若生智能
Drug Database
EZ

ezetimibe + rosuvastatin (NVP1205 / NVP 1205)

✓ Approved

NVP Healthcare · HMGCR · 小分子

什么是 ezetimibe + rosuvastatin？

ezetimibe + rosuvastatin 是一种小分子，由NVP Healthcare研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名NVP1205, NVP 1205
公司NVP Healthcare
药物类别小分子
分子靶点HMGCR, NPC1L1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, NVP Healthcare

作用机制

分子靶点

ezetimibe + rosuvastatin 作用于 2 个分子靶点：

HMGCR3-hydroxy-3-methylglutaryl-CoA reductase (LDLCQ3, LGMDR28)
NPC1L1NPC1 like intracellular cholesterol transporter 1 (SLC65A2, LDLCQ7)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

ezetimibe + rosuvastatin 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Metabolism and nutrition disordersHyperlipidaemia✓ Approved

相关研究文献

PubMedAmerican heart journal plus : cardiology research and practice2026-08-09

Real-world long-term outcomes of clopidogrel-based dual antiplatelet therapy post-drug-eluting stent implantation in all comers patients: A retrospective evaluation.

Parikh Rohan R, Langade Jayshree J, Langade Deepak D

The objective of this study was to describe the real-world clinical outcomes among patients receiving clopidogrel-based dual antiplatelet therapy following PCI with drug-eluting stents. This was a retrospective study. Outcomes were assessed by clopidogrel-aspirin DAPT, lipid-lowering therapy, and stent type. Tertiary care cardiology centre in India to evaluate real-world outcomes following PCI with drug-eluting stents (DES) in all patients. The study included 1039 PCI-DES patients. Clopidogrel-aspirin DAPT. Analyses covered event rates, DAPT duration, repeat interventions, and LVEF. Subgroups were compared by age, sex, infarct type, stent type, and LDL-C targets. Of 1039 patients, 712 had STEMI and 327 had other cardiac conditions. A total of 1349 DES were implanted, mostly sirolimus stents (63.7%). Clopidogrel-based DAPT was very safe, with a MACE rate of 0.29%, slightly higher in older patients (≥55 years), those with ≥4 stents, and those with reduced/unimproved LVEF. Rosuvastatin monotherapy achieved LDL-C < 100 mg/dL with minimal events. Stent type did not affect outcomes, with low repeat interventions (3.4% same vessel, 3.1% other vessels). Clopidogrel with rosuvastatin was safe, effective, and consistent post-PCI, with low events and outcomes independent of stent type.

PMID 42571214
阅读全文 →
PubMedJournal of clinical lipidology2026-08-08

Comparative efficacy of different statin intensities combined with ezetimibe on lipid profile improvement in patients with coronary heart disease: A network meta-analysis.

Niu Qingsheng Q, Yao Peng P, Gan Lu L, Wang Ling L et al.

Despite statin medication, a substantial number of patients with coronary heart disease (CHD) do not meet guideline-recommended lipid goals, increasing dependence on combination lipid-lowering methods. However, evidence comparing the lipid-modifying effectiveness of ezetimibe added to statins of varying intensities is lacking, creating confusion about the best treatment options in clinical practice. This research sought to assess and compare the effectiveness of statins of varying intensities in conjunction with ezetimibe for enhancing lipid profiles in individuals with CHD. PubMed, Embase, Cochrane Library, and Web of Science were searched to January 1, 2026 for randomized controlled trials (RCTs) comparing statin monotherapy with statin-ezetimibe therapy in CHD. Network meta-analysis was performed using Stata 17.0, with surface under the cumulative ranking curve-based ranking. Outcomes were low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), triglycerides (TG), total cholesterol (TC), non-HDL-C, and apolipoprotein B (ApoB). A total of 38 RCTs involving 7340 patients with CHD were included. Network meta-analyses demonstrated that moderate-intensity statin (MIS) therapy coupled with ezetimibe regularly resulted in significant enhancements in LDL-C, HDL-C, TC, non-HDL-C, and ApoB levels. For LDL-C reduction, MIS plus ezetimibe was comparable in efficacy to a high-intensity statin (HIS) plus ezetimibe. For TG, HIS combined with ezetimibe was rated highest, while no significant change was noted in comparison to MIS combined with ezetimibe. Rosuvastatin plus ezetimibe may demonstrate the greatest efficacy among MIS-based combination regimens. Adding ezetimibe to MIS medication in patients with CHD provides a more balanced cholesterol-lowering strategy than statin dosage increase alone, with effectiveness equivalent to HIS-based treatment across several lipid measures.

PMID 42567788
阅读全文 →
PubMedJACC. Advances2026-08-08

Opportunistic Genetic Testing for Familial Hypercholesterolemia in Premature Acute Coronary Syndrome: Results of the ACCURATE Study.

Vaizman Nicol N, Cermakova Lubomira L, Cooper Matthew M, Kramer Adam I AI et al.

Familial hypercholesterolemia (FH) is common among patients with premature acute coronary syndrome (ACS) but remains underdiagnosed and undertreated. The ACCURATE (Advancing Cardiac Care Unit-based Rapid Assessment and Treatment of hypErcholesterolemia) study evaluated whether opportunistic genetic testing in patients with premature ACS increases FH diagnosis and lipid-lowering therapy use. ACCURATE was a nonrandomized, prospective study that recruited 2 sequential cohorts of patients. In phase 1, patients were treated according to usual standard of care, with no genetic testing. In phase 2, patients underwent FH genetic testing with results returned to treating physicians. Eligible patients were <60 years old admitted with ACS and had low-density lipoprotein cholesterol (LDL-C) ≥4 mmol/L (≥155 mg/dL). The primary endpoint was a new diagnosis of definite FH at 15 months post-ACS. Secondary endpoints were changes in lipid-lowering therapy and lipid levels. Overall, 40 patients in phase 1 and 100 patients in phase 2 completed the study, with similar baseline characteristics. A diagnosis of definite FH at follow-up occurred in 10% of patients in phase 2 vs 0% in phase 1. At 15 months, patients in phase 2 were more likely to achieve an LDL-C <1.8 mmol/L (73% vs 53%, P = 0.04), had lower mean LDL-C (1.65 mmol/L vs 1.93 mmol/L [64 mg/dL vs 75 mg/dL]) (P = 0.03), and were more likely to be receiving statin therapy (95% vs 83%, P = 0.04) or statin-ezetimibe combination therapy (52% vs 30%, P = 0.02). Opportunistic genetic testing of young adults with ACS was associated with increased FH diagnosis, more intensive lipid-lowering treatment, and improved lipid target attainment. (Advancing Cardiac Care Unit-based Rapid Assessment and Treatment of hypErcholesterolemia [ACCURATE]; NCT05218005).

PMID 42567095
阅读全文 →
PubMedJournal of molecular graphics & modelling2026-08-07

Dual-site TAS2R14 binding by (-)-epicatechin gallate: A computational framework for neuroprotective drug repurposing.

Sultana Armin A, Das Raju R, Woo JooHan J

Bitter taste receptors, particularly TAS2R14, are widely expressed in extraoral tissues, including the central nervous system, where they have been implicated in neuroinflammatory and neurodegenerative processes. Although numerous pharmacological and natural compounds have demonstrated therapeutic potential against neurodegenerative disorders, clinically effective disease-modifying therapies remain strikingly limited. TAS2R14 is a promising yet underexplored candidate target; however, its mechanistic role in neurodegenerative disorders remains poorly understood. Here, we conducted a structure-based virtual screening of 4138 FDA-approved drugs from the MedChemExpress database to identify potential TAS2R14 ligands for therapeutic repositioning. Top candidates were prioritized through a hierarchical molecular docking workflow and binding free-energy calculations (MM-GBSA), orthogonal GNINA validation, in silico ADMET assessment, followed by 500 ns molecular dynamics (MD) simulations to evaluate the persistence of predicted binding modes and ligand-associated conformational behavior at both extracellular and intracellular binding sites. The selected hits exhibited distinct predicted interaction profiles and conformational dynamics at the two independent binding sites. Among them, (-)-epicatechin gallate exhibited favorable interactions, persistent contact with key binding site residues, and comparatively limited conformational fluctuations at both sites, supporting its prioritization as a potential dual-site TAS2R14 binder. Furthermore, fexofenadine and ezetimibe showed favorable binding stability at the extracellular and intracellular sites, respectively. Hydrogen-bond analysis, principal component analysis, dynamic cross-correlation matrix analysis, and free-energy landscape mapping further revealed ligand-dependent differences in interaction networks and receptor conformational behavior. Notably, (-)-epicatechin gallate, fexofenadine, and ezetimibe exhibited greater predicted binding stability than the reference ligands flufenamic acid, cholesterol, and Comp28.1 throughout the 500 ns simulations. As this study is purely computational, experimental validation through receptor activation assays and relevant biological models will be required to determine whether the predicted binding interaction translates into functional modulation of TAS2R14 and therapeutic benefit. Nevertheless, these findings provide a computational foundation for prioritizing candidate TAS2R14 ligands and support future experimental studies to evaluate receptor activation, specificity, selectivity, and therapeutic efficacy, particularly for (-)-epicatechin gallate, in the context of TAS2R14-targeted neuroprotective drug repositioning.

PMID 42561603
阅读全文 →
PubMedFrontiers in cardiovascular medicine2026-08-06

Ultra-early in-cath lab evolocumab achieves rapid lipid target attainment and lipid quality improvement in acute coronary syndrome: a real-world propensity score-matched study.

Jiang Yufeng Y, Lin Jie J, Ma Mingyu M, Jiang Mei M et al.

Current guidelines mandate stringent low-density lipoprotein cholesterol (LDL-C) control for patients with acute coronary syndrome (ACS). However, real-world evidence regarding the ultra-early, in-cath lab initiation of PCSK9 inhibitors and their impact on lipid quality-specifically the clearance of highly atherogenic small dense LDL (sdLDL)-remains scarce. This study aimed to evaluate the short-term efficacy and safety of this ultra-early evolocumab intervention strategy. This real-world, prospective observational cohort study categorized ACS patients into three treatment groups: statin monotherapy, statin plus ezetimibe, and statin plus evolocumab. Evolocumab was administered ultra-early in the catheterization laboratory immediately after angiographic confirmation. A rigorous propensity score matching (PSM) was conducted to balance baseline characteristics. Primary endpoints included the 4-week LDL-C target achievement rate (<1.4 mmol/L and ≥50% reduction). Secondary endpoints focused on sdLDL clearance and safety outcomes. From an initial screening pool of 665 patients, a rigorous PSM established a final core analysis cohort of 382 matched patients (127 in the statin monotherapy group, 127 in the ezetimibe group, and 128 in the evolocumab group). At 4 weeks, the evolocumab group demonstrated a substantially higher dual LDL-C target attainment rate compared to the ezetimibe group (66.4% vs. 33.1%, Statin + Evolocumab vs. Statin + Ezetimibe; P < 0.001). Additionally, the statin plus ezetimibe group showed significant improvement over statin monotherapy (33.1% vs. 8.7%, Statin + Ezetimibe vs. Statin Monotherapy; P < 0.001). Furthermore, evolocumab exhibited a profound superiority in the clearance of pathogenic sdLDL particles, achieving a median reduction rate of 69.08% vs. 48.07% in the ezetimibe group (Statin + Evolocumab vs. Statin + Ezetimibe; P < 0.001). Safety profiles were comparable across all groups, with no significant differences in overall adverse events (P = 0.171). The ultra-early, in-cath lab initiation of evolocumab in ACS patients drives rapid, large-scale LDL-C target attainment and demonstrates an absolute advantage in the marked reduction of highly atherogenic sdLDL particles. This deep reversal of the lipid burden provides robust real-world evidence supporting the forward-shifting of intensive lipid-lowering interventions in the acute phase of ACS. Chinese Clinical Trial Registry, ChiCTR2600118799.

PMID 42558689
阅读全文 →
PubMedRevista portuguesa de cardiologia : orgao oficial da Sociedade Portuguesa de Cardiologia = Portuguese journal of cardiology : an official journal of the Portuguese Society of Cardiology2026-08-06

Intensive lipid lowering therapy strategies in acute coronary syndrome patients in contemporary clinical practice - the benefit of the "strike early, strike strong" approach.

Andraz Sofia S, Pereira Joana Massa JM, Silva Tânia T, Hamann Lucas L et al.

Current guidelines recommend a stepwise, low-density lipoprotein cholesterol (LDL-C) guided lipid-lowering therapy (LLT) approach for patients after acute coronary syndrome (ACS). This study aimed to assess whether an early intensive "strike early, strike strong" strategy with upfront combination LLT improves LDL-C goal attainment. This single-center retrospective study included 211 consecutive ACS patients admitted between January and October 2020, with a median follow-up of six months. Metabolic profiles were assessed during hospitalization and at follow-up. Patients were grouped by follow-up LDL-C levels (<55 mg/dL and ≥55 mg/dL). Discharge medication, adherence, and LDL-C reduction were compared. A total of 211 patients were included in the analysis, with a mean age of 65±12 years and 74% were male. LDL-C on target (<55 mg/dL) was achieved in 36% of patients during median follow-up of six months. This group was more commonly medicated with a combination therapy [high intensity statin (HI-statin) plus ezetimibe] at discharge (46% vs 31%, p=0.040), had higher adherence rates (94% vs 81%, p<0.001) and had significantly greater LDL-C reduction (80±48 mg/dl vs 49±53 mg/dL, p<0.001). The combination therapy was the only independent predictor for LDL-C on target during follow-up (OR=2.054, 95% CI: 1.063-3.969, p=0.032). Low-density lipoprotein target attainment was suboptimal at median follow-up of six months. The LDL-C target group was associated with combination therapy with HI-statins plus ezetimibe upfront, better adherence and greater LDL-C reduction. These findings support the "strike early, strike strong" approach in very high-risk patients.

PMID 42556783
阅读全文 →

注册免费账户还可查看另外 9422 篇文献

免费注册查看全部文献 →

了解更多ezetimibe + rosuvastatin