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更新于：2026-07-11
Remetinostat
更新于：2026-07-11
概要
基本信息
在研机构- |
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/序列
分子式C16H21NO6 |
InChIKeyXDZAHHULFQIBFE-UHFFFAOYSA-N |
CAS号946150-57-8 |
关联
9
项与 Remetinostat 相关的临床试验NCT07577297
Comparative Study on the Effect of Kinesio Taping in Climacteric Women With Nonspecific Cervical Pain: ARandomized Clinical Trial.
ITMCTR2024000220
A clinical study on the treatment of knee osteoarthritis with homologous acupuncture of shape and qi
NCT03875859
A Phase 2 Open Label, Single Arm Trial to Investigate the Efficacy and Safety of Topical Remetinostat Gel as Neoadjuvant Therapy in Patients Undergoing Surgical Resection of Squamous Cell Carcinoma (SCC)
100 项与 Remetinostat 相关的临床结果
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100 项与 Remetinostat 相关的转化医学
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100 项与 Remetinostat 相关的专利（医药）
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7
项与 Remetinostat 相关的文献（医药）2024-11-01EUROPEAN JOURNAL OF PHARMACOLOGY
Topical histone deacetylase inhibitor remetinostat improves IMQ-induced psoriatic dermatitis via suppressing dendritic cell maturation and keratinocyte differentiation and inflammation
Article
作者: Jiang, Qian ; Zhou, Xingchen ; Huang, Huining ; Jin, Liping
Psoriasis is a chronic inflammatory skin disease characterized by excessive proliferation of keratinocytes and infiltration of immune cells. Although psoriasis has entered the era of biological treatment, there is still a need to explore more effective therapeutic targets and drugs due to the presence of resistance and adverse reactions to biologics. Remetinostat, an HDAC inhibitor, can maintain its potency within the skin with minimal systemic effects, making it a promising topical medication for treating psoriasis. But its effectiveness in treating psoriasis has not been evaluated. In this study, the topical application of remetinostat significantly improved psoriasiform inflammation in an imiquimod-induced mice model by inhibiting CD86 expression of CD11C+I-A/I-E+ dendritic cells (DCs) in the skin. Moreover, remetinostat could dampen the maturation and activation of bone marrow-derived DCs in vitro, as well as the expression of psoriasis-related inflammatory mediators by keratinocytes. In addition, remetinostat could promote keratinocyte differentiation without affecting its proliferation. Our findings demonstrate that remetinostat improves psoriasis by inhibiting the maturation and activation of DCs and the differentiation and inflammation of keratinocytes, which may facilitate the potential application of remetinostat in anti-psoriasis therapy.
2024-10-01ARCHIV DER PHARMAZIE
Soft drug inhibitors for the epigenetic targets lysine‐specific demethylase 1 and histone deacetylases
Article
作者: Baniahmad, Adina A. ; Seitz, Johannes ; Schüle, Roland ; Auth, Marina ; Preissl, Sebastian ; Hein, Lutz ; Schulz‐Fincke, Johannes ; Prinz, Tony ; Jung, Manfred ; Tzortzoglou, Pavlos ; Hau, Mirjam ; Willmann, Dominica ; Schmidtkunz, Karin ; Metzger, Eric
Abstract:
Epigenetic modulators such as lysine‐specific demethylase 1 (LSD1) and histone deacetylases (HDACs) are drug targets for cancer, neuropsychiatric disease, or inflammation, but inhibitors of these enzymes exhibit considerable side effects. For a potential local treatment with reduced systemic toxicity, we present here soft drug candidates as new LSD1 and HDAC inhibitors. A soft drug is a compound that is degraded in vivo to less active metabolites after having achieved its therapeutic function. This has been successfully applied for corticosteroids in the clinic, but soft drugs targeting epigenetic enzymes are scarce, with the HDAC inhibitor remetinostat being the only example. We have developed new methyl ester‐containing inhibitors targeting LSD1 or HDACs and compared the biological activities of these to their respective carboxylic acid cleavage products. In vitro activity assays, cellular experiments, and a stability assay identified potent HDAC and LSD1 soft drug candidates that are superior to their corresponding carboxylic acids in cellular models.
2023-06-01Journal of labelled compounds & radiopharmaceuticals
Nitrilase mediated mild hydrolysis of a carbon‐14 nitrile for the radiosynthesis of 4‐(7‐hydroxycarbamoyl‐[1‐14C‐heptanoyl]‐oxy)‐benzoic acid methyl ester, [14C]‐SHP‐141: A novel class I/II histone deacetylase (HDAC) inhibitor
Article
作者: Moody, Thomas S. ; Chappell, Todd ; Kitson, Sean L. ; Watters, William ; Mazitschek, Ralph
A strategy has been developed for the carbon‐14 radiosynthesis of [14C]‐SHP‐141, a 4‐(7‐hydroxycarbamoyl‐heptanoyloxy)‐benzoic acid methyl ester derivative containing a terminal hydroxamic acid. The synthesis involved four radiochemical transformations. The key step in the radiosynthesis was the conversion of the 7‐[14C]‐cyano‐heptanoic acid benzyloxyamide [14C]‐4 directly into the carboxylic acid derivative, 7‐benzyloxycarbamoyl‐[14C]‐heptanoic acid [14C]‐8 using nitrilase‐113 biocatalyst. The final step involved deprotection of the benzyloxy group using catalytic hydrogenation to facilitate the release of the hydroxamic acid without cleaving the phenoxy ester. [14C]‐SHP‐141 was isolated with a radiochemical purity of 90% and a specific activity of 190 μCi/mg from four radiochemical steps starting from potassium [14C]‐cyanide in a radiochemical yield of 45%.
550
项与 Remetinostat 相关的新闻（医药）2026-07-10
·生物展会
100 项与 Remetinostat 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D10977 | Remetinostat | - |
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 |
|---|---|---|---|---|
| 鲍恩病 | 临床2期 | 美国 | 2019-12-12 | |
| 皮肤鳞状细胞癌 | 临床2期 | 美国 | 2019-12-12 | |
| 基底细胞癌 | 临床2期 | 美国 | 2018-07-07 | |
| 斑秃 | 临床2期 | - | 2017-02-01 | |
| 皮肤T细胞淋巴瘤 | 临床2期 | 美国 | 2014-11-01 | |
| 斑块状银屑病 | 临床1期 | 澳大利亚 | 2012-09-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 25 | 顧衊艱製艱鑰鑰觸繭獵(築餘築繭觸窪襯衊鹽鹹) = 糧鹽鏇糧鬱憲網網範壓 餘鬱廠衊艱範廠鬱蓋餘 (蓋襯膚觸範窪齋鹽鹹淵 ) 更多 | 积极 | 2021-09-01 | |||
临床2期 | 4 | 製觸廠夢遞鑰顧築鹽觸 = 積糧廠繭窪憲構觸選艱 艱觸觸夢壓蓋積獵鑰壓 (範構遞醖顧鬱範襯糧範, 鏇鹹觸顧廠蓋獵鏇蓋壓 ~ 廠糧餘齋範顧夢廠獵廠) 更多 | - | 2021-05-20 | |||
临床2期 | 30 | 積鏇衊蓋壓窪夢衊艱鏇 = 選顧鏇顧窪壓衊衊憲製 夢構繭繭範廠鹽鬱願齋 (觸鬱獵齋積醖蓋淵積餘, 鑰淵築積範鏇膚構鏇憲 ~ 窪蓋願衊鹹壓鹽壓鬱壓) 更多 | - | 2021-01-05 | |||
临床1期 | 18 | 壓糧襯壓鏇鹹遞膚膚築(觸鹽遞遞願鏇廠網醖築) = 簾遞鑰鹹淵觸衊憲範製 鹹鏇蓋蓋構繭膚廠鬱鏇 (範鑰餘鬱繭範鏇餘齋醖 ) 更多 | 积极 | 2014-05-20 | |||
placebo | 壓糧襯壓鏇鹹遞膚膚築(觸鹽遞遞願鏇廠網醖築) = 範遞憲壓淵網築觸鬱鬱 鹹鏇蓋蓋構繭膚廠鬱鏇 (範鑰餘鬱繭範鏇餘齋醖 ) 更多 |
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