GPR119 agonist, demonstrates hepatoprotective and glucose-regulating effects in a 16-week randomized placebo-controlled trial in presumed metabolic dysfunction-associated steatohepatitis (MASH) patients (EASL 2025) - P1b, P2 | "DA-1241 is the first oral GPR119 agonist to demonstrate both hepatoprotective and glucose-regulating effects in presumed MASH patients. These findings support its further development as a potential monotherapy or combination therapy for MASH and metabolic disorders."

Clinical • Late-breaking abstract • Fibrosis • Hepatology • Immunology • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Type 2 Diabetes Mellitus • KRT18

MetaVia Announces Late-Breaking Poster Presentation on DA-1241 at the EASL Congress 2025 (PRNewswire) - "MetaVia Inc...today announced that an abstract highlighting data from its Phase 2a clinical trial of DA-1241...in patients with presumed metabolic dysfunction-associated steatohepatitis (MASH), has been accepted as a late-breaking poster presentation at the European Association for the Study of the Liver (EASL) Congress 2025, taking place May 7-10, 2025 in Amsterdam, the Netherlands."

Late-breaking abstract • P2a data • Metabolic Dysfunction-Associated Steatohepatitis

DA-1241, a GPR119 agonist, ameliorates fatty liver through the upregulation of TFEB-mediated autophagy. (PubMed, Diabetes) - "DA-1241 treatment failed to produce favorable metabolic effects, including reduced hepatic triglyceride levels, in liver-specific Tfeb knockout mice. Thus, DA-1241 attenuates hepatic steatosis through TFEB-mediated autophagy induction."

Journal • Addiction (Opioid and Alcohol) • Diabetes • Dyslipidemia • Hepatology • Inflammation • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Type 2 Diabetes Mellitus • TFEB

MetaVia Reports Year End 2024 Financial Results and Provides Corporate Update (PRNewswire) - "Anticipated Clinical Milestones: DA-1726 in Obesity: Top-line data from the additional cohorts in the MAD Part 2 is expected in April of 2025. The planned Phase 1 Part 3 will evaluate early proof of concept, with the first patient expected to be enrolled during the fourth quarter of 2025, followed by an interim data readout in or around mid-2026 and top-line results are expected in the second half of 2026. DA-1241 in MASH: The full data set from the two-part Phase 2a clinical trial of DA-1241 in MASH are expected to be presented at a major medical meeting in 2025. The Company expects to have an end-of-Phase 2 meeting with the FDA in the first half of 2025."

Enrollment status • FDA event • P1 data • P2a data • Metabolic Dysfunction-Associated Steatohepatitis • Obesity

Pharmaceutical companies continue to challenge themselves to develop 'high difficulty' MASH treatments [Google translation] (Daily Korea) - "Pharmaceutical companies are continuing their efforts to develop treatments for metabolic steatohepatitis (MASH, a chronic liver disease that causes fatty liver, inflammation, and liver fibrosis)...According to the pharmaceutical industry on the 10th, Dong-A ST's US subsidiary Metavia plans to announce the final results of the global phase 2 clinical trial for its MASH treatment drug 'DA-1241' in the second quarter."

P2 data • Metabolic Dysfunction-Associated Steatohepatitis

MetaVia to Participate in the 9th Annual MASH-TAG 2025 Conference After Releasing Positive Top-Line Results From Its Phase 2a Clinical Trial of DA-1241 in Patients with Presumed MASH (PRNewswire) - "MetaVia Inc...today announced that it will participate as a Sponsor and Exhibitor at the upcoming, 9th Annual MASH-TAG 2025 Conference. The company's participation follows the recent release of positive top-line 16-week results from the two-part Phase 2a clinical trial of DA-1241, a novel G-Protein-Coupled Receptor 119 (GPR119) agonist, in patients with presumed metabolic dysfunction-associated steatohepatitis (MASH). Members of MetaVia's management and clinical team will be available in the Exhibit Hall at the Conference to discuss the results of the Phase 2a clinical trial of DA-1241."

P2a data • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis

MetaVia Announces Positive Top-Line Results From Its Phase 2a Clinical Trial of DA-1241 in Patients with Presumed MASH (PRNewswire) - P2a | N=109 | NCT06054815 | Sponsor: NeuroBo Pharmaceuticals Inc. | "DA-1241 100mg showed statistically significant reductions in ALT levels at weeks 4 and 8...and a near statistically significant reduction (p=0.0506) at week 16 compared to placebo. DA-1241 50mg showed a statistically significant improvement in the normalization of ALT levels compared to placebo, with an odds ratio of 10.500 (p=0.0487). DA-1241 100mg and DA-1241 100mg + Sitagliptin 100mg showed significant improvements in the CAP score compared to placebo...DA-1241 100mg + Sitagliptin 100mg showed a statistically significant reduction in the FAST score compared to placebo (p=0.0416). DA-1241 100mg and DA-1241 100mg + Sitagliptin 100mg showed significant reductions in HbA1C from baseline at Week 16 compared to the placebo group...'We look forward to the full data set and expect to have an end of Phase 2 meeting with the U.S. Food and Drug Administration (FDA) in the first half of 2025.'"

P2a data • Metabolic Dysfunction-Associated Steatohepatitis

DA1241_NASH_IIa: Study to Evaluate the Efficacy and Safety of DA-1241 in Subjects With Presumed NASH (clinicaltrials.gov) - P2 | N=109 | Completed | Sponsor: NeuroBo Pharmaceuticals Inc. | Active, not recruiting ➔ Completed

Trial completion • Hepatology • Metabolic Dysfunction-Associated Steatohepatitis

NeuroBo Pharmaceuticals Announces Strategic Realignment Ahead of Important Clinical Milestones with Name Change to MetaVia - Reflecting the Company's Focus on Cardiometabolic Diseases (PRNewswire) - "NeuroBo Pharmaceuticals, Inc...today announced a strategic realignment, ahead of important clinical milestones, with a corporate name change to 'MetaVia Inc.,' which will be effective on November 29, 2024...In parallel, the Company's common stock will begin trading on the Nasdaq Stock Market under the new ticker symbol, 'MTVA,' which is expected to be operative as of the Effective Date. As part of its corporate name change, the company will also launch a new website, metaviatx.com, and a new company logo, on the Effective Date."

Commercial • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis

NeuroBo Pharmaceuticals Completes Last Patient Last Visit in Its Phase 2a Clinical Trial Evaluating DA-1241 for the Treatment of MASH (PRNewswire) - "...'Completion of patient dosing in the Phase 2a clinical trial of DA-1241, in patients with presumed MASH, marks an important milestone for this promising cardiometabolic asset, bringing us one step closer to the topline data readout from both Part 1 and Part 2 of the Phase 2a clinical trial expected in December of this year'....A total of 109 patients were randomized, while 95 patients completed the dosing. These patients were enrolled in either Part 1, which is exploring the efficacy of DA-1241 versus placebo, and randomized in a 1:2:1 ratio into 3 treatment groups: DA-1241 50 mg, DA-1241 100 mg or placebo, or into Part 2, which is exploring the efficacy of DA-1241 in combination with sitagliptin versus placebo, randomized in a 2:1 ratio into 2 treatment groups: DA-1241 100 mg/sitagliptin 100 mg or placebo."

P2a data • Trial status • Metabolic Dysfunction-Associated Steatohepatitis

Study to Evaluate the Efficacy and Safety of DA-1241 in Subjects With Presumed NASH (clinicaltrials.gov) - P2 | N=87 | Active, not recruiting | Sponsor: NeuroBo Pharmaceuticals Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Hepatology • Metabolic Dysfunction-Associated Steatohepatitis

NeuroBo Pharmaceuticals Reports Second Quarter 2024 Financial Results and Provides Corporate Update (PRNewswire) - "DA-1241 in MASH: Top-line results from the two-part Phase 2a clinical trial of DA-1241 in MASH are expected to be available in the fourth quarter of 2024."

P2a data • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis

Investigational new drug approval of DA-1241: what we know about GPR119 targeting for MASH therapy? (PubMed, Expert Opin Investig Drugs) - No abstract available

IND • Journal • Metabolic Dysfunction-Associated Steatohepatitis

Additive hepatoprotective effects of DA-1241, a novel GPR119 agonist, in combination with semaglutide in the GAN diet-induced obese and biopsy-confirmed mouse model of MASH (EASL-ILC 2024) - "GAN DIO-MASH mice received once daily treatment with vehicle, DA-1241 (100 mg/kg, PO) or semaglutide (30 nmol/kg, SC) alone or in combination for 8 weeks. DA-1241 and semaglutide demonstrate more than additive effects on metabolic, biochemical, and histological endpoints in GAN DIO-MASH mice, highlighting the therapeutic potential of dual targeting GPR119 and GLP1R function in MASH with liver fibrosis."

Biopsy • Combination therapy • Preclinical • Fibrosis • Hepatology • Immunology • Inflammation • Liver Cirrhosis • Metabolic Dysfunction-Associated Steatohepatitis • Obesity • COL1A1

DA-1241, a GPR119 agonist, combined with Semaglutide synergistically improved liver fibrosis in mice with CCl4-induced liver fibrosis (EASL-ILC 2024) - "After administering CCl 4 twice weekly for 3 weeks, mice with elevated plasma ALT levels were allocated to receive DA-1241 (oral) or semaglutide (subcutaneous) alone and in combination for 4 weeks. For the first time, we suggest a beneficial combination effect of DA-1241 and semaglutide in the treatment of liver fibrosis, which may be attributed to augmented inhibition of fibrogenesis and inflammation in the liver."

Preclinical • Fibrosis • Hepatology • Immunology • Inflammation • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • CCL2 • COL1A1 • COL3A1 • COL5A1 • COL6A1 • CXCL10 • HHIP • IL1B • TNFA

NeuroBo Pharmaceuticals Reports First Quarter 2024 Financial Results and Provides Corporate Update (PRNewswire) - "DA-1726 in Obesity: Top-line data from the single ascending dose (SAD) Part 1 is expected in the third quarter of 2024. Initiation of the multiple ascending dose (MAD) study Part 2 is expected in the third quarter of 2024 and the top-line data expected in the first quarter of 2025. DA-1241 in MASH: Full enrollment of the two-part Phase 2a clinical trial of DA-1241 in MASH is expected in the third quarter of 2024. Top-line results are expected to be available in the fourth quarter of 2024."

Enrollment status • P1 data • P2a data • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Obesity

Study to Evaluate the Efficacy and Safety of DA-1241 in Subjects With Presumed NASH (clinicaltrials.gov) - P2 | N=87 | Recruiting | Sponsor: NeuroBo Pharmaceuticals Inc.

Trial completion date • Trial primary completion date • Hepatology • Non-alcoholic Steatohepatitis