IDX-184(IDX-184) - 药物靶点：NS5B polymerase_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

NS5B polymerase

作用方式

抑制剂

作用机制

NS5B polymerase抑制剂(丙型肝炎病毒NS5B RNA依赖的RNA聚合酶抑制剂)

治疗领域

感染消化系统疾病

在研适应症-

非在研适应症

慢性丙型肝炎基因型 1

原研机构

Merck Sharp & Dohme Corp.

在研机构-

非在研机构

Merck Sharp & Dohme Corp.

权益机构-

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C25H35N6O9PS

InChIKeyFGHMGRXAHIXTBM-TWFJNEQDSA-N

CAS号1036915-08-8

关联

6

项与 IDX-184 相关的临床试验

NCT01371604

/ Completed临床2期

A Randomized, Double-Blind Study to Evaluate the Safety and Antiviral Activity of IDX184 in Combination With Pegylated Interferon and Ribavirin for 12 Weeks in Treatment-Naïve Subjects With Genotype 1 Chronic Hepatitis C Infection

The purpose of this study is to assess the safety and antiviral activity of IDX184 in combination with pegylated interferon and ribavirin in treatment-naïve subjects with genotype 1 chronic hepatitis C virus (HCV) infection.

开始日期2011-07-01

申办/合作机构

Merck Sharp & Dohme Corp.

NCT01157104

/ Completed临床1期

A Phase I, Double-Blind, Multiple-Dose Study to Evaluate the Pharmacokinetic Drug-Drug Interaction Between IDX320 and IDX184 in Healthy Subjects

This study is designed to evaluate the potential for a pharmacokinetic (PK) drug-drug interaction between IDX320 and IDX184 and to assess the safety and tolerability when the two drugs are administered in combination in healthy participants.

开始日期2010-06-01

申办/合作机构

Merck Sharp & Dohme Corp.

NCT01011166

/ Completed临床2期

A Phase II, Randomized, Double-Blind Study to Evaluate the Safety and Antiviral Activity of IDX184 in Combination With Pegylated Interferon and Ribavirin in Subjects With Genotype 1 Chronic Hepatitis C Infection

This study will assess short term safety, antiviral activity and pharmacokinetics (PK) of IDX184 in combination with Peg-interferon (Peg-IFN)/Ribavirin (RBV) in participants with hepatitis C virus (HCV) genotype (GT) 1 infection. These data will guide dose selection for future, longer term studies.

开始日期2009-11-01

申办/合作机构

Merck Sharp & Dohme Corp.

100 项与 IDX-184 相关的临床结果

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100 项与 IDX-184 相关的转化医学

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100 项与 IDX-184 相关的专利（医药）

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36

项与 IDX-184 相关的文献（医药）

2023-12-21·Journal of Biomolecular Structure and Dynamics

Dynamics and binding affinity of nucleoside and non-nucleoside inhibitors with RdRp of SARS-CoV-2: a molecular screening, docking, and molecular dynamics simulation study

Article

作者: Chinnamadhu, Archana ; Poomani, Kumaradhas ; Suresh, Suganya ; Ramakrishnan, Jaganathan ; Ramadurai, Prakash

In this COVID-19 pandemic situation, an appropriate drug is urgent to fight against this infectious disease to save lives and prevent mortality. Repurposed drugs and vaccines are the immediate solutions for this medical emergency until discover a new drug to treat this disease. As of now, no specific drug is available to cure this disease completely. Several drug targets were identified in SARS-CoV-2, in which RdRp protein is one of the potential targets to inhibit this virus infection. In-Silico studies plays a vital role to understand the binding nature of the drugs at the atomic level against the disease targets. The present study explores the binding mechanism of reported 53 nucleoside and non-nucleoside RdRp inhibitors and Ivermectin which are in clinical trials. These molecules were screened by molecular docking simulation; in which, the molecules are showing high binding affinity and forming interactions with the key amino acids of active site of RdRp protein are chosen for molecular dynamics simulation (MD) and binding free energy analysis. The results of molecular docking and MD simulation studies reveal that IDX184 is a stable molecule and forms strong interactions with the key amino acids and shows high binding affinity towards RdRp. Hence, IDX184 may also be considered as a potential inhibitor of RdRp after clinical study.Communicated by Ramaswamy H. Sarma.

2022-09-22·Journal of Biomolecular Structure and Dynamics

In silico prediction of SARS-CoV-2 main protease and polymerase inhibitors: 3D-Pharmacophore modelling

Article

作者: Kobarfard, Farzad ; Hajiagha Bozorgi, Atefeh ; Rezaeianpour, Maliheh ; Mosayebnia, Mona

The outbreak of the second severe acute respiratory syndrome coronavirus (SARS-CoV-2) known as COVID-19 has caused global concern. No effective vaccine or treatment to control the virus has been approved yet. Social distancing and precautionary protocols are still the only way to prevent person-to-person transmission. We hope to identify anti-COVID-19 activity of the existing drugs to overcome this pandemic as soon as possible. The present study used HEX and AutoDock Vina softwares to predict the affinity of about 100 medicinal structures toward the active site of 3-chymotrypsin-like protease (3Clpro) and RNA-dependent RNA polymerase (RdRp), separately. Afterwards, MOE software and the pharmacophore-derived query methodology were employed to determine the pharmacophore model of their inhibitors. Tegobuvir (19) and compound 45 showed the best binding affinity toward RdRp and 3Clpro of SARS-CoV-2 in silico, respectively. Tegobuvir -previously applied for hepatitis C virus- formed highly stable complex with uncommon binding pocket of RdRp (E total: -707.91 Kcal/mol) in silico. In addition to compound 45, tipranavir (28) and atazanavir (26) as FDA-approved HIV protease inhibitors were tightly interacted with the active site of SARS-CoV-2 main protease as well. Based on pharmacophore modelling, a good structural pattern for potent candidates against SARS-CoV-2 main enzymes is suggested. Re-tasking or taking inspiration from the structures of tegobuvir and tipranavir can be a proper approach toward coping with the COVID-19 in the shortest possible time and at the lowest cost.Communicated by Ramaswamy H. Sarma.

2022-07-01·Future Microbiology3区 · 生物学

Dual Targeting of RdRps of SARS-CoV-2 and the Mucormycosis-Causing Fungus: An in silico Perspective

3区 · 生物学

Article

作者: Elfiky, Abdo A

During the past few months, mucormycosis has been associated with SARS-CoV-2 infections. Molecular docking combined with molecular dynamics simulation is utilized to test nucleotide-based inhibitors against the RdRps of SARS-CoV-2 solved structure and Rhizopus oryzae RdRp model built in silico. The results reveal a comparable binding affinity of sofosbuvir, galidesivir, ribavirin and remdesivir compared with the physiological nucleotide triphosphates against R. oryzae RdRp as well as the SARS-CoV-2 RdRp as reported before. Additionally, other compounds such as setrobuvir, YAK, IDX-184 and modified GTP compounds 2, 3 and 4 show potential calculated average binding affinities against R. oryzae RdRp. The present in silico study suggests the dual inhibition potential of the recommended drugs and compounds against SARS-CoV-2 and R. oryzae RdRps.

100 项与 IDX-184 相关的药物交易

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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
慢性丙型肝炎基因型 1	临床2期	-	Merck Sharp & Dohme Corp.	2009-11-01

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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


NCT01011166 (Pubmed \| Antivir Ther)	临床2期	慢性丙型肝炎	81	IDX184	選鹹顧鬱餘選廠醖鹹窪(夢觸積壓築鬱蓋遞鏇網) = Most adverse events were mild or moderate in severity and were consistent with those associated with P/R. The most common adverse events were fatigue and headache. 膚鏇繭蓋獵糧網範觸網 (簾窪衊繭繭鬱繭憲築遞 )	-	2013-01-01
NCT01011166 (Pubmed \| Antivir Ther)	临床2期	慢性丙型肝炎	81	Pegylated interferon-α2a and ribavirin		-	2013-01-01
Pubmed \| Antimicrob Agents Chemother	N/A	丙型肝炎	8	IDX184	簾積構夢夢鹽顧簾蓋餘(繭蓋築鹹齋壓網鑰齋窪) = 遞淵願淵繭淵餘積醖簾糧築襯衊蓋範蓋蓋鹽顧 (鹽繭憲觸積製夢願簾廠 ) 更多	-	2011-01-01