Angioscopic evaluation of coronary atherosclerotic plaque after revascularization with drug-eluting stent - Intervention trial with statins and cholesterol absorption inhibitors - - The ANTARES Trial

开始日期2013-01-10

申办/合作机构

Nippon Medical School

100 项与 TEI-M01361 相关的临床结果

登录后查看更多信息

100 项与 TEI-M01361 相关的转化医学

登录后查看更多信息

100 项与 TEI-M01361 相关的专利（医药）

登录后查看更多信息

204

项与 TEI-M01361 相关的文献（医药）

2026-02-01·BRAIN RESEARCH

Ezetimibe mitigates microglial activation in Parkinson’s disease via TLR4/JNK pathway inhibition: evidence from network pharmacology and experimental validation

Article

作者: Huang, Xin-Yue ; Zhou, Zeng-Hui ; Hua, You-Hai ; Ma, Jing-Jing ; Wu, Jin

OBJECTIVE:

Neuroinflammation driven by microglial hyperactivation plays a critical role in Parkinson's disease (PD). Ezetimibe, a cholesterol absorption inhibitor widely used for hyperlipidemia, has recently been implicated in neuroprotection. However, its impact on microglial activation in PD remains poorly understood. This study aimed to investigate the therapeutic potential and mechanisms of ezetimibe in modulating microglial activation in PD model.

METHODS:

Network pharmacology was employed to predict ezetimibe targets in PD, followed by validation in lipopolysaccharide (LPS)-stimulated BV2 microglial cells. Protein-protein interaction (PPI) analysis and Gene Ontology (GO) enrichment were used to identify relevant pathways. Molecular docking assessed ezetimibe-TLR4 binding. The effects of ezetimibe on pro-inflammatory mediator production, TLR4/JNK signaling, and microglia-induced dopaminergic neurotoxicity were evaluated using western blotting, qPCR, ELISA, and BV2-SH-SY5Y co-culture assays.

RESULTS:

Network pharmacology identified 53 common targets between ezetimibe and PD, with TLR4, TNF, and IL-1β as hub genes enriched in inflammatory processes. In BV2 cells, ezetimibe markedly reduced LPS-induced expression and secretion of iNOS, COX-2, Nitric oxide (NO), and IL-6 at both protein and transcriptional levels. Molecular docking revealed a strong binding affinity of ezetimibe to TLR4, although ezetimibe did not alter the basal expression of TLR4. Mechanistically, ezetimibe pretreatment suppressed LPS-induced JNK phosphorylation and AP-1 transcriptional activity, key downstream events of TLR4 activation. Consistently, pharmacological inhibition of TLR4 with TLR4-IN-C34 did not produce additional anti-inflammatory effects, confirming that ezetimibe acts through the TLR4 signaling pathway. Moreover, conditioned medium from ezetimibe-pretreated BV2 cells significantly reduced SH-SY5Y neuronal death, as indicated by decreased PI staining, LDH release, CCK8 assay, tyrosine hydroxylase (TH) protein levels and caspase-3 activation.

CONCLUSION:

Ezetimibe suppresses microglial activation by targeting the TLR4/JNK pathway, thereby alleviating dopaminergic neuronal death. These findings highlight ezetimibe as a promising candidate for repurposing in PD therapy.

2026-01-01·Clinical Pharmacology in Drug Development

Pharmacokinetic Interaction Between Atorvastatin and Hybutimibe in Healthy Chinese Volunteers

Article

作者: Cui, Xiao‐feng ; Chen, Wen‐jun ; Yang, Dan‐dan ; Wang, Jia‐ying ; Ruan, Zou‐rong ; Shao, Rong ; Lou, Hong‐gang ; Zhang, Xue‐hua ; Jiang, Bo ; Du, Jia‐qiu

Abstract:

Stains and cholesterol absorption inhibitors are frequently co‐administered in the management of dyslipidemia. This study evaluated the pharmacokinetic (PK) interaction between atorvastatin and hybutimibe in healthy Chinese subjects. A randomized, open‐label, three‐treatment, six‐period crossover study was conducted involving 24 participants. Subjects received once‐daily treatments for 14 days per period (14‐day washout): atorvastatin 20 mg, hybutimibe 10 mg, or their combination. Geometric mean ratios (GMRs) and their 90% confidence intervals (CI) were calculated for the maximum plasma concentration (C max ) and the area under the plasma concentration–time curve (AUC) of atorvastatin, hybutimibe, and their metabolites, comparing combination therapy with monotherapy. At steady state, the GMRs (90% CI) for atorvastatin were 89.9 (74.6, 108.2) for C max and 103.7 (96.0, 112.0) for AUC 0‐∞ when administered with or without hybutimibe. For total hybutimibe, the corresponding values were 120.6 (102.4, 142.0) and 105.7 (97.1, 115.2), respectively. Considering the limited PK changes and good safety profiles of both drugs, the interaction between atorvastatin and hybutimibe will likely have no significant clinical impact.

2025-12-31·ANNALS OF MEDICINE

Ezetimibe and the risk of new-onset type 2 diabetes: a systematic review and meta-analysis

Review

作者: Albawa’neh, Areej S. ; Ahmed, Gamila ; Ali, Bassam R. ; Alqasrawi, Mais N. ; Al-Mahayri, Zeina N. ; Albawaana, Amal ; Al-Rifai, Rami H.

BACKGROUND:

Statins reduce cardiovascular risk but may increase new-onset type 2 diabetes mellitus (NO-T2DM). Ezetimibe, a cholesterol absorption inhibitor, is often added to statins to improve lipid control, yet its impact on NO-T2DM remains uncertain.

OBJECTIVE:

This systematic review evaluated moderate-intensity statin plus ezetimibe dual therapy versus high-intensity statin monotherapy for NO-T2DM risk.

METHODS:

Five databases were searched to identify eligible studies. Random-effects meta-analyses generated pooled relative risks (RR) quantifying the effect of ezetimibe plus moderate-intensity statins on NO-T2DM. The Attributable Risk Fraction (ARF) was quantified utilizing the pooled estimate.

RESULTS:

Ten observational studies and four clinical trials were included. In four cohort studies, ezetimibe plus moderate-intensity statin compared to high-intensity statin monotherapy was significantly linked to 18% reduced risk of NO-T2DM (pooled RR: 0.82; 95% CI: 0.77-0.87; I2 = 0.0%; p < 0.001). In three methodologically similar studies, compared to moderate-intensity statin monotherapy, adding ezetimibe to moderate-intensity statin dual therapy showed non-statistically (p > 0.05) significant 4% increased risk of NO-T2DM development (pooled RR: 1.04; 95% CI: 0.94-1.14, I2= 0.0%). Compared with patients receiving high-intensity statin therapy, 22% of NO-T2DM cases could potentially be averted with dual therapy (moderate-intensity statin plus ezetimibe). In four studies involving 5,072 patients on high-intensity statins who developed NO-T2DM, 1,115 patients (812-1,420) could have been prevented with ezetimibe plus moderate-intensity statin dual therapy.

CONCLUSION:

Incorporating ezetimibe with moderate-intensity statins, rather than relying solely on high-intensity statins, may reduce the risk of NO-T2DM in patients with dyslipidemia and elevated cardiovascular disease risk.

PROSPERO REGISTRATION NUMBER:

CRD42024518630.

项与 TEI-M01361 相关的新闻（医药）

2024-07-31

·drugs

Can Non-Statin Cholesterol Meds Help Your Liver?

WEDNESDAY, July 31, 2024 -- Prior studies have found that statin meds can help lower liver cancer risks, and new research suggests that at least one non-statin cholesterol drug can do the same. A team led by Katherine McGlynn of the U.S. National Cancer Institute looked at the health histories of almost 19,000 people tracked by the U.K.'s Clinical Practice Research Datalink. About 3,700 of them developed liver cancer, and their medication use was compared to almost 15,000 others who did not get the disease. McGlynn's team linked use of a non-statin form of cholesterol-lowering meds, called cholesterol absorption inhibitors, to 31% lower odds of developing liver cancer. Their findings were reported July 29 in the journal Cancer . The link held when the researchers accounted for other risk factors such as diabetes and liver disease status. The study also re-confirmed that statins lower liver cancer risk by 35%. But the use of three other medicines used to lower cholesterol -- fibrates, omega-3 fatty acids and niacin -- did not seem to affect liver cancer risk, the research showed. Risks attributed to another drug type, bile acid sequestrants, were inconclusive. “As few studies have examined the effects of non-statin cholesterol-lowering drugs on liver cancer risk, the results of our study require replication in other populations," McGlynn said in a journal news release. "If our findings are confirmed in other studies, however, our results may inform liver cancer prevention research." Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

2024-07-31

·drugs

Cholesterol Absorption Inhibitors May Cut Risk for Liver Cancer

WEDNESDAY, July 31, 2024 -- The use of cholesterol absorption inhibitors is associated with a reduced risk for liver cancer, according to a study published online July 29 in Cancer . Shahriar A. Zamani, Ph.D., from the National Cancer Institute at the National Institutes of Health in Rockville, Maryland, and colleagues examined the risk for liver cancer for five nonstatin cholesterol-lowering medications (cholesterol absorption inhibitors, bile acid sequestrants, fibrates, niacin, and omega-3 fatty acids). The analysis included 3,719 cases and 14,876 matched controls. The researchers found that cholesterol absorption inhibitor use was associated with reduced liver cancer risk in the overall analysis (odds ratio, 0.69) and when considering type 2 diabetes and chronic liver disease status. Overall, bile acid sequestrant use was associated with increased liver cancer risk (odds ratio, 5.31), but findings were inconsistent when considering type 2 diabetes and chronic liver disease status. There were no associations seen for the other medications and liver cancer risk. "In conclusion, the current results suggest that use of cholesterol absorption inhibitors may be associated with reduced risk of liver cancer," the authors write. "Future studies are needed to confirm the results of this study and to clarify the association of all nonstatin cholesterol-lowering medications and liver cancer." Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果

2021-08-27

·BioSpace

Antihyperlipidemic Drugs Market to Garner $16.86 Billion by 2026 at 7.5% CAGR

Presence of rules suggesting the utilization of statins, ascend in pervasiveness of hyperlipidemia across the globe, and flood in medical services use have helped the worldwide antihyperlipidemic drug market. Allied Market Research as of late distributed a report, named, "Antihyperlipidemic Drugs Market by Drug Class (Statins, PCSK9 Inhibitors, Bile Acid Sequestrants, Cholesterol Absorption Inhibitors, Fibric Acid Derivatives, and Combination): Global Opportunity Analysis and Industry Forecast, 2019–2026". As indicated by the report, the worldwide antihyperlipidemic drug industry was fixed at $9.46 billion of every 2019 and is projected to reach $16.86 billion by 2026, enrolling a CAGR of 7.5% from 2019 to 2026. Motivating forces for market development Presence of rules suggesting the utilization of statins, ascend in pervasiveness of hyperlipidemia across the globe, and flood in medical services use have helped the worldwide antihyperlipidemic drug market. Nonetheless, impending patent lapse of medications hampers the market development. In actuality, high development potential in creating economies is relied upon to set out rewarding open doors soon. Request Sample Report at: Statins portion overwhelmed the market The statins portion held the biggest offer in 2018, adding to almost two-fifths of the market, inferable from flood in the occurrence of cardiovascular problems and its capacity to lessen the danger related with respiratory failures. Notwithstanding, the PCSK9 inhibitors section is projected to enroll the quickest CAGR of 9.7% during the figure time frame, inferable from benefits offered, for example, radical decrease of LDL levels in the blood. North America area held the biggest offer The market across North America held the biggest offer in 2018, represented almost 33% of the market, owing simple accessibility of the antihyperlipidemic drugs and stationary way of life in the area. Unexpectedly, Asia-Pacific district is relied upon to enroll the quickest CAGR of 8.6% from 2019 to 2026, attributable to flood in mindfulness identified with the utilization of antihyperlipidemic medications and flood in the medical care consumption. Major market player Boehringer Ingelheim GmbH Merck KGaA Johnson and Johnson Bayer AG Pfizer, Inc. Takeda Pharmaceutical Co., Ltd. AstraZeneca plc Daiichi Sankyo Company Sanofi S.A. Novartis International AG We have also published few syndicated market studies in the other trending area that might be of your interest. Below are the report title for your reference, considering Impact of Covid-19 over This Market which will help you to assess aftereffects of pandemic on short-term and long-term growth trends of this market. Trending Reports: High Tibial Osteotomy (HTO) Plates Market: Global Opportunity Analysis and Industry Forecast, 2019–2026 Predictive Analytics in Healthcare Market: Global Opportunity Analysis and Industry Forecast, 2018 - 2025 About Us Allied Market Research (AMR) is a full-service market research and business-consulting wing of Allied Analytics LLP based in Portland, Oregon. Allied Market Research provides global enterprises as well as medium and small businesses with unmatched quality of "Market Research Reports" and "Business Intelligence Solutions." AMR has a targeted view to provide business insights and consulting to assist its clients to make strategic business decisions and achieve sustainable growth in their respective market domain. We are in professional corporate relations with various companies and this helps us in digging out market data that helps us generate accurate research data tables and confirms utmost accuracy in our market forecasting. Each and every data presented in the reports published by us is extracted through primary interviews with top officials from leading companies of domain concerned. Our secondary data procurement methodology includes deep online and offline research and discussion with knowledgeable professionals and analysts in the industry. Contact: David Correa 5933 NE Win Sivers Drive #205, Portland, OR 97220 United States USA/Canada (Toll Free): +1-800-792-5285, +1-503-894-6022 UK: +44-845-528-1300 Hong Kong: +852-301-84916 India (Pune): +91-20-66346060 Fax: +1(855)550-5975 help@alliedmarketresearch (dot) com

100 项与 TEI-M01361 相关的药物交易

登录后查看更多信息