Delving into the Latest Updates on Phenethyl Isothiocyanate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Abrassin

Target

HSF1 x Nrf2

Mechanism

HSF1 inhibitors(heat shock transcription factor 1 inhibitors), Nrf2 stimulants(Nuclear factor erythroid 2-related factor 2 stimulants)

Therapeutic Areas

NeoplasmsRespiratory DiseasesUrogenital Diseases

Active Indication

Prostatic HyperplasiaLung CancerAdvanced Prostate Carcinoma+ [1]

Inactive Indication

Tobacco Use Disorder

Originator Organization

University of Minnesota

Active Organization

JC (Wuxi) Co. Inc.

University of Minnesota

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC9H9NS

InChIKeyIZJDOKYDEWTZSO-UHFFFAOYSA-N

CAS Registry2257-09-2

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。

[Translation]

Main study objectives: Phase Ib: Evaluate the safety and tolerability of JC-5411-L in patients with advanced solid tumors, explore the maximum tolerated dose (MTD) of JC-5411-L, and determine the recommended dose (RP2D) for Phase II clinical studies. Phase II: Evaluate the efficacy and safety of JC-5411-L in patients with ovarian cancer. Secondary study objectives: Evaluate the pharmacokinetic (PK) characteristics of JC-5411-L. Preliminary evaluation of the efficacy of JC-5411-L in the treatment of patients with advanced solid tumors. Exploratory study objectives Evaluate the relationship between the level of biomarkers (including but not limited to p53 protein expression level) in tumor specimens or peripheral blood of patients with advanced solid tumors and the efficacy. Evaluate the relationship between the GST genotype and the efficacy of patients with advanced solid tumors.

Start Date13 Dec 2023

Sponsor / Collaborator

JC (Wuxi) Co. Inc.

NCT00691132 / CompletedPhase 2IIT

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.

Start Date01 Feb 2009

Sponsor / Collaborator

University of Minnesota

[+1]

100 Clinical Results associated with Phenethyl Isothiocyanate

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100 Translational Medicine associated with Phenethyl Isothiocyanate

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100 Patents (Medical) associated with Phenethyl Isothiocyanate

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609

Literatures (Medical) associated with Phenethyl Isothiocyanate

21 Nov 2024·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

Author: 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.

01 Oct 2024·Food and Chemical Toxicology

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

Review

Author: 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.

01 Oct 2024·Folia Microbiologica

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

Article

Author: 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 Deals associated with Phenethyl Isothiocyanate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Phenethyl Isothiocyanate	-	DB12695

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Prostate Carcinoma	Phase 2	CN	JC (Wuxi) Co. Inc.	15 Dec 2021
Prostatic Hyperplasia	Phase 2	CN	JC (Wuxi) Co. Inc.	04 Apr 2014
Lung Cancer	Phase 2	-	University of Minnesota	-
Lung Cancer	Phase 2	-	JC (Wuxi) Co. Inc.	-
Advanced Malignant Solid Neoplasm	Phase 1	CN	JC (Wuxi) Co. Inc.	13 Dec 2023
Tobacco Use Disorder	Preclinical	US	University of Minnesota	01 Feb 2009