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更新于：2025-05-16
Timapiprant
更新于：2025-05-16
概要
基本信息
原研机构 |
在研机构- |
权益机构- |
最高研发阶段无进展临床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/序列
分子式C21H17FN2O2 |
InChIKeyFATGTHLOZSXOBC-UHFFFAOYSA-N |
CAS号851723-84-7 |
关联
13
项与 Timapiprant 相关的临床试验NCT02560610
The Effect of OC000459 on Eosinophilic Airway Inflammation and Asthma Control in Subjects With Refractory Eosinophilic Asthma: a Randomised, Double-blind, Placebo Controlled Trial
NCT02341521
An Evaluation of the Plasma and Urine Pharmacokinetics of Parent Compound and a Metabolite of OC000459 in Healthy Male and Female Subjects
NCT02660489
Effect of the CRTH2 Antagonist OC459 on the Response to Rhinovirus Challenge in Asthma
100 项与 Timapiprant 相关的临床结果
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100 项与 Timapiprant 相关的转化医学
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100 项与 Timapiprant 相关的专利（医药）
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31
项与 Timapiprant 相关的文献（医药）2023-12-01International journal of pharmaceutics: X
Investigation on the use of fused deposition modeling for the production of IR dosage forms containing Timapiprant
Article
作者: Piazza, Alessandro ; Tagliabue, Stefano ; Uboldi, Marco ; Zema, Lucia ; Palugan, Luca ; Gazzaniga, Andrea ; Pertile, Marisa ; Melocchi, Alice ; Foppoli, Anastasia ; Chiappa, Arianna
The present work focused on evaluating the feasibility of fused deposition modeling (FDM) in the development of a dosage form containing Timapiprant (TMP), also known as CHF6532, which is a novel active molecule indicated in the potential treatment of eosinophilic asthma upon oral administration. The resulting product could be an alternative, with potential towards personalization, of immediate release (IR) tablets used in the clinical studies. Formulations based on different polymeric carriers were screened, leading to the identification of a polyvinyl alcohol-based one, which turned out acceptable for versatility in terms of active ingredient content, printability and dissolution performance (i.e. capability to meet the dissolution specification set, envisaging >80% of the drug dissolved within 30 min). Following an in-depth evaluation on the influence of TMP solid state and of the voids volume resulting from printing on dissolution, few prototypes with shapes especially devised for therapy customization were successfully printed and were compliant with the dissolution specification set.
2023-05-01Translational vision science & technology
Attenuation of Laser-Induced Choroidal Neovascularization by Blockade of Prostaglandin D2 Receptor 2.
Article
作者: Kaburaki, Toshikatsu ; Aihara, Makoto ; Soga, Hirotsugu ; Inoue, Tatsuya ; Urade, Yoshihiro ; Kawashima, Hidetoshi ; Ueta, Takashi
Purpose:
The purpose of this study was to investigate the impact of prostaglandin D2 (PGD2) receptor 2 (DP2) on choroidal neovascularization (CNV) formation in mice.
Methods:
Using a laser-induced CNV model, the CNV size of wild-type (WT) mice treated with DP2 antagonist (CAY10471 or OC000459) was compared with that of untreated mice. Vascular endothelial growth factor (VEGF) and MCP-1 levels were also compared between the two groups. Similar experiments were performed comparing DP2 knockout (DP2KO) mice with WT mice (8 and 56 weeks old). The number of infiltrating macrophages to laser spots was also compared between the WT and DP2KO mice. We administered a DP2 antagonist to 15-methyl PGD2 (a DP2 agonist)-stimulated ARPE-19 cells and measured VEGF secretion by enzyme-linked immunosorbent assay. Tube formation assay was performed on human umbilical vein endothelial cells with or without a DP2 antagonist.
Results:
CNV sizes were significantly smaller in mice treated with CAY10471 or OC000459 than in those treated with vehicle. Similarly, the CNV size of DP2KO mice was significantly smaller than that of WT mice. The number of macrophages at laser spots in DP2KO mice was significantly lower than that in WT mice. The VEGF concentration of lasered DP2KO mice's eyes was significantly lower than that of lasered WT mice' eyes. DP2 antagonist treatment suppressed VEGF secretion in ARPE-19 cells under 15-methyl PGD2 stimulation. The tube formation assay suggested that lumen formation was inhibited by a DP2 antagonist.
Conclusions:
DP2 blockade attenuated choroidal neovascularization.
Translational Relevance:
Drugs targeting DP2 are potentially a novel treatment for age-related macular degeneration.
2023-02-01Digestive and liver disease : official journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver
Treatment Trends for Eosinophilic Esophagitis and the Other Eosinophilic Gastrointestinal Diseases: Systematic Review of Clinical Trials
Review
作者: Maniero, Daria ; Barberio, Brigida ; de Bortoli, Nicola ; Savarino, Vincenzo ; Ghisa, Matteo ; Greco, Eliana ; Black, Christopher J ; Ford, Alexander C ; Visaggi, Pierfrancesco ; Savarino, Edoardo
BACKGROUND:
Eosinophilic gastrointestinal diseases (EGIDs) are chronic inflammatory disorders of the gut, including eosinophilic esophagitis (EoE), gastritis (EoG), duodenitis (EoD), gastroenteritis (EoGE), and colitis (EoC). Available treatments may be ineffective in some patients, and several clinical trials are investigating alternative treatments.
AIM:
We performed a systematic review of clinical trials to illustrate EGIDs treatment research trends.
METHODS:
We searched clinicaltrials.gov to identify studies investigating EGIDs treatment. For each trial we analysed relevant data, including therapeutic intervention, method of administration, study outcomes, and temporal trends.
RESULTS:
For EoE, 66 studies were eligible: 26 testing topical corticosteroids (39.4%), 17 (25.8%) monoclonal antibodies, eight (12.1%) dietary measures, five (7.6%) immunomodulators, one (1.5%) esophageal dilation, and nine (13.6%) other medical treatment strategies. With regard to EoG, EoD, and EoGE, 10 studies were testing monoclonal antibodies (71.5%), one immunomodulators (7.1%), one dietary measures (7.1%), and two other treatments (14.3%). There were no trials for EoC. Ongoing studies on corticosteroids are focused on novel delivery systems, including viscous suspensions, orally disintegrating tablets, or capsules. Increased research on monoclonal antibodies was seen from 2018, with interleukin (IL)-4 receptor-α, IL-5 receptor-α, IL-5, IL-13, IL-15, and Siglec-8 as the targets.
CONCLUSION:
Clinical trials on EGIDs are predominantly investigating corticosteroids or monoclonal antibodies. EGIDs therapeutic landscape will be trasnformed imminently.
100 项与 Timapiprant 相关的药物交易
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外链
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 哮喘 | 临床3期 | 美国 | 2021-09-22 | |
| 嗜酸性粒细胞性哮喘 | 临床2期 | 英国 | 2016-09-01 | |
| 炎症 | 临床2期 | 英国 | 2016-09-01 | |
| 普通感冒 | 临床2期 | 英国 | 2015-01-01 | |
| 鼻病毒感染 | 临床2期 | 英国 | 2015-01-01 | |
| 中度特应性皮炎 | 临床2期 | 英国 | 2013-10-01 | |
| 重度特应性皮炎 | 临床2期 | 英国 | 2013-10-01 | |
| 嗜酸粒细胞性食管炎 | 临床2期 | 瑞士 | 2010-08-01 | |
| 持续性哮喘 | 临床2期 | 保加利亚 | 2009-04-01 | |
| 持续性哮喘 | 临床2期 | 匈牙利 | 2009-04-01 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 44 | OC459+Rhinovirus (OC459 (CRTH2 Antagonist)) | 鬱選鑰餘繭選糧憲齋觸(網鏇選艱築蓋襯範鏇製) = 襯構觸簾餘壓觸範製憲 遞繭壓簾構製鏇顧獵積 (淵構艱壓積衊鏇製網築, 鏇簾選鹹鬱製糧鏇鑰顧 ~ 鑰鹹遞憲窪窪繭顧獵夢) 更多 | - | 2021-02-26 | ||
Rhinovirus (Placebo) | 鬱選鑰餘繭選糧憲齋觸(網鏇選艱築蓋襯範鏇製) = 窪憲範廠廠鏇鬱鹽艱製 遞繭壓簾構製鏇顧獵積 (淵構艱壓積衊鏇製網築, 醖襯壓壓鬱齋選襯憲網 ~ 選構醖簾構簾淵鹽夢獵) 更多 | ||||||
N/A | 肺嗜酸性粒细胞增多 sputum eosinophil counts | 68 | 願選窪觸範製糧鬱構觸(觸窪遞選齋蓋網積齋醖): ml = 127 (95% CI, -77 ~ 330), P-Value = 0.214 | 积极 | 2019-09-28 | ||
Placebo | |||||||
临床2期 | 142 | (OC000459 Tablets) | 網窪蓋積鏇獵衊繭壓憲(廠夢艱願網鑰選製夢壓) = 壓齋選夢憲膚齋鬱鬱顧 衊廠網顧淵顧遞遞顧艱 (餘鏇鹽網獵夢獵製觸製, 1.72) 更多 | - | 2016-12-08 | ||
(Placebo Tablets) | 網窪蓋積鏇獵衊繭壓憲(廠夢艱願網鑰選製夢壓) = 艱製醖範範夢簾憲遞壓 衊廠網顧淵顧遞遞顧艱 (餘鏇鹽網獵夢獵製觸製, 1.71) 更多 | ||||||
N/A | - | 壓範夢簾鏇選顧繭選獵(鹽鏇範蓋簾遞製襯遞顧) = 壓蓋遞蓋獵艱築製積積 夢網鹽憲餘鑰壓壓積淵 (鏇鑰積鑰齋積壓夢廠築 ) 更多 | - | 2013-10-01 | |||
Placebo | 壓範夢簾鏇選顧繭選獵(鹽鏇範蓋簾遞製襯遞顧) = 襯製醖遞鹹構選製夢淵 夢網鹽憲餘鑰壓壓積淵 (鏇鑰積鑰齋積壓夢廠築 ) 更多 | ||||||
临床2期 | 132 | 廠襯蓋選願簾襯獵窪廠(鑰觸網蓋範衊窪衊範選) = 壓糧範餘壓簾糧積壓蓋 鑰構鏇艱觸積鏇網觸醖 (壓夢膚鏇艱構範糧齋窪 ) | 积极 | 2012-01-01 | |||
Placebo | 廠襯蓋選願簾襯獵窪廠(鑰觸網蓋範衊窪衊範選) = 構襯壓遞鬱衊網襯壓憲 鑰構鏇艱觸積鏇網觸醖 (壓夢膚鏇艱構範糧齋窪 ) |
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