苯乙基异硫氰酸酯(Phenethyl Isothiocyanate) - 药物靶点：HSF1 x Nrf2_在研适应症：前列腺增生症，肺癌，晚期前列腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Abrassin

靶点

HSF1 x Nrf2

作用机制

HSF1抑制剂(heat shock transcription factor 1 inhibitors)、Nrf2刺激剂(核转录因子的激活红细胞2相关因子刺激剂)

治疗领域

肿瘤呼吸系统疾病泌尿生殖系统疾病

在研适应症

前列腺增生症肺癌晚期前列腺癌+ [1]

非在研适应症

烟草依赖

原研机构

University of Minnesota

在研机构

无锡杰西医药股份有限公司

University of Minnesota

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评-

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结构

分子式C9H9NS

InChIKeyIZJDOKYDEWTZSO-UHFFFAOYSA-N

CAS号2257-09-2

关联

5

项与苯乙基异硫氰酸酯相关的临床试验

NCT00005883 / Completed临床1期IIT

A Phase I - Part B Multiple Dose Trial of Phenethyl Isothiocyanate

RATIONALE: Chemoprevention therapy is the use of certain drugs to try to prevent the development or recurrence of cancer. Phenethyl isothiocyanate may be effective in preventing lung cancer in smokers.
PURPOSE: Phase I trial of phenethyl isothiocyanate in preventing lung cancer in people who smoke.

开始日期-

申办/合作机构

NYU Langone Health

[+1]

CTR20232507 / Recruiting临床1期

JC-5411-L 在晚期实体瘤患者中的安全性、耐受性、药代动力学及初步疗效的多中心、开放Ⅰb/Ⅱ 期临床研究

主要研究目的： Ⅰb期：评价JC-5411-L在晚期实体瘤患者的安全性和耐受性，探索JC-5411-L的最大耐受剂量（MTD），确定II期临床研究推荐剂量（RP2D）。 Ⅱ期：评价JC-5411-L在卵巢癌患者中的有效性和安全性。次要研究目的：评价JC-5411-L的药代动力学（PK）特征。初步评价JC-5411-L治疗晚期实体瘤患者的疗效。探索性研究目的评价晚期实体瘤患者的肿瘤标本或外周血中的生物标记物水平（包括但不限于p53 蛋白表达水平）与疗效的关系。评价晚期实体瘤患者的GST基因型与疗效的关系。

开始日期2023-12-13

申办/合作机构

无锡杰西医药股份有限公司

NCT00691132 / Completed临床2期IIT

Randomized Trial of PEITC as a Modifier of NNK Metabolism in Smokers

RATIONALE: Chemoprevention is the use of certain drugs to keep cancer from forming. The use of phenethyl isothiocyanate may prevent lung cancer in people who smoke cigarettes.
PURPOSE: This randomized clinical trial is studying phenethyl isothiocyanate to see how well it works in preventing lung cancer in smokers.

开始日期2009-02-01

申办/合作机构

University of Minnesota

[+1]

100 项与苯乙基异硫氰酸酯相关的临床结果

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100 项与苯乙基异硫氰酸酯相关的转化医学

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100 项与苯乙基异硫氰酸酯相关的专利（医药）

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609

项与苯乙基异硫氰酸酯相关的文献（医药）

2024-11-21·Toxicology Mechanisms and Methods

Naturally-derived phenethyl isothiocyanate modulates apoptotic induction through regulation of the intrinsic cascade and resulting apoptosome formation in human malignant melanoma cells

Article

作者: Kyriakou, Sotiris ; Tragkola, Venetia ; Panayiotidis, Mihalis I. ; Anestopoulos, Ioannis ; Pappa, Aglaia ; Franco, Rodrigo ; Amery, Tom

Malignant melanoma is the most aggressive type of skin cancer with increasing incidence rates worldwide. On the other hand, watercress is a rich source of phenethyl isothiocyanate (PEITC), among others, which has been widely investigated for its anticancer properties against various cancers. In the present study, we evaluated the role of a watercress extract in modulating apoptotic induction in an in vitro model of human malignant melanoma consisting of melanoma (A375, COLO-679, COLO-800), non-melanoma epidermoid carcinoma (A431) and immortalized, non-tumorigenic keratinocyte (HaCaT) cells. Moreover, the chemical composition of the watercress extract was characterized through UPLC MS/MS and other analytical methodologies. In addition, cytotoxicity was assessed by the alamar blue assay whereas apoptosis was determined, initially, by a multiplex activity assay kit (measuring levels of activated caspases -3, -8 and -9) as well as by qRT-PCR for the identification of major genes regulating apoptosis. In addition, protein expression levels were evaluated by western immunoblotting. Our data indicate that the extract contains various phytochemicals (e.g. phenolics, flavonoids, pigments, etc.) while isothiocyanates (ITCs; especially PEITC) were the most abundant. In addition, the extract was shown to exert a significant time- and dose-dependent cytotoxicity against all malignant melanoma cell lines while non-melanoma and non-tumorigenic cells exhibited significant resistance. Finally, expression profiling revealed a number of genes (and corresponding proteins) being implicated in regulating apoptotic induction through activation of the intrinsic apoptotic cascade. Overall, our data indicate the potential of PEITC as a promising anti-cancer agent in the clinical management of human malignant melanoma.

2024-10-01·Food and Chemical Toxicology

RIFM fragrance ingredient safety assessment, phenethyl alcohol, CAS Registry Number 60-12-8

Review

作者: Jones, L ; Sullivan, G ; Muldoon, J ; Bartlett, A ; Belsito, D ; Schember, I ; Thakkar, Y ; Bryant-Freidrich, A ; Api, A M ; Lavelle, M ; Burton, G A ; Penning, T M ; Joshi, K ; Ritacco, G ; Botelho, D ; Dagli, M L ; Lapczynski, A ; Tokura, Y ; Sadekar, N ; Moustakas, H ; Schultz, T W ; Deodhar, C ; Lee, I ; Chon, H ; Fryer, A D ; Farrell, K ; Cancellieri, M A ; Siddiqi, F ; Dekant, W ; Sipes, I G ; Bruze, M

A review.Phenethyl alc. was evaluated for genotoxicity, repeated dose toxicity, reproductive toxicity, local respiratory toxicity, photoirritation/photoallergenicity, skin sensitization, and environmental safety.The existing information supports the use of this material as described in this safety assessment.The Expert Panel for Fragrance Safety concludes that this material is safe as described in this safety assessment.

2024-10-01·Folia Microbiologica

Efficacy of outer membrane permeabilization in promoting aromatic isothiocyanates-mediated eradication of multidrug resistant Gram-negative bacteria and bacterial persisters

Article

作者: Lo, Chung-Cheng ; Yeh, Tzu-Hui ; Wang, Tzu-Hui ; Lo, Horng-Ren ; Jao, Ya-Hsuan

Multidrug resistant (MDR) bacteria are recognized to be one of the most important problems in public health. The outer membrane permeability is a critical intrinsic mechanism of bacterial resistance. In addition, bacteria produce a small number of dormant persister cells causing multidrug tolerance that reduces antimicrobial efficacy. This study aimed to evaluate the inhibitory effects of the combination of aromatic isothiocyanates (ITCs) with membrane-active agents on bacterial persisters and MDR Gram-negative bacteria. Our study demonstrated that membrane-active agents, particularly ethylenediaminetetraacetic acid (EDTA) synergistically enhanced the inhibitory activity of aromatic benzyl ITC and phenethyl ITC against most Gram-negative bacteria strains with fractional inhibitory concentration index values ranging from 0.18 to 0.5 and 0.16 to 0.5, respectively, and contributed to an 8- to 64-fold minimal inhibitory concentration reduction compared with those of aromatic ITCs alone. The EDTA-aromatic ITCs combination effectively reduced the survival rates of tested bacteria and significantly eradicated bacterial persisters (p = 0.033 and 0.037, respectively). The growth kinetics analysis also supported the enhanced inhibitory effect of EDTA-aromatic ITCs combination against tested bacteria. Our results suggested an alternate treatment strategy against Gram-negative bacteria, promoting the entry of aromatic ITCs into bacterial cytoplasm to facilitate bacterial clearance and thus preventing the development of bacterial resistance.

100 项与苯乙基异硫氰酸酯相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	苯乙基异硫氰酸酯	-	DB12695

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
晚期前列腺癌	临床2期	中国	无锡杰西医药股份有限公司	2021-12-15
前列腺增生症	临床2期	中国	无锡杰西医药股份有限公司	2014-04-04
肺癌	临床2期	-	University of Minnesota	-
肺癌	临床2期	-	无锡杰西医药股份有限公司	-
晚期恶性实体瘤	临床1期	中国	无锡杰西医药股份有限公司	2023-12-13
烟草依赖	临床前	美国	University of Minnesota	2009-02-01

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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


AACR2011	N/A	乳腺癌	-	Phenethyl isothiocyanate (PEITC)	衊窪積遞鬱鬱網鹹淵襯(範淵鏇構鏇簾製憲鏇餘) = 構鬱窪鬱簾廠憲遞夢願衊淵淵製膚窪齋餘糧鬱 (網繭簾獵觸膚鏇壓選憲 )	-	2011-04-15