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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

PubMedJACC. Case reports2026-09-10

Early Coronary Atherosclerosis in Homozygous Familial Hypercholesterolemia: The Importance of Aggressive Lipid Lowering.

Zachariah Don D, Thomas Anjana A, Nkheli Lindinkululeko L, Mansfield Brett B et al.

Homozygous familial hypercholesterolemia (HoFH) causes severe lifelong low-density lipoprotein-cholesterol (LDL-C) elevation and accelerated atherosclerosis from childhood. A 10-year-old boy presented with extensive tuberous xanthomas and was diagnosed with HoFH due to bi-allelic pathogenic variants in the low-density lipoprotein receptor gene. Baseline LDL-C was 663 mg/dL (17.14 mmol/L). Treatment with atorvastatin, followed by rosuvastatin and ezetimibe, reduced LDL-C to 235 mg/dL (6.08 mmol/L) with marked regression of xanthomas. One year later, he developed exertional chest pain. Coronary angiography and intravascular ultrasound demonstrated early coronary atherosclerosis with a nonobstructive 28% stenosis of the right coronary artery. This case provides an opportunity to discuss the role and limitations of currently available lipid-lowering therapies in HoFH. We review current lipid-lowering therapies and the challenges of achieving LDL-C targets in patients with HoFH, particularly in resource-limited settings. Early recognition and aggressive LDL-C lowering are essential in HoFH to prevent atherosclerosis.

PMID 42720648
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PubMedJournal of clinical lipidology2026-09-09

Efficacy and diabetes risk of moderate-intensity statin plus ezetimibe versus high-intensity statin after percutaneous coronary intervention: A systematic review and meta-analysis.

Kelly Francinny Alves FA, Moreira Rêgo Luis Henrique Rios LHR, Rebelo Thiago Gorayeb TG, da Silva Raissa Martins RM et al.

Patients undergoing percutaneous coronary intervention (PCI) have a high cardiovascular risk. Current guidelines recommend a ≥50% low-density lipoprotein cholesterol (LDL-C) reduction from baseline. Notably, the recently published 2026 American College of Cardiology/American Heart Association/Multisociety Dyslipidemia Guideline continues to support >50% LDL-C reduction while reinstating specific LDL-C targets for very high-risk patients. Statins are widely used to achieve these goals; however, higher-intensity therapy has been associated with adverse effects, including new-onset diabetes mellitus through mechanisms that may include impaired insulin sensitivity, reduced insulin secretion, and altered adipokine signaling. The combination of ezetimibe with a moderate-intensity statin may offer an effective lipid-lowering strategy with fewer metabolic side effects. This meta-analysis aimed to compare the efficacy and risk of diabetes in patients receiving moderate-intensity statin plus ezetimibe vs high-intensity statin therapy after PCI. A systematic search was conducted in MEDLINE, Scopus, Cochrane Library, and Web of Science through July 18, 2025. Relative risks (RR) with 95% CIs were estimated using random-effects or fixed-effects models. Heterogeneity was assessed with the I² statistic. Analyses were performed in RStudio 4.4.2. Seven studies, including 121,480 patients, were analyzed. Of these, 26,228 (21.5%) received moderate-intensity statin plus ezetimibe, and 95,252 (78.4%) received high-intensity statins. The moderate-intensity group showed a lower risk of new-onset diabetes requiring medication (RR = 0.83; 95% CI: 0.76-0.91), and all-cause mortality favors moderate-intensity statin plus ezetimibe (RR: 0.89; 95% CI: 0.84-0.95). No significant differences were observed in major adverse cardiovascular events (RR: 0.99; 95% CI: 0.65-1.52) or revascularization (RR: 0.96; 95% CI: 0.83-1.12). This meta-analysis suggests that moderate-intensity statin therapy combined with ezetimibe provides cardiovascular protection equivalent to high-intensity statin therapy, while significantly reducing the risk of new-onset diabetes in patients undergoing PCI.

PMID 42716850
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PubMedArchives of disease in childhood2026-09-09

Paediatric familial hypercholesterolaemia in Australia: a real-world registry study.

Martin Andrew C AC, Srinivasan Shubha S, Justo Robert N RN, Waddell-Smith Kathryn E KE et al.

To describe the characteristics, detection and management of children and adolescents with familial hypercholesterolaemia (FH) enrolled in the Australian National FH Registry. Cross-sectional registry analysis. 17 specialist lipid clinics across Australia. 341 children and adolescents under 18 years of age with FH, enrolled between February 2015 and March 2026. None, observational study. Age at enrolment, mode of FH detection, uptake of genetic testing, lipid-lowering therapy patterns, attainment of low-density lipoprotein-cholesterol (LDL-C) goals and testing of lipoprotein(a) [Lp(a)]. The mean age at enrolment was 11.9 years; 51.4% were male and 53.5% were index cases. Only 52.6% had undergone genetic testing. The mean untreated LDL-C was 6.2 mmol/L. At follow-up, 85.4% were on lipid-lowering therapy, with 91.3% on a moderate-intensity or high-intensity statin but only 12.7% received combination therapy with ezetimibe. The mean treated LDL-C was 3.8 mmol/L and only 48.3% achieved the guideline-recommended goal. Factors associated with goal attainment included a lower pre-treatment LDL-C and use of lipid-lowering therapy. Lp(a) was tested in only 33.7% of children. This study reveals five critical gaps in the care of Australian children with FH: late diagnosis after the recommended age to commence therapy; non-attainment of LDL-C goals despite treatment; under-utilisation of genetic testing; infrequent cascade testing and infrequent testing of Lp(a). Addressing these gaps demands a coordinated multilevel response, including a universal childhood FH screening programme coupled with state-based cascade testing hubs and rigorous implementation of evidence-based paediatric guidelines.

PMID 42716708
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PubMedJournal of clinical lipidology2026-09-08

Efficacy and safety of add-on bempedoic acid on maximal dose of rosuvastatin and ezetimibe in patients with established coronary artery disease (ADDBEMPERE study).

Garg Naveen N, Jaiswal Amit A, Kapoor Aditya A, Tewari Satendra S et al.

Bempedoic acid (BA) has emerged as an add-on therapy to statin and ezetimibe combination to achieve low-density lipoprotein cholesterol (LDL-C) targets. Data are limited regarding the efficacy and safety of adding BA in patients who are receiving the maximal dose of rosuvastatin in combination with ezetimibe. This study evaluated the efficacy and safety of adding bempedoic acid on the maximal dose of rosuvastatin with ezetimibe to achieve LDL cholesterol target in patients with established CAD. Postcoronary angioplasty patients having LDL >70 mg/dL despite being on a stable dose of ezetimibe and rosuvastatin (40 mg) combination were initiated on BA. Follow-up was done at 12, 24, and 48 weeks. Efficacy of BA was assessed by changes in lipid parameters. Safety assessments included clinical adverse events and changes in laboratory parameters. Adverse events of special interest included musculoskeletal safety, uric acid levels, hepatic and renal safety, and new-onset diabetes. The study involved 322 patients. Baseline LDL-C was 82.1 ± 15.6 mg/dL (mean ± SD) and was reduced to 57.6 ± 32.0 (-29.8%) at 12 weeks (P < .001) without any further significant reduction. LDL-C levels of <70 and <55 mg/dL were achieved in 84.8% and 69.6% patients, respectively, at 48 weeks. However, LDL-C levels of <30 mg/dL were achieved only in 14.6% patients. A significant reduction in high-sensitivity C-reactive protein was observed. A significant increase in uric acid was noted. However, clinical gout occurred in only 3 patients. None of our patients developed myopathy, new-onset diabetes, hepatic or renal impairment. Addition of BA to the full dose of rosuvastatin and ezetimibe leads to a significant reduction in LDL-C. Benefits start early and are sustained. Therapy is well tolerated.

PMID 42711169
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PubMedFrontiers in medicine2026-09-08

Contemporary non-statin therapies for dyslipidemia management: achieving current lipid targets.

Ponte-Negretti Carlos I CI, Lorenzatti Alberto A, Wyss-Quintana Fernando F, Alonso Rodrigo R et al.

The current treatment of dyslipidemia in patients with cardiovascular risk (CR) is based on three well-defined principles: First, given the extensive evidence demonstrating the association between elevated low-density lipoprotein cholesterol (LDL-C) levels and cardiovascular risk, the primary therapeutic target is LDL-C. Second, as current guidelines recommend LDL-C targets below 55 mg/dL for high-risk patients, therapeutic goals according to risk level should be achieved as early as possible, and combination therapy is increasingly necessary. Third evidence indicates that non-statin therapies-including ezetimibe, bempedoic acid, PCSK9 inhibitors (evolocumab and alirocumab), and inclisiran-provide substantial LDL-C reductions and reduce cardiovascular events. These agents are particularly effective in very high-risk and statin-intolerant populations, with bempedoic acid addressing both lipid and inflammatory pathways. Additionally, the fixed-dose combination of bempedoic acid and ezetimibe produces an approximately 36.2% reduction in LDL-C in high-risk patients. Risk-stratified guidelines recommend ezetimibe as first-line add-on therapy, followed by PCSK9 inhibitors or bempedoic acid based on residual LDL-C levels and tolerability. Alirocumab has demonstrated a significant reduction in the primary composite endpoint of major adverse cardiovascular events (MACE), with a favorable trend in all-cause mortality. Furthermore, inflammation (measured by hsCRP) provides complementary prognostic information beyond LDL-C. This expert position paper proposes practical algorithms for a precision medicine approach in Latin America, matching treatment intensity to individual risk profiles for the primary and secondary prevention of atherosclerotic cardiovascular disease.

PMID 42708006
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PubMedPraxis2026-09-08

[Dyslipidaemia guideline issued by the Department of Internal Medicine (DIM) at the University Hospital Zurich (USZ)].

Rosemann Andrea A, von Eckardstein Arnold A, Sudano Isabella I, Senn Oliver O et al.

This guideline (GL) provides an overview of the management of dyslipidaemia based on international guidelines and new evidence from studies published up to June 2026. The GL focuses on primary care and takes into account the specific characteristics of the Swiss healthcare system. Lipid-lowering therapy should be risk-adapted, with the current 2025/2026 AGLA, ESC/EAS, and ACC/AHA dyslipidaemia GLs recommending a target-based treatment strategy. Our GL presents a structured approach to cardiovascular risk stratification and supports clinicians in selecting the most appropriate risk prediction model for individual patients. Risk modifiers - including family history, ethnicity, comorbidities, biomarkers, and lipoprotein(a) - should be considered in addition to traditional cardiovascular risk factors. In addition to lifestyle optimization, statins remain the first-line treatment. If the required LDL-C reduction is not achieved with statins alone, Ezetimibe, bempedoic acid, and PCSK9 inhibitors should be added sequentially.

PMID 42708198
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