A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis

BackgroundCurrent guidelines to treat atopic dermatitis (AD) overlook disease heterogeneity, limiting personalized care. This study assessed NuGel, a topical GPCR19 agonist, for efficacy, safety, and predictive baseline biomarkers in AD patients.MethodsIn a multicenter, double-blind, randomized, pla...

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Main Authors: Gyeong Ho Baek, Bo Ri Kim, Jung-Won Shin, Chang Hun Huh, Jungjoong Hwang, Sungmin Ko, Siwon Kim, Pil-Su Ho, Kyu-Han Kim, Chun Wook Park, Seong Jun Seo, Chang-Ook Park, Dongyoon Shin, Yeongshin Kim, Youngsoo Kim, Seung-Yong Seong, Jung-Im Na
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Published: Frontiers Media S.A. 2025-05-01
Series:Frontiers in Immunology
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Online Access:https://www.frontiersin.org/articles/10.3389/fimmu.2025.1560447/full
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author Gyeong Ho Baek
Bo Ri Kim
Bo Ri Kim
Jung-Won Shin
Chang Hun Huh
Jungjoong Hwang
Sungmin Ko
Siwon Kim
Pil-Su Ho
Kyu-Han Kim
Chun Wook Park
Seong Jun Seo
Chang-Ook Park
Dongyoon Shin
Yeongshin Kim
Yeongshin Kim
Youngsoo Kim
Youngsoo Kim
Seung-Yong Seong
Seung-Yong Seong
Seung-Yong Seong
Seung-Yong Seong
Jung-Im Na
Jung-Im Na
author_facet Gyeong Ho Baek
Bo Ri Kim
Bo Ri Kim
Jung-Won Shin
Chang Hun Huh
Jungjoong Hwang
Sungmin Ko
Siwon Kim
Pil-Su Ho
Kyu-Han Kim
Chun Wook Park
Seong Jun Seo
Chang-Ook Park
Dongyoon Shin
Yeongshin Kim
Yeongshin Kim
Youngsoo Kim
Youngsoo Kim
Seung-Yong Seong
Seung-Yong Seong
Seung-Yong Seong
Seung-Yong Seong
Jung-Im Na
Jung-Im Na
author_sort Gyeong Ho Baek
collection DOAJ
description BackgroundCurrent guidelines to treat atopic dermatitis (AD) overlook disease heterogeneity, limiting personalized care. This study assessed NuGel, a topical GPCR19 agonist, for efficacy, safety, and predictive baseline biomarkers in AD patients.MethodsIn a multicenter, double-blind, randomized, placebo-controlled Phase 2a trial (August 2020–September 2021, five hospitals, 80 participants), patients received placebo, 0.3% NuGel, or 0.5% NuGel twice daily for four weeks.ResultsNuGel (0.3% [Nu0.3] and 0.5% [Nu0.5]) was well-tolerated, with no adverse drug reactions or serious adverse events. Nu0.3 showed a significant decrease in EASI score from baseline (-12.2%, [-30.3%, 5.9%], p = 0.04). Treatment with Nu0.5 resulted in a numerically decreased EASI score (-11.9%, [-34.9%, 11.1%], p > 0.05), which is comparable with placebo group (-2.9%, [-21.5%, 15.6%], p > 0.05). No significant difference was observed between groups (p>0.05). Plasma proteomic analysis identified biomarkers associated with blood coagulation, complement activation, and cell adhesion as predictors of response to Nu0.5. Patients with baseline profiles characterized by K2C5high, ENTP6low, or CRKlow demonstrated significant clinical improvement when treated with Nu0.5 compared to the placebo group. Among these, the CRKlow subgroup, comprising 54.3% of the biomarker analysis set, showed a ΔEASI of -61.3% [-99.9, -22.8; p = 0.003] and a ΔIGA of -35.2% [-58.2, -12.1; p = 0.004] compared to the placebo group. The biomarker signature demonstrated high predictive accuracy (AUC = 0.92, p = 0.002). Logistic regression analysis revealed that the threshold of predicted probability derived from the baseline plasma level of K2C5 and ENTP6 successfully stratified 100% of participants who responded to Nu0.5 (ΔEASI from baseline ≤ -50%), whereas none (0%) in the placebo group responded (p = 0.035).ConclusionBaseline biomarkers, such as K2C5, ENTP6, and CRK, may serve as predictors of clinical improvement in AD patients treated with Nu0.5, highlighting the potential for personalized treatment strategies. Further research is required to validate these findings in larger patient cohorts.Clinical trial registrationhttps://clinicaltrials.gov/, identifier NCT04530643.
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spelling doaj-art-e2fe8978db3f4eb4974b84ec0f876d4e2025-08-20T02:25:17ZengFrontiers Media S.A.Frontiers in Immunology1664-32242025-05-011610.3389/fimmu.2025.15604471560447A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysisGyeong Ho Baek0Bo Ri Kim1Bo Ri Kim2Jung-Won Shin3Chang Hun Huh4Jungjoong Hwang5Sungmin Ko6Siwon Kim7Pil-Su Ho8Kyu-Han Kim9Chun Wook Park10Seong Jun Seo11Chang-Ook Park12Dongyoon Shin13Yeongshin Kim14Yeongshin Kim15Youngsoo Kim16Youngsoo Kim17Seung-Yong Seong18Seung-Yong Seong19Seung-Yong Seong20Seung-Yong Seong21Jung-Im Na22Jung-Im Na23Department of Dermatology, Seoul National University Bundang Hospital, Seongnam, Republic of KoreaDepartment of Dermatology, Seoul National University Bundang Hospital, Seongnam, Republic of KoreaDepartment of Dermatology, Seoul National University College of Medicine, Seoul, Republic of KoreaDepartment of Dermatology, Seoul National University Bundang Hospital, Seongnam, Republic of KoreaDepartment of Dermatology, Seoul National University Bundang Hospital, Seongnam, Republic of KoreaAimce Center, Shaperon Inc., Gangnam-gu, Seoul, Republic of KoreaAimce Center, Shaperon Inc., Gangnam-gu, Seoul, Republic of KoreaAimce Center, Shaperon Inc., Gangnam-gu, Seoul, Republic of KoreaAimce Center, Shaperon Inc., Gangnam-gu, Seoul, Republic of KoreaDepartment of Dermatology, Veterans Health Service Medical Center, Seoul, Republic of KoreaDepartment of Dermatology, Kangnam Sacred Heart Hospital, Hallym University, Seoul, Republic of KoreaDepartment of Dermatology, Chung-Ang University College of Medicine, Seoul, Republic of KoreaDepartment of Dermatology, Severance Hospital, Yonsei University College of Medicine, Seoul, Republic of KoreaProteomics Research Team, CHA Institute of Future Medicine, Seongnam, Republic of KoreaProteomics Research Team, CHA Institute of Future Medicine, Seongnam, Republic of KoreaDepartment of Medical Science, School of Medicine, CHA University, Seongnam, Republic of KoreaProteomics Research Team, CHA Institute of Future Medicine, Seongnam, Republic of KoreaDepartment of Medical Science, School of Medicine, CHA University, Seongnam, Republic of KoreaAimce Center, Shaperon Inc., Gangnam-gu, Seoul, Republic of Korea0Wide River Institute of Immunology, Seoul National University College of Medicine, Hongcheon, Gangwon, Republic of Korea1Department of Microbiology and Immunology, Seoul National University College of Medicine, Seoul, Republic of Korea2Department of Biomedical Sciences, Seoul National University College of Medicine, Seoul, Republic of KoreaDepartment of Dermatology, Seoul National University Bundang Hospital, Seongnam, Republic of KoreaDepartment of Dermatology, Seoul National University College of Medicine, Seoul, Republic of KoreaBackgroundCurrent guidelines to treat atopic dermatitis (AD) overlook disease heterogeneity, limiting personalized care. This study assessed NuGel, a topical GPCR19 agonist, for efficacy, safety, and predictive baseline biomarkers in AD patients.MethodsIn a multicenter, double-blind, randomized, placebo-controlled Phase 2a trial (August 2020–September 2021, five hospitals, 80 participants), patients received placebo, 0.3% NuGel, or 0.5% NuGel twice daily for four weeks.ResultsNuGel (0.3% [Nu0.3] and 0.5% [Nu0.5]) was well-tolerated, with no adverse drug reactions or serious adverse events. Nu0.3 showed a significant decrease in EASI score from baseline (-12.2%, [-30.3%, 5.9%], p = 0.04). Treatment with Nu0.5 resulted in a numerically decreased EASI score (-11.9%, [-34.9%, 11.1%], p > 0.05), which is comparable with placebo group (-2.9%, [-21.5%, 15.6%], p > 0.05). No significant difference was observed between groups (p>0.05). Plasma proteomic analysis identified biomarkers associated with blood coagulation, complement activation, and cell adhesion as predictors of response to Nu0.5. Patients with baseline profiles characterized by K2C5high, ENTP6low, or CRKlow demonstrated significant clinical improvement when treated with Nu0.5 compared to the placebo group. Among these, the CRKlow subgroup, comprising 54.3% of the biomarker analysis set, showed a ΔEASI of -61.3% [-99.9, -22.8; p = 0.003] and a ΔIGA of -35.2% [-58.2, -12.1; p = 0.004] compared to the placebo group. The biomarker signature demonstrated high predictive accuracy (AUC = 0.92, p = 0.002). Logistic regression analysis revealed that the threshold of predicted probability derived from the baseline plasma level of K2C5 and ENTP6 successfully stratified 100% of participants who responded to Nu0.5 (ΔEASI from baseline ≤ -50%), whereas none (0%) in the placebo group responded (p = 0.035).ConclusionBaseline biomarkers, such as K2C5, ENTP6, and CRK, may serve as predictors of clinical improvement in AD patients treated with Nu0.5, highlighting the potential for personalized treatment strategies. Further research is required to validate these findings in larger patient cohorts.Clinical trial registrationhttps://clinicaltrials.gov/, identifier NCT04530643.https://www.frontiersin.org/articles/10.3389/fimmu.2025.1560447/fullatopic dermatitisGPCR19inflammasomeprecision medicinetaurodeoxycholic acidclinical trial
spellingShingle Gyeong Ho Baek
Bo Ri Kim
Bo Ri Kim
Jung-Won Shin
Chang Hun Huh
Jungjoong Hwang
Sungmin Ko
Siwon Kim
Pil-Su Ho
Kyu-Han Kim
Chun Wook Park
Seong Jun Seo
Chang-Ook Park
Dongyoon Shin
Yeongshin Kim
Yeongshin Kim
Youngsoo Kim
Youngsoo Kim
Seung-Yong Seong
Seung-Yong Seong
Seung-Yong Seong
Seung-Yong Seong
Jung-Im Na
Jung-Im Na
A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis
Frontiers in Immunology
atopic dermatitis
GPCR19
inflammasome
precision medicine
taurodeoxycholic acid
clinical trial
title A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis
title_full A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis
title_fullStr A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis
title_full_unstemmed A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis
title_short A phase 2a double-blind, placebo-controlled, randomized clinical trial evaluating the efficacy and safety of NuGel, a novel topical GPCR19-mediated inflammasome inhibitor, in patients with mild to moderate atopic dermatitis: a proof-of-concept study with Post-hoc biomarker analysis
title_sort phase 2a double blind placebo controlled randomized clinical trial evaluating the efficacy and safety of nugel a novel topical gpcr19 mediated inflammasome inhibitor in patients with mild to moderate atopic dermatitis a proof of concept study with post hoc biomarker analysis
topic atopic dermatitis
GPCR19
inflammasome
precision medicine
taurodeoxycholic acid
clinical trial
url https://www.frontiersin.org/articles/10.3389/fimmu.2025.1560447/full
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