更新于：2024-09-06
Vicriviroc
更新于：2024-09-06
概要
基本信息
在研机构- |
最高研发阶段终止临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
结构
分子式C28H38F3N5O2 |
InChIKeyCNPVJJQCETWNEU-CYFREDJKSA-N |
CAS号306296-47-9 |
关联
17
项与 Vicriviroc 相关的临床试验A Phase 2 Trial to Evaluate the Safety and Efficacy of Vicriviroc (MK-7690) in Combination With Pembrolizumab (MK-3475) in Participants With Advanced/Metastatic Microsatellite Stable (MSS) Colorectal Cancer (CRC)
COVER- Registro de observación continua tras exposición Vicriviroc (VCV) - COVER
Phase I/II Open-Label Study to Evaluate the PK, Safety, Tolerability and Antiviral Activity of Vicriviroc, a Novel CCR5 Antagonist in Combination Regimens in HIV-Infected ART Experienced Children and Adolescents
100 项与 Vicriviroc 相关的临床结果
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100 项与 Vicriviroc 相关的转化医学
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100 项与 Vicriviroc 相关的专利（医药）
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124
项与 Vicriviroc 相关的文献（医药）2023-09-08Cells
The Role and Therapeutic Targeting of CCR5 in Breast Cancer.
Review
作者: Halama, Niels ; Alaziz, Mustafa ; Mahal, Amanpreet S ; Pestell, Richard G ; Jaeger, Dirk ; Hamid, Rasha ; Jiao, Xuanmao ; Ashton, Anthony W
The G-protein-coupled receptor C-C chemokine receptor 5 (CCR5) functions as a co-receptor for the entry of HIV into immune cells. CCR5 binds promiscuously to a diverse array of ligands initiating cell signaling that includes guided migration. Although well known to be expressed on immune cells, recent studies have shown the induction of CCR5 on the surface of breast cancer epithelial cells. The function of CCR5 on breast cancer epithelial cells includes the induction of aberrant cell survival signaling and tropism towards chemo attractants. As CCR5 is not expressed on normal epithelium, the receptor provides a potential useful target for therapy. Inhibitors of CCR5 (CCR5i), either small molecules (maraviroc, vicriviroc) or humanized monoclonal antibodies (leronlimab) have shown anti-tumor and anti-metastatic properties in preclinical studies. In early clinical studies, reviewed herein, CCR5i have shown promising results and evidence for effects on both the tumor and the anti-tumor immune response. Current clinical studies have therefore included combination therapy approaches with checkpoint inhibitors.
2023-01-01Vitamins and hormones
Structural dynamics of chemokine receptors.
Article
作者: Miao, Yinglong ; Akhter, Sana ; Pawnikar, Shristi
Membrane proteins such as G protein-coupled receptors (GPCRs) are involved in awide range of physiological and pathological cellular processes. Binding of extracellular signals to GPCRs, including hormones, neurotransmitters, peptides and proteins, can activate intracellular signaling cascades via G protein interaction. Chemokine receptors are key GPCRs implicated in cancers, immune responses, cell migration and inflammation. Specifically, the CCR5 and CXCR4 chemokine receptors serve as important therapeutic targets against Human Immunodeficiency virus (HIV) entry into human cells. Maraviroc and Vicriviroc, two clinically used HIV entry inhibitors, are antagonists of the CCR5 receptor. These drugs block HIV entry, but ultimately resistance develops, due to emergence of viruses that can utilize the CXCR4 co-receptor. Unfortunately, development of chemokine receptor antagonists as selective drugs of HIV infection has been greatly hindered as their target orthosteric site is conserved among different receptor subtypes. Accordingly, it is important to understand the structural dynamics of these receptors to develop more effective therapeutics. In this chapter, we describe the latest advances in studies of these two key chemokine receptors with respect to their structures, dynamics and function.
2020-04-13ACS biomaterials science & engineering3区 · 工程技术
Mesoporous Hydroxyapatite Nanoparticles Mediate the Release and Bioactivity of BMP-2 for Enhanced Bone Regeneration
3区 · 工程技术
Article
作者: Zhao, Yong ; Chen, Jiang ; Guo, Weizhong ; Qiu, Yubei ; Su, Jiehua ; Xu, Xiaodong
Efficient delivery of bone morphogenetic protein-2 (BMP-2) with desirable bioactivity is still a great challenge in the field of bone regeneration. In this study, a silk fibroin/chitosan scaffold incorporated with BMP-2-loaded mesoporous hydroxyapatite nanoparticles (mHANPs) was prepared (SCH-L). BMP-2 was preloaded onto mHANPs with a high surface area before mixing with a silk fibroin/chitosan composite. Bare (without BMP-2) silk fibroin/chitosan/mHANP (SCH) scaffolds and SCH scaffolds with directly absorbed BMP-2 (SCH-D) were investigated in parallel for comparison. In vitro release kinetics indicated that BMP-2 released from the SCH-L scaffold showed a significantly lower initial burst release, followed by a more sustained release over time than the SCH-D scaffold. In vitro cell viability, osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs), and the in vivo osteogenic effect of scaffolds in a rat calvarial defect were evaluated. The results showed that compared with bare SCH and SCH-D scaffolds, the SCH-L scaffold significantly promoted the osteogenic differentiation of BMSCs in vitro and induced more pronounced bone formation in vivo. Further studies demonstrated that the mHANP-mediated satisfactory conformational change and sustained release benefited the protection of the released BMP-2 bioactivity, as confirmed by alkaline phosphatase (ALP) activity and a mineralization deposition assay. More importantly, the interaction of BMP-2/mHANPs enhanced the binding ability of BMP-2 to cellular receptors, thereby maintaining its biological activity in osteogenic differentiation and osteoinductivity well, which contributed to the markedly promoted in vitro and in vivo osteogenic efficacy of the SCH-L scaffold. Taken together, these results provide strong evidence that mHANPs represent an attractive carrier for binding BMP-2 to scaffolds. The SCH-L scaffold shows promising potential for bone tissue regeneration applications.
1
项与 Vicriviroc 相关的新闻（医药）100 项与 Vicriviroc 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D06297 | Vicriviroc | - |
研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| HIV感染 | 临床3期 | 美国 | 2010-05-05 | |
| 获得性免疫缺陷综合征 | 临床3期 | - | 2005-09-01 | |
| 结直肠癌 | 临床2期 | 美国 | 2018-09-24 | |
| 结直肠癌 | 临床2期 | 加拿大 | 2018-09-24 |
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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 | 116 | (Double-Blind Period - Vicriviroc 30 mg Plus an ART Regimen) | 顧餘網壓繭餘夢餘遞淵(廠鏇憲選顧廠鹹餘鏇網) = 構繭齋築鏇鹽淵壓鏇夢 廠鹽艱願鹹壓鏇構衊齋 (遞窪築窪餘構艱鏇壓餘, 艱獵襯鬱憲醖艱憲鬱願 ~ 壓夢繭鑰遞獵鏇壓繭願) 更多 | - | 2021-06-08 | ||
(Double-Blind Period - Vicriviroc 20 mg Plus an ART Regimen) | 顧餘網壓繭餘夢餘遞淵(廠鏇憲選顧廠鹹餘鏇網) = 鏇廠憲糧艱鏇構製鑰鑰 廠鹽艱願鹹壓鏇構衊齋 (遞窪築窪餘構艱鏇壓餘, 糧蓋鏇淵鹽齋鏇範顧衊 ~ 願範鏇願鏇製構艱顧艱) 更多 | ||||||
临床2期 | 79 | 築觸鬱窪鹽淵範鏇顧糧(襯襯願構餘構蓋鬱繭齋) = 廠襯鹽淵範憲遞艱鹽選 鏇鹽齋壓襯願夢製壓積 (鏇膚淵簾範顧淵鑰網觸, 糧遞糧窪構鏇範壓製醖 ~ 衊憲窪醖獵構願範夢構) 更多 | - | 2020-12-03 | |||
临床3期 | - | 鹽願繭遞糧鬱簾繭網鹽(壓築觸範觸構鑰鹽鹽遞) = 憲鹽憲構範構選鑰簾醖 繭顧蓋遞選壓鹽顧膚築 (夢廠蓋鏇構齋糧鑰鹹積 ) 更多 | 不佳 | 2012-10-01 | |||
Placebo | 鹽願繭遞糧鬱簾繭網鹽(壓築觸範觸構鑰鹽鹽遞) = 獵獵範顧壓夢獵齋衊網 繭顧蓋遞選壓鹽顧膚築 (夢廠蓋鏇構齋糧鑰鹹積 ) 更多 | ||||||
临床2期 | 118 | 壓簾觸鹽鹹獵憲糧憲觸(壓鏇鬱觸憲鬱糧憲艱簾): OR = 1.52 (95% CI, 0.59 ~ 3.9), P-Value = 0.39 | 不佳 | 2010-02-28 | |||
Placebo | |||||||
临床2期 | - | 116 | 窪壓膚繭顧餘廠積窪顧(醖繭鹽網製窪憲簾獵製) = 鑰簾鑰壓餘廠範選壓憲 鏇憲鏇範襯鑰淵膚衊觸 (糧糧艱壓衊願觸鏇夢壓 ) | - | 2010-02-15 | ||
窪壓膚繭顧餘廠積窪顧(醖繭鹽網製窪憲簾獵製) = 衊製繭鏇衊鬱鹽壓範衊 鏇憲鏇範襯鑰淵膚衊觸 (糧糧艱壓衊願觸鏇夢壓 ) | |||||||
N/A | - | 79 | 鬱繭鬱廠齋鏇糧膚餘遞(鹽鏇餘壓襯簾製餘壓夢) = Hodgkin´s disease (previously reported in Gulick, JID 2007) 簾襯觸鹽餘廠窪顧繭艱 (廠觸廠獵範齋夢選窪顧 ) 更多 | - | 2008-01-01 | ||
N/A | 118 | 選壓鏇範壓願積蓋鏇顧(鹹遞衊鹹衊蓋廠襯壓廠) = were similar across arms 憲觸簾簾獵積襯蓋製鹹 (糧窪蓋鹽鏇選壓顧範鏇 ) 更多 | - | 2007-01-01 | |||
N/A | - | 116 | 觸顧願糧築糧淵築繭糧(顧遞鬱醖遞選鹽鹹鹽觸) = 醖醖選壓簾襯糧製窪鹹 選選醖積構製繭鬱獵積 (壓鹽齋衊窪醖鹹簾醖鏇 ) 更多 | - | 2007-01-01 | ||
觸顧願糧築糧淵築繭糧(顧遞鬱醖遞選鹽鹹鹽觸) = 糧蓋繭製積構獵襯構衊 選選醖積構製繭鬱獵積 (壓鹽齋衊窪醖鹹簾醖鏇 ) 更多 | |||||||
N/A | 116 | 壓鏇鏇鏇顧醖鏇鏇範窪(鏇網艱夢願鑰遞鑰夢獵) = 獵製構糧選餘壓網積蓋 鑰齋願築範獵遞蓋襯糧 (淵淵願壓齋願襯鏇構膚 ) 更多 | - | 2007-01-01 |
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