UR-1505(UR-1505) - 药物靶点：Cytokines x NFATC1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Cytokines x NFATC1

作用机制

细胞因子抑制剂、NFATC1抑制剂(活化T细胞核因子-1抑制剂)、淋巴细胞抑制剂

治疗领域

免疫系统疾病遗传病与畸形皮肤和肌肉骨骼疾病+ [1]

在研适应症-

非在研适应症

特应性皮炎器官移植排斥炎症性肠病+ [2]

原研机构

Palau Pharma SA

在研机构-

非在研机构

Palau Pharma SA

Noucor Health SA

最高研发阶段终止临床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

分子式C10H7F5O4

InChIKeyBLEWPNAUDGZWPU-UHFFFAOYSA-N

CAS号651331-92-9

关联

2

项与 UR-1505 相关的临床试验

EUCTR2007-005672-13-FR / Unknown statusN/A

DOUBLE-BLIND STUDY, RANDOMISED, ACTIVE AND PLACEBO CONTROLLED TO ASSESS THE CLINICAL EFFICACY, SKIN TOLERABILITY AND PHARMACOLOGICAL ACTIVITY OF UR-1505 OINTMENT AT THREE DIFFERENT STRENGHTS IN PATIENTS WITH MILD TO MODERATE PLAQUE-TYPE PSORIASIS

开始日期2007-12-28

申办/合作机构

Palau Pharma SA

EUCTR2007-002550-27-FR / Unknown statusN/A

DOUBLE-BLIND, RANDOMISED, ACTIVE AND PLACEBO CONTROLLED STUDY TO ASSESS THE CLINICAL EFFICACY, SKIN TOLERABILITY AND PHARMACOLOGICAL ACTIVITY OF A NEW TOPICAL COMPOUND (UR-1505 0.5%, 1% AND 2%) IN PATIENTS WITH MILD TO MODERATE ATOPIC DERMATITIS

开始日期2007-07-31

申办/合作机构

Palau Pharma SA

100 项与 UR-1505 相关的临床结果

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100 项与 UR-1505 相关的转化医学

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100 项与 UR-1505 相关的专利（医药）

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4

项与 UR-1505 相关的文献（医药）

2015-09-01·Clinical Therapeutics4区 · 医学

Safety and Activity of UR-1505 in Atopic Dermatitis: A Randomized, Double-blind Phase II Exploratory Trial

4区 · 医学

Article

作者: Pontes, Caridad ; Millier, Aurelie ; Sarasa, Maria ; Vives, Roser

PURPOSEUR-1505 is a new small molecule with immune modulator properties intended for the topical treatment of inflammatory skin diseases that has shown anti-inflammatory effects in models of skin inflammation. We compared the activity of UR-1505 ointment against its vehicle in the treatment of atopic dermatitis. Secondary objectives included exploring dose response, safety, and local tolerability of UR-1505.METHODSPatients with AD lesions on 2 symmetrical topographic areas (arms, leg, or trunk) were included in this unicenter randomized, double-blind, within-patient, controlled Phase II exploratory trial and received simultaneously 2 different treatments (0.5%, 1%, or 2% UR-1505 and vehicle or 0.1% tacrolimus ointment) once daily during 28 days. The primary efficacy end point was the change from baseline in the Investigator Global Assessment score at Day 28. Secondary end points were percentage of area clearance, local Eczema Area Severity Index (local EASI), and local tolerability. A linear mixed model was used, fitting treatment, body side, and group (treatment at the contralateral side) as fixed factors and the patient as a random effect.FINDINGSTwenty-eight patients were randomized and 25 patients were included in the per protocol analysis, with 50 evaluable lesions (n = 13 for vehicle, n = 8 for UR-1505 0.5%, n = 9 for 1% UR-1505, n=8 for 2% UR-1505, and n=12 for tacrolimus). The mean Investigator Global Assessment score change from baseline at Day 28 was -1.7 for vehicle, -1.0, -1.2, and -1.5 for 0.5%, 1%, and 2% UR-1505, respectively, and -2.6% for tacrolimus (P = 0.002). No serious nor causal adverse reactions were reported in this study, but patients reported numerous local symptoms after product applications, especially itching, tingling, tightness, and heat/burning sensations at frequencies that were similar for vehicle, 1% UR-1505, and 2% UR-1505; more frequent with 0.5% UR-1505; and lowest for tacrolimus.IMPLICATIONSThis study found that UR-1505 may not be a suitable option for the treatment of atopic dermatitis due to its lack of clinically relevant effect compared with its vehicle and 0.1% tacrolimus ointment.

2009-01-01·Journal of Pharmacological Sciences3区 · 医学

The New Salicylate Derivative UR-1505 Modulates the Th2/Humoral Response in a Dextran Sodium Sulphate Model of Colitis That Resembles Ulcerative Colitis

3区 · 医学

ArticleOA

作者: Julio Gálvez ; Isabel Ramis ; Antonio Zarzuelo ; Mònica Comalada ; Juan Román ; Manuel Merlos ; Dolors Balsa ; Pedro Michelena ; Elvira Bailón

The aim of the present study was to evaluate the inmunomodulatory effects of UR-1505, a new salicylate derivative, on the T helper (Th)2/humoral response produced during dextran sodium sulfate (DSS)-induced rat colitis. In the in vitro studies, UR-1505 (300 microM) inhibited both the production of interleukin (IL)-10 and IL-5 in concanavalin A (Con A)-activated splenocytes and the production of immunoglobulin (Ig) G and IgA by B-lymphocytes. However, in contrast to the in vitro results, the administration of UR-1505 (10 and 30 mg/kg per day) to rats with established DSS-colitis enhanced both IL-10 and IgA production, whereas it inhibited IgG production, thus ameliorating the intestinal inflammation.

2007-11-01·Biochemical Pharmacology2区 · 医学

The intestinal anti-inflammatory effects of the novel agent UR-1505 in the TNBS model of rat colitis are mediated by T-lymphocyte inhibition

2区 · 医学

Article

作者: Angel Concha ; Juan Román ; Ana Nieto ; Alberto Fernández de Arriba ; Desirée Camuesco ; Antonio Zarzuelo ; Julio Gálvez ; Mònica Comalada ; Elvira Bailón ; Manuel Merlos ; Isabel Ramis

UR-1505 is a novel pentafluoropropoxy derivative of salicylic acid, selected from a series of salicylate derivatives, according to their activity as inhibitors of T-lymphocyte activation. This study describes the anti-inflammatory activity of UR-1505 on trinitrobenzenesulphonic acid-induced colitis in rat, an experimental model that resembles to Crohn's disease (CD), as well as its in vitro effects on T-cells and bone marrow-derived macrophages (BMDM) activation. UR-1505 showed intestinal anti-inflammatory effect, associated with reduced colonic levels of TNFalpha and LTB(4), inhibition of the expression of IFNgamma and iNOS, and lower colonic leukocyte infiltration. The in vitro assays revealed that UR-1505 also inhibited T-lymphocyte proliferation and IL-12/IFNgamma production, two of the main pro-inflammatory cytokines involved in the pathogenesis of CD. However, UR-1505 did not modify LPS- nor IFNgamma-induced activation in BMDM. Thus, UR-1505 specifically affects T-cells without modifying the activation of BMDM. In conclusion, the intestinal anti-inflammatory activity of UR-1505 seems to be mediated by a reduction in the recruitment of immune cells to the inflammatory foci, together with the inhibition of T-cell activation. These results suggest that UR-1505 may be an interesting candidate to be explored for the treatment of CD.

100 项与 UR-1505 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
特应性皮炎	临床2期	法国	Palau Pharma SA	-
特应性皮炎	临床2期	-	Noucor Health SA	-
特应性皮炎	临床2期	西班牙	Palau Pharma SA	-
器官移植排斥	临床2期	西班牙	Palau Pharma SA	-
炎症性肠病	临床2期	西班牙	Palau Pharma SA	-
银屑病	临床2期	西班牙	Palau Pharma SA	-
银屑病	临床2期	-	Noucor Health SA	-
类风湿关节炎	临床2期	西班牙	Palau Pharma SA	-