尿素/水杨酸/维A酸/丙酸氯倍他索(Carbamide/Salicylic acid/TRETINOIN/CLOBETASOL PROPIONATE) - 药物靶点：COXs x GR x RARα x RARβ2 x RARγ_在研适应症：斑块状银屑病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

GN 037、GN-037、GN037

靶点

COXs x GR x RARα x RARβ2 x RARγ

作用方式

抑制剂、激动剂

作用机制

COX抑制剂(环氧化酶抑制剂)、GR激动剂(糖皮质激素受体激动剂)、RARα激动剂(维甲酸受体α激动剂)

治疗领域

免疫系统疾病皮肤和肌肉骨骼疾病

在研适应症

斑块状银屑病

非在研适应症-

原研机构

Erciyes Üniversitesi

在研机构-

非在研机构

Erciyes Üniversitesi

权益机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C25H32ClFO5

InChIKeyCBGUOGMQLZIXBE-XGQKBEPLSA-N

CAS号25122-46-7

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关联

2

项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的临床试验

NCT05706870

/ Completed临床2期

A Multicenter Randomized Double-blind Placebo-controlled Parallel Group Phase II Study Evaluating the Clinical Efficacy and Safety of GN-037 Cream Used in the Treatment of Mild to Moderate Plaque Psoriasis

This Phase II study was designed as a multicenter, randomized, double-blind, placebo-controlled and 3-parallel arm, to assess clinical efficacy, safety, and tolerability of GN-037 versus clobetasol 17-propionate and placebo in patients diagnosed with mild to moderate plaque psoriasis at least 6 months ago

开始日期2022-12-07

申办/合作机构

Monitor CRO

NCT05428202

/ Completed临床1期IIT

Phase I Study to Assess Safety, Tolerability and Clinical Benefits of Topically Applied GN-037 Cream in Healthy Volunteers and Patients Diagnosed With Psoriasis

In this Phase I study, three different doses (low, medium and high dose, on the basis of surface area applied) of GN-037 cream (12 volunteers in total) and placebo (6 volunteers in total) will be administered to healthy volunteers. In the active dose arm, 4 healthy volunteers will receive GN-037 cream and 2 healthy volunteers will receive placebo. Randomization in each dose arm will be 2:1.

开始日期2022-03-28

申办/合作机构

Erciyes Üniversitesi

[+1]

100 项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的临床结果

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100 项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的转化医学

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100 项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的专利（医药）

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2

项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的文献（医药）

2024-12-01·Dermatology and Therapy

A Multicenter Randomized Double-Blind Vehicle-Controlled Parallel Group Phase 2 Study Evaluating the Efficacy and Safety of GN-037 Cream in Patients with Mild-to-Moderate Plaque Psoriasis

Article

作者: Pehlivan Ulutaş, Gizem ; Ulu, Nadir ; Altuğ, Sedat ; Uçgun, Hanife ; Demirel Öğüt, Neslihan ; Çınar, Salih Levent ; Türkoğlu, Zafer ; Zindancı, İlkin ; Yaşar, Şirin ; Doğramacı, Asena Çiğdem ; Melikoğlu, Mehmet ; Güler Özden, Müge ; Özkök Akbulut, Tuğba Özkök ; Kozlu, Serhat ; Kartal, Selda Pelin ; Karstarlı Bakay, Özge Sevil ; Hızlı, Pelin ; Topkarcı, Zeynep ; Hapa, Fatma Aslı ; Engin, Burhan ; Temiz, Selami Aykut ; Canpolat, Filiz ; Serdaroğlu, Server ; Dursun, Recep ; Türsen, Ümit ; Polat Ekinci, Algün ; Küçük, Özlem Su ; Bülbül Başkan, Emel

Abstract:

Introduction:

Topical therapies are used in almost all patients with psoriasis. A novel fixed topical combination cream (GN-037) with a lower concentration (0.0356%) of clobetasol 17-propionate (CP) was developed together with urea, salicylic acid, and retinoic acid to provide a better benefit–risk ratio. The present multicenter randomized double-blind vehicle-controlled parallel group phase 2 study aimed to investigate the efficacy and safety of GN-037 in patients with mild-to-moderate plaque psoriasis (MMPP).

Methods:

Patients (n = 190) were randomized (2:2:1) to receive GN-037 or CP or vehicle (V) cream twice daily to a selected target body lesion for 4 weeks. The primary endpoint was treatment success defined as percentage of patients with at least two-grade improvement in Investigator’s Global Assessment Score (IGA) and IGA score equal to 0 or 1 evaluated at weeks 2, 4, 6, and 8 in each arm compared with baseline. Treatment-emergent adverse events (TEAEs) and safety were evaluated throughout the study.

Results:

GN-037 demonstrated statistically significant superiority over V throughout the study. At week 4, treatment success was achieved in 37.9% of patients in the GN-037 arm compared with 29.2% and 9.1% in the CP and V arms, respectively. At least two-grade improvement compared with baseline was achieved by 57.6%, 72.7%, and 80.3% of the patients in the GN-037 arm for erythema, plaque elevation, and scaling, respectively. The mean changes in affected BSA were −2.1 ± 2.9, −1.8 ± 2.4, and −0.5 ± 1.6 in the GN-037, CP, and V arms, respectively. The TEAEs were similar among the arms and the most frequently observed TEAEs were Psoriasis Area and Severity Index (PASI) increase in all arms.

Conclusions:

GN-037 was more effective than V in achieving primary and all secondary endpoints throughout the study. Safety data did not reveal any new safety concerns with the combination cream product. Therefore, 4 weeks of GN-037 treatment demonstrated an excellent efficacy and safety profile in patients with MMPP.

Trial Registration number:

ClinicalTrials.gov identifier, NCT05706870.

2023-07-01·Dermatology and therapy

Safety and Efficacy of a Novel Combination Cream (GN-037) in Healthy Volunteers and Patients with Plaque Psoriasis: A Phase 1 Trial

Article

作者: Cinar, Salih L ; Inal, Ahmet ; Altug, Sedat ; Mazicioglu, Mustafa M ; Karasulu, Hatice Y ; Mehmetoglu Al, Ayca ; Kozlu, Serhat ; Ulu, Nadir ; Sezer, Zafer ; Diril, Mine

INTRODUCTION:

Psoriasis is a common skin disorder associated with physical and psychological burdens. Visible disfiguration can trigger a negative reaction which can cause much of the readily measurable psychological burden of the disease. Although many biological treatments provide some success in the initial clearance of lesions, there is a dispute about the long-term maintenance of the disease, as no current biological treatment has been shown to be curative. Topical therapies are still the most widely used agents as first-line and maintenance treatment for psoriasis. The present study aimed to investigate the safety, tolerability, and, to some extent, efficacy of GN-037 cream in patients with psoriasis and healthy volunteers.

METHODS:

A randomized, double-blind, single-center, placebo-controlled phase 1 clinical study was conducted to evaluate the safety, tolerability, and clinical efficacy of GN-037 cream topically applied twice daily for 2 weeks in healthy subjects (n = 12) and patients (n = 6) diagnosed with plaque-type psoriasis. Six healthy subjects received placebo. Patients with plaque psoriasis were evaluated by a dermatologist, and Physician Global Assessment (PGA) score was required to be ≥ 3 (moderate psoriasis) at screening.

RESULTS:

A total of 31 adverse events (AEs) occurred in 13 participants during the study: 9 AEs in healthy subjects receiving GN-037 cream, 3 AEs in healthy subjects receiving placebo, and 1 AE in one psoriatic patient. The most frequently reported AEs were reactions at the application site, including erythema, exfoliation, pruritus, and burning sensation. During the baseline evaluation, one patient had a PGA score of 3 (moderate) and five patients had a PGA score of 4 (severe). On day 14, in treatment, four patients experienced second grade and two patients third grade improvements compared with baseline, indicating a shift of patients from moderate and severe disease to mild disease and to almost clear (score 2 or 1). There were slight increases in plasma tumor necrosis factor (TNF)-α, interleukin-17 (IL-17) and interleukin-23 (IL-23) levels in both healthy volunteers and patients throughout the study, as compared with baseline.

CONCLUSION:

The results of this phase 1 trial conducted in 18 healthy volunteers and 6 patients with plaque psoriasis demonstrated a favorable safety and tolerability profile for GN-037; therefore, further clinical development of GN-037 in a phase 2 clinical trial has been initiated in patients with mild to moderate plaque psoriasis (NCT05706870).

TRIAL REGISTRATION NUMBER:

NCT05428202.

1

项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的新闻（医药）

2024-09-25

·BioSpace

GEN Announces Positive Phase 2 Clinical Trial Results for GN-037 Topical Cream in Patients With Mild to Moderate Plaque Psoriasis

ANKARA, TURKEY / ACCESSWIRE / September 25, 2024 / GEN Pharmaceuticals (GENIL.IS), a leading Turkish pharmaceutical company, has announced the positive results of its Phase 2 clinical trial evaluating the safety and efficacy of its investigational drug, GN-037 topical cream , in treating mild to moderate plaque psoriasis. The findings were presented at Amsterdam’s European Academy of Dermatology and Venereology (EADV) 2024 Congress . GEN Pharmaceuticals GEN Pharmaceuticals Manufacturing Facility This multicenter, randomized, double-blind, placebo-controlled Phase 2 study involved 190 patients across 19 clinical centers in Türkiye. Patients were treated with GN-037 , clobetasol 17-propionate , or placebo twice daily for four weeks, followed by an additional four-week observation period. The study demonstrated GN-037’s statistically significant superiority in reducing psoriasis symptoms compared to placebo, positioning it as a promising new treatment option for psoriasis patients worldwide. Key Findings: The GN-037 Phase 2 trial met the primary endpoint: treatment success,defined as the percentage of patients with at least a 2-grade improvement in Investigator’s Global Assessment (IGA) score and achieving an IGA score of 0 or 1. 37.9% of patients treated with GN-037 achieved treatment success at week four compared to 9.1% in the placebo group ( P =0.006 ). GN-037 demonstrated significant improvements in reducing erythema (57.6%, P =0.008) , plaque elevation (72.7%, P =0.001) , and scaling (80.3%, P =0.006) compared to placebo. 31.8% of patients in the GN-037 group achieved at least a 75% reduction in PASI , compared to 6.1% in the placebo group ( P =0.009 ). No new safety concerns emerged with similar treatment-emergent adverse events across all arms. Abidin Gülmüş , Chairman of GEN, stated: “We are thrilled to announce the positive results of our Phase 2 clinical trial. We believe GN-037 offers new hope for the global psoriasis community.” Nadir Ulu, MD, PhD , Vice President of R&D, added: “Our Phase 2 trial results highlighted GN-037’s potential to improve patient outcomes significantly, and it may provide a novel, well-tolerated treatment option for patients with mild to moderate plaque psoriasis.” About GEN: Founded in 1998, GEN is Türkiye’s leading speciality pharmaceutical company. It is focused on developing innovative therapies across multiple therapeutic areas, with significant R&D investments and a commitment to advancing global healthcare. GEN actively works in both in-licensing and out-licensing business models. GEN partners with leading global pharmaceutical companies to bring innovative therapies and rare solutions to communities in its countries. It also develops and produces highly demanded and competitive therapeutic products in its GMP-certified manufacturing facility to bring therapy solutions required in international markets. For more information, visit . For inquiries: Bulutay GÜNEŞ , Head of Corporate Brand, b.gunes@genilac.com Ali KETENCİOĞLU , Investor Relations Manager, a.ketencioglu@genilac.com Contact Information Bulutay Güneş Head of Corporate Brand b.gunes@genilac.com Ali Ketencioğlu Investor Relations Manager a.ketencioglu@genilac.com SOURCE: GEN Pharmaceuticals View the original press release on newswire.com.

临床结果临床2期

100 项与尿素/水杨酸/维A酸/丙酸氯倍他索相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
斑块状银屑病	临床2期	土耳其	-	2022-12-07
银屑病	临床1期	土耳其	Erciyes Üniversitesi	2022-03-28

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05706870 (not provided, Pubmed \| Dermatol Ther (Heidelb))	临床2期	斑块状银屑病	190	GN-037 Cream	蓋鏇齋醖廠網選鬱網餘(蓋獵觸繭鹽糧製齋顧餘) = 膚齋獵淵艱窪積鹹遞鑰蓋艱願繭廠鏇範製憲膚 (糧糧憲範醖網餘夢製網 )	积极	2024-12-01
				Clobetasol 17-propionate (CP) Cream	蓋鏇齋醖廠網選鬱網餘(蓋獵觸繭鹽糧製齋顧餘) = 鬱觸齋齋餘觸夢製衊顧蓋艱願繭廠鏇範製憲膚 (糧糧憲範醖網餘夢製網 )
NCT05706870 (Biospace) 人工标引	临床2期	斑块状银屑病	190	GN-037GN-037 topical cream	製鑰鑰鏇夢網醖觸憲鏇(廠築構醖製夢壓憲艱襯) = 窪範積遞製構窪鑰鑰積簾鏇簾襯廠範獵獵製製 (繭膚範築壓獵觸鹹鏇鏇 ) 达到更多	积极	2024-09-25
				Placebo	製鑰鑰鏇夢網醖觸憲鏇(廠築構醖製夢壓憲艱襯) = 鑰繭鑰鏇醖顧網淵願鹽簾鏇簾襯廠範獵獵製製 (繭膚範築壓獵觸鹹鏇鏇 ) 达到更多
NCT05428202 (Phase 1 Trial, Pubmed \| Dermatol Ther (Heidelb))	临床1期	斑块状银屑病一线 \| 维持	-	GN-037 cream	壓遞齋鏇積鹹遞憲獵願(鏇窪壓網網願範齋艱糧) = 構齋鏇衊廠遞衊繭製衊夢範窪築鬱選範製簾選 (願齋願獵齋鑰膚積願齋 )	积极	2023-07-01
				Placebo	壓遞齋鏇積鹹遞憲獵願(鏇窪壓網網願範齋艱糧) = 範觸膚蓋廠遞衊觸淵簾夢範窪築鬱選範製簾選 (願齋願獵齋鑰膚積願齋 )