Asivatrep(Asivatrep) - 药物靶点：TRPV1_在研适应症：寻常痤疮，瘙痒_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

TRPV1

作用机制

TRPV1拮抗剂(类香草素受体拮抗剂)

治疗领域

皮肤和肌肉骨骼疾病

在研适应症

寻常痤疮瘙痒

非在研适应症

脂溢性皮炎轻度特应性皮炎中度特应性皮炎+ [1]

原研机构

Amorepacific Corp.

在研机构

Amorepacific Corp.

非在研机构-

最高研发阶段临床3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C21H22F5N3O3S

InChIKeyUKGJZDSUJSPAJL-YPUOHESYSA-N

CAS号1005168-10-4

关联

13

项与 Asivatrep 相关的临床试验

NCT02965118 / Completed临床3期

Multi Center, Randomized, Double-blind, Placebo-controlled Parallel-group, Phase III Clinical Trial to Evaluate the Safety and Efficacy of PAC-14028 Cream in Mild to Moderate Atopic Dermatitis Patients

This is a phase III study to investigate the safety and efficacy of PAC-14028 cream in Atopic Dermatitis patients.

开始日期2016-11-01

申办/合作机构

Amorepacific Corp.

NCT02748993 / Completed临床1/2期

A Randomized, Double-blind, Placebo-Controlled, Parallel Study to Investigate the Safety, Tolerability, Systemic Exposure and Efficacy of PAC-14028 in Children With Mild to Moderate Pediatric Atopic Dermatitis

This is a phase 1 and 2 study to assess the safety and efficacy of PAC-14028 cream in children with atopic dermatitis.

开始日期2016-03-01

申办/合作机构

Amorepacific Corp.

NCT02757729 / Completed临床2期

Multi Center, Randomized, Double-blind, Placebo-controlled Parallel-group, Phase II Clinical Trial to Evaluate the Safety and Efficacy of PAC-14028 Cream in Mild to Moderate Atopic Dermatitis Patients

This is a phase 2 study to investigate the safety and efficacy of PAC-14028 cream in Atopic Dermatitis patients.

开始日期2015-10-01

申办/合作机构

Amorepacific Corp.

100 项与 Asivatrep 相关的临床结果

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100 项与 Asivatrep 相关的转化医学

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100 项与 Asivatrep 相关的专利（医药）

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12

项与 Asivatrep 相关的文献（医药）

2024-06-01·Allergy

Treatment of atopic dermatitis: Recently approved drugs and advanced clinical development programs

Review

作者: Maintz, Laura ; Müller, Svenja ; Bieber, Thomas

AbstractAtopic dermatitis (AD) represents the most common skin disease characterized by heterogeneous endophenotypes and a high disease burden. In Europe, six new systemic therapies for AD have been approved: the biologics dupilumab (anti‐interleukin‐4 receptor (IL‐4R) α in 2017), tralokinumab (anti‐IL‐13 in 2021), lebrikizumab (anti‐IL‐13 in 2023), and the oral janus kinase (JAK) inhibitors (JAKi) targeting JAK1/2 (baricitinib in 2020 in the EU) or JAK1 (upadacitinib in 2021 and abrocitinib in 2022). Herein, we give an update on new approvals, long‐term safety, and efficacy. Upadacitinib and abrocitinib have the highest short‐term efficacy among the approved systemic therapies. In responders, dupilumab and tralokinumab catch up regarding long‐term efficacy and incremental clinical benefit within continuous use. Recently, the European Medicines Agency has released recommendations for the use of JAKi in patients at risk (cardiovascular and thromboembolic diseases, malignancies, (former) smoking, and age ≥65 years). Furthermore, we give an overview on emerging therapies currently in Phase III trials. Among the topical therapies, tapinarof (aryl hydrocarbon receptor), ruxolitinib (JAK1/2i), delgocitinib (pan‐JAKi), asivatrep (anti‐transient receptor potential vanilloid), and phosphodiesterase‐4‐inhibitors (roflumilast, difamilast) are discussed. Among systemic therapies, current data on cord‐blood‐derived mesenchymal stem cells, CM310 (anti IL‐4Rα), nemolizumab (anti‐IL‐31RA), anti‐OX40/OX40L‐antibodies, neurokinin‐receptor‐1‐antagonists, and difelikefalin (κ‐opioid‐R) are reported.

2022-05-01·Annals of Translational Medicine

Study on the intervention effect and mechanism of bacillus Calmette-Guerin polysaccharide and nucleic acid injection on atopic dermatitis by targeting the transient receptor potential vanilloid subtype 1 pathway

Article

作者: Ding, Changrui ; Wu, Di ; Duan, Tingting ; Wang, Xiufen ; Lv, Shukun ; Liu, Ying ; Xu, Yulong ; Cui, Liran

BackgroundThis study aimed to explore the mechanism of Bacillus Calmette-Guerin polysaccharide and nucleic acid injection (BCG-PSN) targeting the transient receptor potential vanilloid subtype 1 (TRPV1) pathway for atopic dermatitis (AD) in mice.MethodsExperiment 1: a total of 30 Kunming (KM) mice were randomized into blank control, model, BCG-PSN low-dose (25 g/kg), BCG-PSN medium-dose (75 g/kg), BCG-PSN high-dose (225 g/kg), and positive drug (hydrocortisone 25 mg/kg) control groups. The AD model mice were established by induction with 2,4-Dinitrochlorobenzene (DNCB). After treatment in groups, the symptom score and scratching frequency in skin lesions were observed. The levels of immunoglobulin E (IgE), interleukin (IL)-4, IL-31, and IL-13 in serum were detected, as well as the levels of tumor necrosis factor-α (TNF-α), TRPV1, and nuclear factor (NF)-κB p65 in skin lesions in each group. Experiment 2: the optimal dose of BCG-PSN in Experiment 1 was adopted. A total of 20 KM mice were randomized into blank control, model, BCG-PSN, and BCG-PSN + PAC (PAC-14028) groups. The symptom score and scratching frequency in skin lesions were observed. The levels of IgE, IL-4, IL-31, and IL-13 in serum were detected, as well as the levels of TNF-α and TRPV1 in skin lesions in each group.ResultsIn Experiment 1, compared with the blank control group, the ear tissues of mice in model groups developed AD, with increased symptom score, scratching frequency, levels of IgE, IL-4, IL-31, and IL-13 in serum and levels of TNF-α, TRPV1, and NF-κB p65 in skin lesions. Compared with the model group, BCG-PSN low-dose, BCG-PSN medium-dose, BCG-PSN high-dose, and positive drug control groups had reduced AD symptoms, decreased symptom score, and decreased scratching frequency, with declined expression of each inflammatory substance, including the greatest decrease in the medium-dose group. In Experiment 2, after BCG-PSN was combined with PAC, the inflammation indexes decreased compared with those in the model group, and increased compared with those in the BCG-PSN group.ConclusionsIntramuscular BCG-PSN can target the TRPV1 pathway, inhibit inflammation, and improve the symptoms of AD mice.

2022-04-01·Journal of Allergy and Clinical Immunology1区 · 医学

Asivatrep, a TRPV1 antagonist, for the topical treatment of atopic dermatitis: Phase 3, randomized, vehicle-controlled study (CAPTAIN-AD)

1区 · 医学

Article

作者: Lee, Dong Hun ; Nam, Hyun-Jin ; Lee, Yang Won ; Park, Chun Wook ; Won, Chonghyun ; Jung, Kyoungmi ; Park, Miyoung ; Park, Chang Ook ; Chung, Bo Young ; Kim, Kyu Han ; Park, Young-Ho ; Kim, Beom Joon ; Choi, Gyeyoung

BACKGROUNDAsivatrep is a potent and selective antagonist of transient receptor potential vanilloid subfamily V member 1 (TRPV1), which plays an important role in itch and inflammation in atopic dermatitis (AD).OBJECTIVEThis current study aimed to evaluate the efficacy and safety of asivatrep cream in patients with AD.METHODSFor this phase 3 double-blind, vehicle-controlled study, patients aged ≥12 years with mild to moderate AD were enrolled and randomly assigned 2:1 to the 1.0% asivatrep or vehicle group for 8 weeks of twice-daily application (n = 240). The primary end point was the proportion of patients with an Investigator's Global Assessment score (IGA) of 0 or 1 at week 8. Standard safety assessments were conducted.RESULTSAt week 8, significantly more patients in the asivatrep group (36.0%) than in the vehicle group (12.8%) had IGA scores of 0 or 1 (P < .001); significantly more had ≥2 points of improvement on the IGA from baseline score (20.3% vs 7.7%; P = .01). The mean percentage reduction in the Eczema Area and Severity Index (EASI) score was 44.3% for the asivatrep group and 21.4% for the vehicle group at week 8 (P < .001). Significantly more asivatrep-treated patients experienced an improvement of at least 50%, 75%, and 90% on the EASI than the vehicle group. The mean ± SD change in the pruritus visual analog scale score at week 8 was -2.3 ± 2.4 for the asivatrep group and -1.5 ± 2.4 for the vehicle group (P = .02). No significant safety issues were reported.CONCLUSIONAsivatrep improved clinical signs and symptoms of AD and was well tolerated.

100 项与 Asivatrep 相关的药物交易

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