ITX-5061(ITX-5061) - 药物靶点：SCARB1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

SCARB1

作用机制

SCARB1 抑制剂(清道夫受体B类成员-1 抑制剂)

治疗领域

感染消化系统疾病

在研适应症-

非在研适应症

丙型肝炎

原研机构

iTherX Pharmaceuticals, Inc.

在研机构-

非在研机构

iTherX Pharmaceuticals, Inc.

最高研发阶段无进展临床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C30H38ClN3O7S

InChIKeyICIJBYYMEBOTQP-UHFFFAOYSA-N

CAS号1252679-52-9

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关联

3

项与 ITX-5061 相关的临床试验

NCT01560468

/ Terminated临床1期IIT

Phase I Study of Hepatitis C Virus (HCV) Entry Inhibitor (ITX 5061) in Liver Transplant Recipients With HCV Infection

This study will test the safety and tolerability of HCV Entry Inhibitor ITX 5061 in Liver Transplant Recipients with Hepatitis C infection. The investigators hypothesize that ITX 5061 oral monotherapy will be safe in adults during and after liver transplantation and that therapy will also inhibit HCV infection of newly transplanted livers in adults with prior HCV infection.

开始日期2012-03-01

申办/合作机构

iTherX Pharmaceuticals, Inc.

NCT01292824

/ Completed临床1期IIT

Phase I Study of Hepatitis C Virus (HCV) Entry Inhibitor (ITX 5061) in Liver Transplant Recipients With HCV Infection

This is a phase I pilot study to determine the safety and preliminary efficacy of a novel hepatitis C virus (HCV) entry inhibitor (ITX 5061) in patients with HCV infection undergoing liver transplantation.

开始日期2011-02-01

申办/合作机构

University of Birmingham

[+2]

NCT01165359

/ Completed临床1期IIT

A Randomized, Double-Blind, Phase 1b Study to Assess the Safety and Activity of the HCV Entry Inhibitor ITX 5061 in Treatment-Naive HCV Mono-Infected Adults

Hepatitis C (HCV) is a disease that affects the liver. ITX 5061 is a new medication that is being tested to treat HCV. This study will evaluate the safety of ITX 5061 and examine different doses of the medication to evaluate which dose is the most effective at lowering the amount of HCV in the blood.

开始日期2010-09-01

申办/合作机构

National Institute of Allergy & Infectious Diseases

100 项与 ITX-5061 相关的临床结果

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100 项与 ITX-5061 相关的转化医学

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100 项与 ITX-5061 相关的专利（医药）

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11

项与 ITX-5061 相关的文献（医药）

2023-06-01·Mini-Reviews in Medicinal Chemistry

Inhibitors Targeting Hepatitis C Virus (HCV) Entry

Review

作者: de Araújo-Júnior, João Xavier ; da Silva-Júnior, Edeildo Ferreira ; da Silva Santos-Júnior, Paulo Fernando

Abstract:Infections caused by the Hepatitis C virus (HCV) affect around 70 million people worldwide, leading to serious liver problems, such as fibrosis, steatosis, and cirrhosis, in addition to progressing to hepatocellular carcinoma and becoming globally the main cause of liver disease. Despite great therapeutic advances in obtaining pan-genotypic direct-acting antivirals (DAAs), around 5-10% of affected individuals are unable to eliminate the virus by their own immune system’s activity. Still, there are no licensed vaccines so far. In this context, the orchestrated process of virus entry into host cells is a crucial step in the life cycle and the infectivity capability of most viruses. In recent years, the entry of viruses has become one of the main druggable targets used for designing effective antiviral molecules. This goal has come to be widely studied to develop pharmacotherapeutic strategies against HCV, combined or not with DAAs in multitarget approaches. Among the inhibitors found in the literature, ITX 5061 corresponds to the most effective one, with EC50 and CC50 values of 0.25 nM and >10 μM (SI: 10,000), respectively. This SRBI antagonist completed the phase I trial, constituting a promising compound against HCV. Interestingly, chlorcyclizine (an antihistamine drug) showed action both in E1 apolipoproteins (EC50 and CC50 values of 0.0331 and 25.1 μM, respectively), as well as in NPC1L1 (IC50 and CC50 values of 2.3 nM and > 15 μM, respectively). Thus, this review will discuss promising inhibitors targeting HCV entry, discussing their SAR analyzes, recent contributions, and advances in this field.

2018-04-01·EMBO Molecular Medicine1区 · 医学

Sprouty2 loss‐induced IL 6 drives castration‐resistant prostate cancer through scavenger receptor B1

1区 · 医学

ArticleOA

作者: Repiscak, Peter ; Fleming, Janis ; Ahmad, Imran ; Teo, Katy ; Harle, Victoria ; Loveridge, Carolyn ; Blomme, Arnaud ; Hedley, Ann ; Mackay, Gillian ; Mui, Ernest ; Leung, Hing Y ; Patel, Rachana ; van den Broek, Niels ; Edwards, Joanne ; Sansom, Owen J ; Hamdy, Freddie C ; Salji, Mark

Metastatic castration-resistant prostate cancer (mCRPC) is a lethal form of treatment-resistant prostate cancer and poses significant therapeutic challenges. Deregulated receptor tyrosine kinase (RTK) signalling mediated by loss of tumour suppressor Sprouty2 (SPRY2) is associated with treatment resistance. Using pre-clinical human and murine mCRPC models, we show that SPRY2 deficiency leads to an androgen self-sufficient form of CRPC Mechanistically, HER2-IL6 signalling axis enhances the expression of androgen biosynthetic enzyme HSD3B1 and increases SRB1-mediated cholesterol uptake in SPRY2-deficient tumours. Systemically, IL6 elevated the levels of circulating cholesterol by inducing host adipose lipolysis and hepatic cholesterol biosynthesis. SPRY2-deficient CRPC is dependent on cholesterol bioavailability and SRB1-mediated tumoral cholesterol uptake for androgen biosynthesis. Importantly, treatment with ITX5061, a clinically safe SRB1 antagonist, decreased treatment resistance. Our results indicate that cholesterol transport blockade may be effective against SPRY2-deficient CRPC.

2016-04-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration

4区 · 医学

Article

作者: Parham, Janet ; Zhou, Huiqiang ; Generaux, Claudia ; Rimele, Thomas ; Moncol, David ; Sparks, Steven M ; Harston, Lindsey ; Jayawickreme, Channa ; Condreay, Patrick

The identification of a low-permeability scavenger receptor BI (SR-BI) inhibitor starting from the ITX-5061 template is described. Structure-activity and structure-permeability relationships were assessed for analogs leading to the identification of compound 8 as a potent and nonabsorbable SR-BI inhibitor.

100 项与 ITX-5061 相关的药物交易

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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
丙型肝炎	临床2期	美国	iTherX Pharmaceuticals, Inc.	2015-01-05

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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


NCT01292824 (Pubmed \| Liver Transpl)	临床1期	丙型肝炎	23	Control group	壓獵壓願鬱夢簾膚遞齋(糧鏇醖醖艱窪鬱夢鏇構) = treatment was associated with a sustained reduction in HCV RNA levels compared to the control group 獵餘築衊製壓廠鹽範壓 (鬱淵餘積獵鑰壓餘壓遞 )	-	2016-03-01
NCT01292824 (Pubmed \| Liver Transpl)	临床1期	丙型肝炎	23	ITX5061 150mg		-	2016-03-01
NCT01560468 (Pubmed \| J Infect Dis)	临床1期	丙型肝炎	-	ITX5061	齋選網鏇齋廠衊鹹蓋範(願餘願鏇膚廠遞餘網鏇) = 鏇夢範襯齋鏇廠淵衊餘壓繭遞壓願網餘選繭醖 (簾膚積遞構鹹艱繭淵鑰 )	-	2014-03-01