bersiporocin (DWN12088) / Daewoong Pharma, Biocon, CS Pharma - LARVOL DELTA

Baseline Clinical and Functional Spectrum of Idiopathic Pulmonary Fibrosis Patients in a Fully Enrolled Global Phase 2 Trial of the PRS Inhibitor Bersiporocin (ERS 2026) - P2 | "Participants were randomized 2:1 to receive bersiporocin 150 mg twice daily or placebo for 24 weeks and stratified by background antifibrotic use (pirfenidone or nintedanib vs no antifibrotics). In this fully enrolled Phase 2 trial of bersiporocin, mean baseline FVC was numerically higher in patients not receiving background antifibrotics. Similar trends have been noted in recent IPF trials by baseline antifibrotic use. These baseline data provide context for planned subgroup interpretation of efficacy and safety outcomes by treatment status."

Clinical • P2 data • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Daewoong Pharmaceutical participated in the 2026 European Respiratory Society (ERS 2026) held in Barcelona, Spain on Sep. 6 local time, and presented the analysis results of all registered patients in the global Phase 2 clinical trial of its self-developed new drug candidate Bersiporocin as a poster (Business Korea) - "According to the analysis data announced this time, among the total 104 patients who participated in the clinical trial, 55 (52.9%) were South Koreans and 49 (47.1%) were Americans. In particular, the number of patients already receiving existing anti-fibrotic agents reached 71 (68.3%), suggesting that it will be possible to confirm the efficacy of not only single administration but also combination therapy. The patients’ average forced vital capacity (FVC) was found to be at about 77% of the normal predicted value, and the diffusing capacity of the lung for carbon monoxide (DLCO) was at about 51%....Daewoong Pharmaceutical is accelerating the completion of the clinical trial and plans to announce the top-line results of the Phase 2 clinical trial in the first half of 2027."

P2 data • Idiopathic Pulmonary Fibrosis

Authors' Reply to "Methodological and Outcome Interpretation Concerns for the Food-Effect Study of Bersiporocin" [Response to Letter]. (PubMed, Drug Des Devel Ther) - No abstract available

Journal

Methodological and Outcome Interpretation Concerns for the Food-Effect Study of Bersiporocin [Letter]. (PubMed, Drug Des Devel Ther) - No abstract available

Journal

The Effect of Food on the Pharmacokinetics and Gastrointestinal Tolerability of Bersiporocin, a Novel Oral Prolyl-tRNA-Synthetase Inhibitor. (PubMed, Drug Des Devel Ther) - "A high-fat meal delayed the oral absorption rate of bersiporocin but did not have a clinically significant effect on systemic exposure to bersiporocin or M8. Given the increased incidence of GI AEs under early postprandial conditions, administration under fasted conditions or at least 2 hours postprandially may be appropriate for future clinical studies."

Clinical • First-in-human • Journal • PK/PD data • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Clinical Trial to Evaluate the Safety and Efficacy of DWN12088 in Patients With IPF (clinicaltrials.gov) - P2 | N=102 | Active, not recruiting | Sponsor: Daewoong Pharmaceutical Co. LTD. | Recruiting ➔ Active, not recruiting

Enrollment closed • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Dysregulated Proline Metabolism Exacerbates Hepatocellular Carcinoma Metastasis via EPRS1-Mediated mRNA Translation. (PubMed, Cancer Commun (Lond)) - "Finally, the inhibitory effect of bersiporocin on HCC metastasis was confirmed in patient-derived orthotopic xenograft models. Our findings not only revealed the critical role of l-proline-bound EPRS1 in promoting HCC metastasis but also indicated that inhibiting this binding could be a promising strategy to prevent metastasis."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor • EPRS1 • ITGB1 • PIK3CA

Daewoong Pharmaceutical announced on May 6 that it has completed patient enrollment for the global Phase 2 clinical trial (NCT05389215) of its idiopathic pulmonary fibrosis (IPF) treatment candidate, bersiporocin (DWN12088) (The Asia Business Daily) - "The clinical trial is currently underway in both Korea and the United States, evaluating the safety, tolerability, and efficacy of bersiporocin both as a monotherapy and in combination with existing antifibrotic drugs (nintedanib and pirfenidone)....Based on the results of the global Phase 2 trial, which are expected in the first quarter of 2027, Daewoong Pharmaceutical plans to focus on global partnerships and out-licensing opportunities."

Enrollment closed • P2 data • Idiopathic Pulmonary Fibrosis

Daewoong Pharmaceutical: Third IDMC Reaffirms Safety of Bersiporocin and Recommends Continuation of Global Phase 2 Clinical Trial (PRNewswire) - "The IDMC conducted an in-depth evaluation of interim safety data from 89 enrolled patients and found no significant safety concerns that would impact the trial's continuation. To date, Daewoong has enrolled 94 participants, representing approximately 92% of the target population (102 patients), and the study is progressing as planned....Interim baseline characteristics to be presented at the 2025 KATRD International Conference."

DSMB • P2 data • Trial status • Idiopathic Pulmonary Fibrosis

Clinical Trial to Evaluate the Safety and Efficacy of DWN12088 in Patients With IPF (clinicaltrials.gov) - P2 | N=102 | Recruiting | Sponsor: Daewoong Pharmaceutical Co. LTD. | Trial completion date: Dec 2025 ➔ Jan 2027 | Trial primary completion date: Sep 2025 ➔ Oct 2026

Trial completion date • Trial primary completion date • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Daewoong Pharmaceutical Presents Phase 2 Clinical Trial Poster on 'Bersiporocin' at ATS 2025, Highlights Global Patient Demographics (PRNewswire) - P2 | N=102 | NCT05389215 | Sponsor: Daewoong Pharmaceutical Co. LTD | "TThe interim analysis highlighted key baseline demographic and clinical characteristics of enrolled participants, including racial distribution and antifibrotic medication use. Approximately 70% of participants were receiving Bersiporocin in combination with approved antifibrotic therapies (nintedanib or pirfenidone), while the remaining 30% participated without any background treatment. Notably, more than half of the enrolled patients are Asian— enabling exploratory assessment of treatment responses across ethnic subgroups, in contrast to prior IPF studies which were predominantly limited to White populations....As of April 2025, 80 patients (approximately 80% of target enrollment) had completed registration."

P2 data • Trial status • Idiopathic Pulmonary Fibrosis

A Novel Prolyl-Transfer RNA Synthetase Inhibitor Bersiporocin Phase 2 Trial in Idiopathic Pulmonary Fibrosis: Study Design and Baseline Demographics (ATS 2025) - P2 | "Current therapies, such as pirfenidone and nintedanib, slow disease progression but have limitations, creating a high unmet need for safer and more effective options. The preliminary demographic analysis of the Phase 2 trial for Bersiporocin provides foundational data on the baseline characteristics of IPF patients, with a unique representation of approximately 50% Asian and predominantly White participants. This diversity offers an opportunity to explore treatment responses across different demographic profiles, contributing to a broader understanding of Bersiporocin's therapeutic potential. Further evaluations will assess the clinical implications of baseline characteristics, with potential insights for optimizing treatment strategies for IPF in diverse patient populations."

P2 data • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Prolyl-tRNA synthetase inhibitor as a novel first-in-class keloid treatment: Downregulation of de novo collagen synthesis and inflammatory cascade. (PubMed, Br J Dermatol) - "DWN12088, a selective PRS inhibitor, may be a novel first-in-class treatment modality that effectively prevents keloid development. Further clinical trials are required to verify the safety and clinical efficacy of PRS inhibitors for keloids. We believe that our study has applicability across several fibrotic wound problems such as hypertrophic scars."

Journal • Fibrosis • Immunology • Inflammation

EPRS1-mediated fibroblast activation and mitochondrial dysfunction promote kidney fibrosis. (PubMed, Exp Mol Med) - "Moreover, C57BL/6 EPRS1tm1b heterozygous knockout (Eprs1+/-) and pharmacological EPRS1 inhibition with the first-in-class EPRS1 inhibitor DWN12088 protected against kidney fibrosis and dysfunction by preventing fibroblast activation and proximal tubular injury...Our findings suggest that the EPRS1-mediated ECM accumulation induces kidney fibrosis via fibroblast activation and mitochondrial dysfunction. Therefore, targeting EPRS1 could be a potential therapeutic target for alleviating fibrotic injury in chronic kidney disease."

Journal • Chronic Kidney Disease • Fibrosis • Immunology • Metabolic Disorders • Nephrology • Renal Disease • EPRS1 • SMAD3

Daewoong’s phase 2 study into IPF drug moves forward with IDMC endorsement (Korea Biomedical Review) - "Daewoong Pharmaceutical said Berisiporocin...has passed a key safety milestone in phase 2 clinical trials, bringing it closer to commercialization....In this latest review, safety data from 59 enrolled patients, including 51 who completed the trial, revealed no significant safety concerns. The IDMC plans a final safety review at the third meeting scheduled for early next year. The phase 2 trial aims to be completed by 2025."

Trial completion date • Trial status • Idiopathic Pulmonary Fibrosis • Immunology

Clinical Trial to Evaluate the Safety and Efficacy of DWN12088 in Patients With IPF (clinicaltrials.gov) - P2 | N=102 | Recruiting | Sponsor: Daewoong Pharmaceutical Co. LTD. | Trial completion date: Aug 2024 ➔ Dec 2025 | Trial primary completion date: Jun 2024 ➔ Sep 2025

Trial completion date • Trial primary completion date • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Daewoong Pharmaceutical’s 413 billion won technology transfer ’Bersiporocin’ phase 2 clinical trial underway [Google translation] (News1 Korea) - "Daewoong Pharmaceutical is accelerating the development of 'bersiporocin' (project name DWN12088), a first-in-class new drug candidate for idiopathic pulmonary fibrosis. According to the Ministry of Food and Drug Safety...Daewoong Pharmaceutical is recruiting patients for phase 2 clinical trials of bersiporocin. Bersiporocin phase 2 clinical trials are underway in Korea and the United States."

Trial status • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease

Glutamyl-prolyl-tRNA synthetase (EPRS1) drives tubulointerstitial nephritis-induced fibrosis by enhancing T cell proliferation and activity. (PubMed, Kidney Int) - "The use of an EPRS1-targeting small molecule inhibitor (bersiporocin) under clinical trials to evaluate its therapeutic potential against idiopathic pulmonary fibrosis, alleviated immunofibrotic aggravation in TIN. EPRS1 expression was also observed in human kidney tissues and blood-derived T cells, and high expression was associated with worse patient outcomes. Thus, EPRS1 may emerge as a therapeutic target in toxin- and drug-induced TIN, modulating the proliferation and activity of infiltrated T cells."

Journal • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Nephrology • Pulmonary Disease • Respiratory Diseases • CD4 • CD8 • EPRS1 • IL17A • RAG1

Daewoong Pharmaceutical’s Bersiporocin Receives ’Orphan Drug Designation’ in Europe to Treat Idiopathic Pulmonary Fibrosis (PRNewswire) - "Daewoong Pharmaceutical's Bersiporocin (DWN12088) has been recognized as a significant advancement in treating idiopathic pulmonary fibrosis (IPF), a rare and debilitating disease. This first-in-class PRS inhibitor has recently received 'Orphan Drug Designation (ODD)' from the European Medicines Agency (EMA)...Bersiporocin has successfully completed phase 1 clinical trials in Korea and Australia...Multinational phase 2 clinical trials are currently in progress in Korea and the U.S."

European regulatory • Idiopathic Pulmonary Fibrosis

DWN12088, A Prolyl-tRNA Synthetase Inhibitor, Alleviates Hepatic Injury in Nonalcoholic Steatohepatitis. (PubMed, Diabetes Metab J) - "Our findings provide new insights about DWN12088, namely that it plays an important role in the overall improvement of NASH. Hence, DWN12088 shows great potential to be developed as a new integrated therapeutic agent for NASH."

Journal • Fibrosis • Genetic Disorders • Hepatology • Idiopathic Pulmonary Fibrosis • Immunology • Inflammation • Liver Failure • Non-alcoholic Fatty Liver Disease • Non-alcoholic Steatohepatitis • Obesity • Pulmonary Disease • Respiratory Diseases • AMPK • ATF4 • PERK • SMAD2 • STAT6 • TCF4 • TGFB1

No drug-drug interactions between selective prolyl-trna synthetase inhibitor, bersiporocin, and pirfenidone or nintedanib in healthy participants. (PubMed, Clin Transl Sci) - "There was no significant difference in the pharmacokinetic profiles after administration of bersiporocin alone or in combination therapy between CYP2D6 phenotypes. In conclusion, there is no significant DDI regarding the pharmacokinetics, safety, and tolerability of bersiporocin administration with pirfenidone or nintedanib."

Journal • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Daewoong Pharmaceutical’s idiopathic pulmonary fibrosis new drug ‘Versiporosin’ selected as one of KDDF’s top 10 excellent projects [Google translation] (Health Korea News) - "Clinical research on ‘versiporosin’ (DWN12088)...is being conducted by the Korea New Drug Development Foundation (KDDF). It was selected as one of the top 10 excellent tasks (hereinafter referred to as 'excellent tasks') of the 2023 National New Drug Development Project....'We plan to complete a phase 2 clinical study to evaluate safety and efficacy on a total of 102 idiopathic pulmonary fibrosis patients within 2025.'"

Trial completion date • Idiopathic Pulmonary Fibrosis • Immunology

“Daewoong Pharmaceutical increases sales of major products such as Nabota, Enblo, and Pexuclu” [Google translation] (Insight) - "Kyobo Securities reported...that Daewoong Pharmaceutical's third quarter performance will slightly fall below market expectations....'Phase 2 results for DWN12088, an IPF treatment candidate, are scheduled to be announced in 2024.'"

P2 data • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease

Daewoong Pharmaceutical Publishes Molecular Mechanism of Bersiporocin as an Antifibrotic in EMBO Molecular Medicine (PRNewswire) - "Daewoong Pharmaceutical...announced on the 25th that the molecular mechanism behind safety and efficacy of Bersiporocin as an antifibrotic for idiopathic pulmonary fibrosis was published in EMBO Molecular Medicine on the 21st. The title of the publication is 'Control of Fibrosis via Asymmetric Inhibition of Prolyl-tRNA Synthetase', and the study was in collaboration with research teams of Prof. Sunghoon Kim from Yonsei University and Prof. Kwang Yeon Hwang from Korea University."

Clinical • Idiopathic Pulmonary Fibrosis • Immunology • Respiratory Diseases

Daewoong Pharmaceutical signs 3 technology export deals totaling over ₩1 trillion (Korea Biomedical Review) - "Daewoong Pharmaceutical said it has already licensed out three drug candidates this year, totaling more than 1 trillion won ($749.6 million). The deals come as the government emphasizes fostering and exporting the pharmaceutical bio industry to overcome the global economic downturn and industry investment reduction since last year. Most recently, Daewoong signed a licensing deal to transfer the rights to the global development and commercialization of DWP213388, an oral autoimmune treatment drug candidate, to Vitalli Bio for $477 million, excluding royalties."

Sales • Idiopathic Pulmonary Fibrosis • Interstitial Lung Disease