A Randomized, Double-blind, Placebo-controlled, Multicenter, Phase 2 Study to Evaluate the Efficacy and Safety of HY209 Gel in Patients With Mild to Moderate Atopic Dermatitis(AD)

This is a randomized, double-blind, placebo-controlled, multi-center, phase 2 study in patients with mild to moderate Atopic Dermatitis(AD), which consists of 2 parts.

Start Date01 Mar 2024

Sponsor / Collaborator

Shaperon, Inc.

NCT06533878

/ Enrolling by invitationPhase 1

(Part A) A Non-randomized, Open, Single-dose Escalation to Evaluate Tolerability and Safety of Single Oral Dose of HY209; (Part B) A Block-randomized, Double-blinded, Placebo-controlled, Multiple-dose Escalation to Evaluate Tolerability and Safety of Multiple Oral Doses of HY209 Phase 1 Clinical Trial in Healthy Volunteers

* Primary study objectives in Parts A and B To determine the Maximum Tolerable Dose(MTD) of the study drug (repeated or single dose).
* Endpoint: • Adverse event(AEs), including objective and subjective symptoms, after the IP dosing as well as physical examinations, vital signs, ECGs, and laboratory tests findings related to the IP dosing
• Dose-limiting toxicities (DLTs)
* Justification for endpoints: The safety will be assessed comprehensively by performing safety assessment and evaluating relevant variables by dose group.
The tolerability will be assessed in DLT analysis set. In a first-in-human clinical trial, tolerability of the drug administered is usually assessed through determination of dose-limiting toxicity (DLT). An accurate dose proportionality of toxicity was not observed, but toxicity was found at high doses, not at low doses following IV and oral administrations, except transdermal treatment. Thus, a relationship between toxicity and doses was confirmed.
In addition, HY209 showed a dose dependence in some efficacy endpoints, including dose-dependent inhibition of release of Tumor Necrosis Factor(TNF)-α and Il-1β, key inflammation factors related to inflammatory bowel disease. Thus, evaluating the occurrence of DLTs through sequential dose escalation is determined appropriate to assess the tolerability and safety of HY209.
* Primary study objectives in Part A (Dose levels 4-6): To evaluate the effects of food on HY209 bioavailability (absorption rate and volume) following a single oral dose in healthy volunteers.
* Endpoint: PK of HY209 at a fasting condition and after a high-fat meal Point estimates for the geometric mean ratio of variables (Area under concentration-time curve;AUC₀-₆, AUCₗₐₛₜ, AUC₀-∞, and Cmax) and the 90% confidence interval(CI) and Tmax .
* Justification for endpoints: For oral drugs, effects of food on bioavailability of the drugs are usually evaluated. Especially, a systemic exposure to bile acid drugs of enterohepatic circulation can be explained with a spillover from the liver to systemic circulatory system. Thus, a systemic exposure is thought to be affected by food, but the actual effects of food are triggered by combination of factors that affect in vivo elution of a drug and absorption of the active pharmaceutical ingredient(API) of the drug. As estimating the extent of effects on bioavailability is difficult without conducting an actual food effect study, there is a need for clinical evaluation.

Start Date13 Sep 2023

Sponsor / Collaborator

Kukjeon Pharm Co., Ltd.

EUCTR2022-001152-42-BG

/ Not yet recruitingPhase 2/3

A Randomized, Double-blinded, Placebo-controlled, Parallel-treatment Group, Adaptive Design, Multi-center, Phase 2b/3 Trial to Evaluate Efficacy and Safety of NuSepin® Intravenous Infusion in COVID-19 Pneumonia Patients

Start Date05 Sep 2022

Sponsor / Collaborator

Shaperon, Inc.

100 Clinical Results associated with Taurodeoxycholic acid

100 Translational Medicine associated with Taurodeoxycholic acid

100 Patents (Medical) associated with Taurodeoxycholic acid

3,658

Literatures (Medical) associated with Taurodeoxycholic acid

31 Dec 2025·Gut Microbes

The microbiota-derived bile acid taurodeoxycholic acid improves hepatic cholesterol levels in mice with cancer cachexia

Article

Author: Thibaut, Morgane M. ; Thissen, Jean-Paul ; Muccioli, Giulio G. ; Bonetto, Andrea ; Bindels, Laure B. ; Piron, Edwige ; Rodriguez, Julie ; Roumain, Martin ; Neyrinck, Audrey M. ; Loriot, Axelle ; Gillard, Justine ; Delzenne, Nathalie M. ; Massart, Isabelle ; Pin, Fabrizio ; Huot, Joshua R.

Alterations in bile acid profile and pathways contribute to hepatic inflammation in cancer cachexia, a syndrome worsening the prognosis of cancer patients. As the gut microbiota impinges on host metabolism through bile acids, the current study aimed to explore the functional contribution of gut microbial dysbiosis to bile acid dysmetabolism and associated disorders in cancer cachexia. Using three mouse models of cancer cachexia (the C26, MC38 and HCT116 models), we evidenced a reduction in the hepatic levels of several secondary bile acids, mainly taurodeoxycholic (TDCA). This reduction in hepatic TDCA occurred before the appearance of cachexia. Longitudinal analysis of the gut microbiota pinpointed an ASV, identified as Xylanibacter rodentium, as a bacterium potentially involved in the reduced production of TDCA. Coherently, stable isotope-based experiments highlighted a robust decrease in the microbial 7α-dehydroxylation (7α-DH) activity with no changes in the bile salt hydrolase (BSH) activity in cachectic mice. This approach also highlighted a reduced microbial 7α-hydroxysteroid dehydrogenase (7α-HSDH) and 12α-hydroxysteroid dehydrogenase (12α-HSDH) activities in these mice. The contribution of the lower production of TDCA to cancer cachexia was explored in vitro and in vivo. In vitro, TDCA prevented myotube atrophy, whereas in vivo hepatic whole transcriptome analysis revealed that TDCA administration to cachectic mice improved the unfolded protein response and cholesterol homeostasis pathways. Coherently, TDCA administration reversed hepatic cholesterol accumulation in these mice. Altogether, this work highlights the contribution of the gut microbiota to bile acid dysmetabolism and the therapeutic interest of the secondary bile acid TDCA for hepatic cholesterol homeostasis in the context of cancer cachexia. Such discovery may prove instrumental in the understanding of other metabolic diseases characterized by microbial dysbiosis. More broadly, our work demonstrates the interest and relevance of microbial activity measurements using stable isotopes, an approach currently underused in the microbiome field.

01 Apr 2025·Environmental Research

Maternal per- and polyfluoroalkyl substances exposure, cord blood lipidomics and infant anthropometry: A mediation analysis

Article

Author: Yang, Lan ; Miao, Maohua ; Xie, Zhenzhen ; Ji, Honglei ; Yuan, Wei ; Li, Likang ; Liu, Xiaofang ; Wang, Yan ; Liang, Hong ; Xi, Jianya

Maternal exposure to per- and polyfluoroalkyl substances (PFAS) has been associated with offspring adiposity; however, underlying mechanisms remain unclear. In this study, we quantified 11 PFAS in maternal plasma collected between 12 and 16 gestational weeks and 104 lipid metabolites in the cord blood of 525 mother-infant pairs. Principal components of multiple PFAS compounds, extracted by principal component analysis, were employed to investigate the effect of the PFAS mixture. Infant anthropometric indicators included weight, length, waist/arm circumference, and abdominal/triceps/subscapular skinfold thickness at birth and 6 and 12 months old. Multiple linear regression showed that maternal PFAS exposure was primarily associated with increased glycerophospholipids and decreased fatty acyls and bile acids in cord blood. Four glycerophospholipids (16:0 PI, 16:0-18:1 PI, 18:0-20:4 PI, and 18:0-18:1 PS), fatty acyls (5(S)-HETE, 15(S)-HETE, 13-HDoHE, and dhkPGF2), and bile acids (GCA, TCA, TCDA, and TDCA) partially mediated the positive associations of the first principle component of PFAS compounds (with positive loadings for all PFAS compounds), PFNA, and PFUdA with infant skinfold thickness with mediating proportions ranging from 15.24% to 33.39%. Our findings provide novel insights into mechanisms underlying the effects of maternal PFAS exposure on infant growth.

01 Mar 2025·Aquaculture

Metabolic responses of small yellow croaker (Larimichthys polyactis) liver to hypoxic stress: Insights into glucose and lipid metabolism

Author: Wang, Li ; Zhu, Junquan ; Liu, Feng ; Liu, Yang ; Wang, Jingqian ; Chen, Yiner ; Lou, Bao

Hypoxia neg. affect metabolism, growth and development of fish.To explore the effects of hypoxic stress on energy metabolism in Larimichthys polyactis, we performed untargeted metabolomic anal., biochem. assays, and real-time fluorescence quant. PCR (RT-qPCR) to explore the dynamic changes in hepatic glucose and lipid metabolism under sustained 96 h hypoxic stress.The findings showed that after 6 h of hypoxia, starch and sucrose metabolism was significantly enriched, with potentially enhanced glycolysis and gluconeogenesis.After 96 h of hypoxia, steroid biosynthesis and unsaturated fatty acid biosynthesis were significantly enriched, with the potential for a significant increase in lipid decompositionAddnl., in the first 24 h of hypoxia, the serum glucose, pyruvate, and lactate contents increased, whereas the activities of the aerobic respiratory enzymes pyruvate dehydrogenase (PDH) and succinate dehydrogenase (SDH) in the liver decreased.The activities of the anaerobic glycolytic enzymes, hexokinase (HK), phosphofructokinase (PFK), pyruvate kinase (PK), lactate dehydrogenase (LDH), as well as the glucose metabolism-related genes, glut1, hk2, pfkp, ldha, and mct4 mRNA levels in the liver increased.After 24 h of hypoxia, liver aerobic respiratory enzyme activity increased, whereas anaerobic glycolytic enzyme activity and gene expression levels decreased.At the same time, serum triglyceride (TG) levels decreased while free fatty acid (FFA) levels increased.Lipase (LPS) activity and lipid degradation-related genes hsl and mgl mRNA levels in the liver also increased.Conversely, acetyl-CoA carboxylase (ACC) activity and fatty acid synthesis-related genes acc1 and fasn mRNA levels decreased.Fatty acid oxidation enzyme-related gene cpt-1 mRNA level also decreased.These results indicate that during the early phase of hypoxia (in the first 24 h), aerobic respiration was inhibited, anaerobic glycolysis became the primary energy source.As the duration of hypoxia increased (after 24 h), anaerobic glycolysis decreased, lipid metabolism became an important energy pathway.Our study revealed the effects of different durations of hypoxic stress on glucose and lipid metabolism in the liver of L. polyactis, helping to elucidate metabolic adaptation mechanisms in fish under hypoxic conditions and providing theor. guidance for screening and breeding new varieties of hypoxia-tolerant fish.

News (Medical) associated with Taurodeoxycholic acid

18 Mar 2024

·www.biospace.com

Shaperon Enrolls Its First Patient in Phase 2 U.S. Clinical Trial for Atopic Dermatitis Therapy 'Nugel'

210 Patients With Multi-Racial Atopic Dermatitis...Phase 2 Clinical Trial Begins CAMBRIDGE, Mass. & SEOUL, South Korea--(BUSINESS WIRE)-- Shaperon, Inc. (Kosdaq: 378800), a biotechnology company developing innovative immune drugs, announced the enrollment of the first patient in the Phase 2 clinical trial for Nugel, its therapy for Atopic Dermatitis. This milestone marks the start of a crucial phase in Shaperon’s effort to advance treatment for patients globally. With FDA approval secured for the Global Phase 2 Clinical Trials (IND) of Nugel in September 2023, Shaperon is dedicated to evaluating its efficacy in improving the Eczema Area Severity Index (EASI) across a diverse cohort of 210 patients with mild to moderate atopic dermatitis. Employing a rigorous double-blind, placebo-controlled methodology, the trial is anticipated to conclude by the first half of 2026. Market research forecasts indicate a robust growth of over 8.7%, projecting the global atopic dermatitis market to reach $19.1 billion by 2030. Presently, patients rely on steroids and FDA-approved medications, yet there remains a pressing need for novel drugs due to their adverse effects and limited efficacy. Of particular note, more than 70% of patients exhibit positive responses to the biomarker discovered during Shaperon's phase 2 clinical trials in Korea, categorized as "A type A atopic patients." This treatment, distinguished by its superior safety and efficacy compared to existing JAK inhibitors or PDE4 inhibitors in the market, has garnered attention at U.S. and European forums. Shaperon has already initiated patent applications for this biomarker, enabling tailored treatments for patients showing exceptional responses to Nugel. Nugel represents a paradigm shift in atopic dermatitis therapy as the world's first inflammation control drug targeting 'GPCR19' action. Its unique mechanism of action, exclusive to immune-related cells, offers minimal side effects while effectively addressing inflammatory pathways. Beyond atopic dermatitis, Nugel holds promise for treating a spectrum of skin conditions, further underscoring its potential impact on global healthcare. Dr. Seung-Yong Seong, CEO of Shaperon, reaffirms Shaperon's commitment to advancing Nugel's global presence and facilitating technology transfer through the Phase 2 clinical trials. Leveraging innovative approaches such as a smartwatch-based AI medication management system demonstrates Shaperon's dedication to optimizing patient outcomes and data reliability. The establishment of Hudson Therapeutics, Shaperon's U.S.-based subsidiary, reinforces its strategic vision for global expansion and technology exports. ABOUT SHAPERON Shaperon is a clinical stage biotech company developing novel inflammasome inhibitors. Its unique mechanism of action of GPCR19-P2X7 modulation suppresses a broad spectrum of inflammatory cytokines including IL-1β, IL-18, IL-6, and TNF-α by controlling both priming and activation phase of inflammasome, whereas conventional approaches are designed to suppress only the activation phase. With this unique and novel modality which is best suited to address complex immune-mediated inflammatory disorders, Shaperon is currently developing multiple clinical programs in atopic dermatitis, cytokine release syndrome, Alzheimer’s disease, Obesity and MASH. ABOUT Hudson Therapeutics Hudson Therapeutics, a US subsidiary of Shaperon, was founded in 2023 to lead global clinical trials and business development of assets from Shaperon. Hudson’s pipeline includes immunology clinical assets in Atopic Dermatitis, Covid-19, Alzheimer’s Disease and preclinical programs focused in Obesity and other indications, combined with their nanobody platform. View source version on businesswire.com: Contacts Ellie Jung (ellie@hudsontherapeutics.com) Source: Shaperon View this news release online at:

Phase 2

19 Apr 2022

·www.prnewswire.com

Bridge Biotherapeutics Enters into an Exclusive License Agreement with Shaperon to Strengthen Its IPF Franchise

Bridge Biotherapeutics (KQ288330), a South Korean clinical-stage biotechnology company focused on developing novel drugs for fibrosis, inflammation, and cancer, today announced that the company has signed an exclusive in-license agreement with Shaperon, a South Korean clinical-stage biotech company, for its GPCR19 (G protein-coupled receptor 19) agonist, coded "BBT-209", in order to develop a novel therapy for the treatment of idiopathic pulmonary fibrosis (IPF). Shaperon, the originator, has identified that BBT-209, a first-in-class GPCR19 agonist, controls GPCR19-P2X7 expressions and downregulates component proteins of NLRP3 so that inflammation signaling networks can be significantly suppressed by the compound's mode of action. Through IPF animal models, Bridge Biotherapeutics has confirmed that the drug candidate shows treatment efficacy through its robust anti-inflammatory activities. The company will utilize this data when developing monotherapy and/or combination therapy strategies. By entering into the license agreement, Bridge will make an upfront payment of approximately USD 1.63 million (KRW 2 billion). The potential deal value equates to approximately USD 24.4 million (KRW 30 billion) including upfront, milestone, and royalty payments. "We are highly excited to in-license BBT-209, which is known to be the first-in-class GPCR19 agonist for the treatment of idiopathic pulmonary fibrosis," said James Lee, CEO of Bridge Biotherapeutics. "By jointly working with Shaperon, our development team will make the best effort to ensure the rapid advancement for our novel drug candidate, along with the other pipeline assets under the company's IPF franchise," James added. "We hope that BBT-209 will become a breakthrough therapy for patients with IPF, who are currently lacking treatment options" and "We will accelerate the development of innovative treatments, to help improve the quality of life for patients suffering from rare diseases, such as IPF, through our partnership with Bridge Biotherapeutics, which has a proven track record in both global drug development and business development," said Seung-Yong Seong, M.D., Ph.D., and Myung-Sea Lee M.D., M.B.A., co-CEOs of Shaperon. Bridge Biotherapeutics reinforces its strategic focus on disease areas with significant unmet medical needs and lacks novel approved therapies, including cancers and various fibrotic diseases. Relating to idiopathic pulmonary fibrosis, the company has been accelerating the development of BBT-877 (an autotaxin inhibitor), BBT-301 (an ion channel modulator), and BBT-209 (a GPCR19 agonist).

Idiopathic Pulmonary FibrosisLicense out/inCollaborateBreakthrough TherapyFirst in Class

100 Deals associated with Taurodeoxycholic acid

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
COVID-19	Phase 3	South Korea	Shaperon, Inc.	12 Apr 2022
Mild Atopic Dermatitis	Phase 2	United States	Shaperon, Inc.	01 Mar 2024
Moderate Atopic Dermatitis	Phase 2	United States	Shaperon, Inc.	01 Mar 2024
Dermatitis, Atopic	Phase 2	South Korea	Shaperon, Inc.	26 Aug 2020
Sepsis	Phase 2	United States	Shaperon, Inc.	05 Dec 2019
Dementia	Phase 1	South Korea	Kukjeon Pharm Co., Ltd.	13 Sep 2023
Alzheimer Disease	Phase 1	South Korea	Shaperon, Inc.	-
Idiopathic Pulmonary Fibrosis	Preclinical	South Korea	Shaperon, Inc.	01 Feb 2025
Idiopathic Pulmonary Fibrosis	Preclinical	United States	BridgeBio Pharma, Inc.	01 Feb 2025

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03492398 (Shaperon, CTgov)	Phase 1	Dermatitis, Atopic	56	HY209 (Cohort A HY209 0.05% Gel)	pxuxyaqdme(cfcyralwld) = jsnmifssuu jpleringod (xtnueladul, ykkbxmkvxs - rgfrhojguj) View more	-	19 Oct 2020
				HY209 (Cohort A HY209 0.1% Gel)	pxuxyaqdme(cfcyralwld) = ojjaslmsay jpleringod (xtnueladul, smscixfpzd - xjwpbtcidy) View more

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