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

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

Control of fibrosis with enhanced safety via asymmetric inhibition of prolyl-tRNA synthetase 1. (PubMed, EMBO Mol Med) - "The mutations disrupting PARS1 homodimerization restored the sensitivity to DWN12088, validating negative communication between PARS1 promoters for the DWN12088 binding. Thus, this work suggests that DWN12088, an asymmetric catalytic inhibitor of PARS1 as a novel therapeutic agent against fibrosis with enhanced safety."

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

Safety, tolerability, pharmacokinetic/pharmacodynamic characteristics of bersiporocin, a novel prolyl-tRNA synthetase inhibitor, in healthy subjects. (PubMed, Clin Transl Sci) - "The levels of pro-peptide of type 3 procollagen were lower after treatment with bersiporocin than after the placebo in the MAD study, whereas no significant change was observed in other idiopathic pulmonary fibrosis (IPF) biomarkers. In conclusion, the safety, PK, and PD profile of bersiporocin supported its further investigation in patients with IPF."

Clinical • Journal • PK/PD data • Fibrosis • Gastrointestinal Disorder • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Daewoong Pharmaceutical secures 50 billion won in R&D funds from the sale of treasury stocks… New drug development spur [Google translation] (Sisaweek) - "Daewoong Pharmaceutical secured 50 billion won in R&D funds by disposing of about 427,000 treasury stocks to parent company Daewoong Co., Ltd. on the 8th to invest in future growth such as new drug development. The funds secured this time are characterized by securing cash flow without interest burden....In addition, versiphorosin, a treatment for idiopathic pulmonary fibrosis, which is being developed as the world's first new drug (first-in-class), was designated as a fast track by the US Food and Drug Administration (FDA) last year. For fast-track designated new drugs, it is possible to have close consultations with the FDA during the approval process, such as consulting on clinical design at each stage of development and listening to advice on acquired data. In addition, after completing the phase 2 clinical trial, it is possible to apply for accelerated approval and priority review."

Fast track designation • Financing • Idiopathic Pulmonary Fibrosis • Interstitial Lung Disease

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. | Not yet recruiting ➔ Recruiting | Trial completion date: May 2024 ➔ Aug 2024

Enrollment open • Trial completion date • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Daewoong Pharmaceutical begins the first administration of the Bersiporocin, new treatment for idiopathic pulmonary fibrosis, as Phase II clinical trial (Pharma Focus Asia) - "'We are working hard to develop a new treatment for patients with idiopathic pulmonary fibrosis.' said the chair of the Trial steering committee, Toby Maher, MD, PhD...'The Phase II clinical trial of Daewoong Pharmaceutical's Bersiposocin represents an important step in developing treatments that address the shortcomings of existing anti fibrotic therapies.'"

Media quote • Idiopathic Pulmonary Fibrosis • Pulmonary Disease

Daewoong Pharmaceutical begins the first administration of the Bersiporocin, new treatment for idiopathic pulmonary fibrosis, as Phase II clinical trial (PRNewswire) - "Daewoong Pharmaceutical...announced that the first patient has been administrated in Phase II on the 6th. The Bersiporocin's multinational Phase II has been performed by approx. 30 institutions in Korea and US. A total of 102 patients are evaluated for the safety of Bersiporocin and the efficacy of changes in the improvement rate of FVC(forced vital capacity) after administering the Bersiporocin or placebo for 24 weeks. They are aiming to complete the administration to the subjects and check the results by 2024."

Trial status • Idiopathic Pulmonary Fibrosis • Interstitial Lung Disease

Daewoong Pharmaceutical, possibility of approval in China for ’Nabota’…Raising expectations for new products [Google translation] (eDaily) - "R&D costs in the fourth quarter are expected to increase by 45% year-on-year to KRW 37 billion, and costs have increased due to the phase 2 trial of DWN12088, a PRS inhibitor for idiopathic pulmonary fibrosis, and the phase 1 trial of DWP213388, an autoimmune disease treatment."

Commercial • Graft versus Host Disease • Idiopathic Pulmonary Fibrosis • Immunology • Interstitial Lung Disease

Daewoong Pharmaceutical announces the results of Phase 1 clinical trial in Australia for ’DWN12088’ [Google translation] (Medical News) - P1, N=72; "Daewoong Pharmaceutical released the clinical results of the world's first (first-in-class) idiopathic pulmonary fibrosis drug 'DWN12088' that inhibits PRS (Prolyl-tRNA Synthetase)...In this study, a single dose escalation test (SAD) and a multiple dose escalation test (MAD) were conducted in Australia in 72 healthy adults of various races to evaluate the safety of 'DWN12088' and its pharmacokinetic characteristics such as absorption, distribution, and metabolism in the body...Clinical Outcomes 'DWN12088' We have verified the safety, after drug administration has laid a basis for analyzing the capacity needed to establish therapeutic plasma levels."

P1 data • Idiopathic Pulmonary Fibrosis

Drug-drug interactions and safety assessment between selective Prolyl-tRNA Synthetase inhibitor, DWN12088, and “pirfenidone” or “nintedanib” in healthy subjects (ERS 2022) - "Overall, there are no clinically significant changes in safety, tolerability, and pharmacokinetic drug interaction when the concomitant use of DWN12088 and pirfenidone or nintedanib is administered. DWN12088 is anticipated to initiate phase II study for IPF in 3Q, 2022."

Clinical • Fibrosis • Gastroenterology • Gastrointestinal Disorder • Immunology

Daewoong Pharmaceutical enters phase 2 new drug for idiopathic pulmonary fibrosis in Korea after US (docdocdoc.co.kr) - "Daewoong Pharmaceutical received IND (clinical trial plan) approval for a phase 2 clinical trial for a new drug for idiopathic pulmonary fibrosis in Korea following the US....On the 6th, the Ministry of Food and Drug Safety (MFDS) approved the second phase of Daewoong Pharmaceutical's idiopathic pulmonary fibrosis treatment candidate 'DWN12088'."

New P2 trial • Idiopathic Pulmonary Fibrosis