RELEASE: Daewoong Pharmaceutical publishes the molecular mechanism of bersiporocin as an antifibrotic

-Daewoong Pharmaceutical publishes the molecular mechanism of bersiporocin as an antifibrotic in EMBO Molecular Medicine

SEOUL, South Korea, May 26, 2023 /PRNewswire/ -- Daewoong Pharmaceutical (CEO Lee Chang-jae and Jeon Sengho) announced on the 25th that the molecular mechanism underlying the safety and efficacy of bersiporocin as an antifibrotic for idiopathic pulmonary fibrosis was published on the 21st in EMBO Molecular Medicine. The title of the publication is "Control of fibrosis by asymmetric inhibition of Prolyl-tRNA synthetase", and the study was carried out in collaboration with the research teams of Professor Sunghoon Kim of Yonsei University and Professor Kwang Yeon Hwang of Korea University.

EMBO Molecular Medicine is a SCIE (Science Citation Index Expanded) publication. EMBO is a world-renowned magazine with an impact factor of 14,005 and a ranking in the top 5%. The magazine enjoys an international reputation for its quality and originality.

Bersiporocin inhibits the catalytic activity of PARS1 (Prolyl-tRNA Synthetase1 or PRS), which is involved in collagen synthesis. Studies have been carried out to inhibit the catalytic activity of PARS1 as an antifibrotic, but the challenge was to modulate the potency of the enzymatic inhibition of PARS1, since it is a critical enzyme for protein production. Daewoong has attempted to overcome the hurdle by inhibiting PARS1 just enough to provide therapeutic benefits without compromising safety. Through this publication, bersiporocin has been shown to bind asymmetrically to a pair of PARS1 enzymes avoiding excessive inhibition of catalytic activity, thus eliminating safety concerns while exerting its therapeutic benefits.

PARS1 exists as a homodimer, and the catalytic activity of PARS1 is directly involved in collagen synthesis and other profibrotic markers. Bersiporocin can strongly bind only one of the PARS1 homodimers, which can lead to inhibition of enzyme activity and consequent collagen production. As bersiporocin binds, the tertiary structure of the homodimer is altered, preventing bersiporocin from binding to the other side of the homodimer. This allows PARS1 to be able to maintain viable function while its enzymatic activity is reduced. Therefore, bersiporocin can provide an antifibrotic effect through the reduction of enzyme activity while still maintaining its critical role in homeostasis.

Professor Sunghoon Kim (Yonsei University College of Pharmacy and Medical School), author of the publication, commented that "investigating new targets and new mechanisms is crucial for precision medicine and global drug discovery. This landmark study an important milestone in the discovery of drugs that target essential enzymes like PARS1."

Joon Seok Park, Head of the Drug Discovery Center, commented, "This study will support the unique mode of action underlying bersiporocin as a first-class antifibrotic, and encourage ongoing Phase II clinical studies on IPF. We believe that the Bersiporocin will become the next therapeutic option for patients who continue to suffer from this devastating disease."

Bersiporocin has received Orphan Drug Designation from the FDA, as well as Fast Track Designation for IFP. Daewoong's Bersiporocin program has been selected as a national drug development project and has received financial support for the phase II clinical trial from the Korea Drug Development Fund (KDDF, CEO: Muk, Hyunsang). All these milestones represent the great potential of bersiporocin as the next innovative therapeutic agent for fibrosis.

About idiopathic pulmonary fibrosis

Idiopathic pulmonary fibrosis is a devastating rare disease characterized by progressive loss of lung function due to excessive deposition of collagen in the lung. The estimated prevalence of the disease is about 13 people per 100,000 worldwide. The 5-year survival rate for idiopathic pulmonary fibrosis is less than 40%, although current standard treatment continues to have limitations in terms of efficacy and safety. Therefore, there are huge unmet medical needs to develop and offer better therapeutic options to patients.

Acerca de Daewoong Pharmaceutical. Co., Ltd.

Founded in 1945, Daewoong Pharmaceutical Co., Ltd. is a leading South Korean pharmaceutical company that develops, manufactures, and markets pharmaceutical products for the domestic and international markets. With strong and innovative in-house R&D and advanced manufacturing facilities, Daewoong provides a comprehensive sanitary solution to customers around the world. Continuing with its goal of becoming a strong global healthcare company, Daewoong has expanded its international operations by opening branches and research centers in Asia and the United States. Daewoong has also expanded its strategic partnerships in more than 100 countries around the world. For more information about Daewoong Pharmaceutical, please visit our official website.

forward-looking statements

This press release contains forward-looking statements based on the current beliefs and expectations of Daewoong Pharmaceutical's management. These statements are subject to various risks, uncertainties and assumptions that could cause actual results to differ materially from those anticipated in such forward-looking statements. Factors that could cause or contribute to such differences include, but are not limited to: (1) Regulatory and Government Approvals: The approval process for pharmaceutical products is subject to extensive regulations and can involve uncertainties and delays. Failure to obtain the necessary approvals or delays in the approval process could adversely affect Daewoong Pharmaceutical's business and results. (2) Clinical trials: The success of Daewoong Pharmaceutical's products depends on the results of clinical trials. The results of early clinical trials may not be indicative of the results of later or larger-scale clinical trials.

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