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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

PubMedJournal of clinical medicine2026-06-12

Rosuvastatin Attenuates Pulmonary Damage in Rats with Cecal Ligation and Puncture-Induced Sepsis.

Yıldız Safiye İnşira Sİ, Saydam Faruk F, Topçu Atilla A, Tümkaya Levent L et al.

Background/Objectives: Sepsis is a life-threatening syndrome arising from a dysregulated host response to infection, frequently leading to multiple organ dysfunction, with the lungs being among the most severely affected organs. Oxidative stress, inflammation, apoptosis, and DNA damage play key roles in the pathogenesis of sepsis-induced acute lung injury (ALI). Beyond its lipid-lowering effects, rosuvastatin possesses anti-inflammatory and antioxidant properties that may confer protective effects in sepsis. This study was designed to investigate the dose-dependent prophylactic efficacy of rosuvastatin in mitigating pulmonary damage in rats with cecal ligation and puncture (CLP)-induced sepsis. Methods: Sprague-Dawley rats were randomly divided into six groups: Sham, Sham + rosuvastatin (10 mg/kg), Sham + rosuvastatin (20 mg/kg), CLP, CLP + rosuvastatin (10 mg/kg), and CLP + rosuvastatin (20 mg/kg). Rosuvastatin was administered via oral gavage 4 h before the surgical procedures in the experimental groups. All animals were sacrificed 16 h following surgical procedures. Lung tissues were analyzed for biochemical markers, including malondialdehyde (MDA) and reduced glutathione (GSH), as well as histopathological changes and immunohistochemical expression of NF-κB/p65, caspase-3, and 8-OHdG. Results: CLP-induced sepsis significantly increased MDA levels while decreasing GSH levels, indicating enhanced oxidative stress. Rosuvastatin treatment significantly reversed these changes. Histopathological analysis revealed marked lung injury in the CLP group, including alveolar inflammation, interstitial inflammation, vascular congestion, and increased alveolar septal thickness, all of which were significantly reduced following rosuvastatin administration. Immunohistochemical findings demonstrated increased expression of NF-κB/p65, caspase-3, and 8-OHdG in the CLP group, whereas rosuvastatin significantly attenuated these expressions. No significant difference in prophylactic efficacy was observed between the 10 mg/kg and 20 mg/kg doses of rosuvastatin. Conclusions: Rosuvastatin demonstrated a protective effect against sepsis-induced pulmonary damage by reducing oxidative stress, inflammation, apoptosis, and DNA damage. These findings suggest that rosuvastatin may have prophylactic potential in sepsis; however, further support is needed from investigations of cellular pathways in different mechanistic directions.

PMID 42278973
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PubMedDiabetes/metabolism research and reviews2026-06-11

Lower Risk of Type 2 Diabetes Mellitus With PCSK9 Inhibitors Compared With Other Lipid-Lowering Agents Among Patients With Hyperlipidaemia.

Lin Jiun-Lu JL, Hsu Christine C, Lo Shao-Wei SW, Nigam Nishtha N et al.

The purpose of this paper is to compare the risk of incident type 2 diabetes mellitus (T2DM) among patients with hyperlipidaemia treated with proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors versus statins and other nonstatin lipid-lowering agents. This target trial emulation study used a retrospective, propensity score-matched cohort design based on the TriNetX Global Collaborative Network. Adults (≥ 18 years) with hyperlipidaemia diagnosed between January 2015 and December 2024 were included. Patients with preexisting diabetes, malignancy, or death during follow-up were excluded. Three active-comparator analyses compared PCSK9 inhibitors with statins, ezetimibe and fenofibrates under a per-protocol framework. Propensity score matching (1:1) balanced demographics, comorbidities, BMI, lipid profiles and healthcare utilization. Incident T2DM was identified using ICD-10 codes and analysed. Multiple sensitivity analyses including intention-to-treat analysis were performed. In the main analysis model, PCSK9 inhibitor use was associated with a significantly lower risk of incident T2DM than statins (HR 0.815; 95% CI 0.764-0.869), ezetimibe (HR 0.919, 95% CI 0.867-0.974), and fenofibrates (HR 0.517; 95% CI 0.493-0.542). Findings were consistent across subgroups and sensitivity analyses. No significant difference was observed between different PCSK9 inhibitor modalities. In this large-scale real-world cohort, PCSK9 inhibitors were associated with a lower risk of new-onset T2DM compared with other lipid-lowering therapies, supporting their metabolic safety and clinical use in patients at risk for diabetes.

PMID 42274293
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PubMedWound repair and regeneration : official publication of the Wound Healing Society [and] the European Tissue Repair Society2026-06-11

Topical Statin Therapy in Wound Healing: A Systemic Review of Therapeutic Outcomes.

Stratman Scott S, Campbell Caroline C, He Helen H

This systematic review evaluates the therapeutic potential of topical statin therapy in cutaneous wound healing across in vitro and in vivo animal and human studies. A PRIMSA-guided PubMed search identified 31 eligible studies evaluating simvastatin, atorvastatin, pravastatin, rosuvastatin, or mevastatin formulated a creams, ointments, hydrogels, nanoemulgels, liposomal gels, nanosponges, films, and advanced dressing for diabetic, excisional, burn, infected, pressure, vascular, and postoperative wounds. Across models, topical statins consistently accelerated wound closure and improved histological quality through convergent mechanisms, including enhanced angiogenesis and lymphoangiogenesis, promotion of re-epithelialization, modulation of collagen deposition and extracellular matrix remodelling, and attenuation of pro-inflammatory and infectious burden. Mechanistic studies demonstrated activation of intracellular signalling pathways, upregulation of vascular endothelial growth factor and CD31, macrophage polarization, restoration of epidermal growth factor receptor signalling via caveolin-1 and glucocorticoid receptor modulation, and context-dependent regulation of collagen I/III and myofibroblast activity. Clinical data, although limited, showed some initial promise in pressure ulcers and laparotomy wound healing. Safety profiles were generally favorable, with xerosis and increased transepidermal water loss reported only at higher simvastatin concentrations. Overall, topical statins represent a promising, mechanistically rational adjunct for wound management; however, heterogeneity in wound types, formulations, dosing, and comparators, together with sparse, small clinical trials, underscores the need for rigorously designed human studies to define optimal indication, concentrations, and delivery systems.

PMID 42273908
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PubMedJournal of chemical information and modeling2026-06-11

Structural Characterization of the Type IV Secretion System in Brucella melitensis for Virtual Screening-Based Therapeutic Targeting.

Kapoor Jahnvi J, Panda Amisha A, Rajagopal Raman R, Kumar Sanjiv S et al.

Brucellosis is a globally important zoonotic disease caused by Brucella melitensis, the most virulent and clinically significant species affecting both humans and livestock. Unlike many Gram-negative pathogens, B. melitensis lacks conventional virulence factors and instead relies on specialized systems such as the Type IV Secretion System (T4SS) for the secretion of effector proteins. In this study, an integrated computational pipeline was implemented to identify, model, and assemble the T4SS components encoded by virB operon from the complete B. melitensis proteome. Template-based modeling strategies were employed to model T4SS subcomplexes, referencing crystallographic data from E. coli T4SS. Structural superposition with E. coli homologues revealed highly conserved architecture despite only 30-50% sequence identity. Stereochemical validation confirmed favorable interactions among most VirB protein pairs, and membrane insertion analysis corroborated the spatial orientation of the modeled T4SS. Potential of T4SS as a drug target was explored by targeting dimeric interface of VirB11 ATPase to disrupt protein-protein interactions. Virtual screening of compounds from DrugBank revealed compounds with docking score ≤-7.0 kcal/mol, and ADMET screening yielded three promising candidates─Ezetimibe (Drug ID: DB00973), Chlordiazepoxide (Drug ID: DB00475), and Alloin (Drug ID: DB15477). MM-GBSA analysis and molecular dynamics simulation supported favorable protein-ligand interactions. Collectively, these findings provide new insights into the architecture of B. melitensis T4SS and identify three potential drug molecules targeting T4SS. This supports FDA-approved drug repurposing as an effective strategy for antivirulence therapy against Brucellosis.

PMID 42270450
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PubMedJournal of the Saudi Heart Association2026-06-11

Advancing Lipid Management: Saudi Heart Association Position Statement on PCSK9-targeted Therapies in the Primary and Secondary Prevention of Cardiovascular Disease.

AlHabeeb Waleed W, Alamri Hussein H, Elbadawi Hussein H, AlRuthia Yazed S YS et al.

Despite robust evidence for low-density lipoprotein cholesterol (LDL-C) reduction in atherosclerotic cardiovascular disease (ASCVD) prevention, attainment of guideline-recommended targets remains suboptimal in Saudi Arabia, especially among high- and very high-risk patients. Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9)-targeted therapies, which include monoclonal antibodies (evolocumab, alirocumab) and small interfering RNA (inclisiran), offer potent LDL-C lowering that can help address this gap. The Saudi Heart Association (SHA) convened a multidisciplinary panel to review evidence from randomized controlled trials, real-world studies, and economic analyses on PCSK9-targeted therapies. Recommendations were developed through expert consensus, contextualized to the Saudi healthcare environment. PCSK9 inhibitors (evolocumab, alirocumab) lower LDL-C substantially by around 60% and reduce the risk of adverse cardiovascular outcomes when added to maximally tolerated statins. Inclisiran achieves similar LDL-C reductions with biannual dosing, potentially improving adherence, though cardiovascular outcome data are pending. Both drug classes are well tolerated across diverse patient populations, including those with high or very high-risk, familial hypercholesterolemia (FH), recent acute coronary syndrome (ACS), or statin intolerance. The SHA expert panel recommends the early integration of upfront combination treatment including PCSK9-targeted therapies for patients with high risk features unlikely to reach LDL-C goals with statins ± ezetimibe, including recent ACS, FH, established ASCVD, metabolic conditions with end-organ damage, and statin intolerance. For Saudi populations, targeted integration of these agents into combination regimens offers a significant opportunity to close LDL-C treatment gaps and reduce residual ASCVD risk.

PMID 42273077
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PubMedAtherosclerosis2026-06-11

Persistent gaps in management and risk factor control among patients with atherosclerotic cardiovascular disease: All of us research program.

Bene-Alhasan Yakubu Y, Al Osta Soad S, Issaka Yussif Y, Acquah Isaac I et al.

Contemporary guidelines recommend aggressive low-density lipoprotein cholesterol (LDL-C) lowering in patients with atherosclerotic cardiovascular disease (ASCVD), yet significant treatment gaps persist in clinical practice. We evaluated lipid-lowering therapy (LLT) use, LDL-C control, and prevelance of cardiovascular risk factors among patients with coronary artery disease (CAD), peripheral artery disease (PAD), cerebral atherosclerosis (CAS) and those with all three (polyvascular disease) using real-world data from the NIH-run All of Us Research Program. We analyzed electronic health records from 26,935 patients with ASCVD (CAD 21,573; PAD 4752; CAS 6864; and polyvascular 902) enrolled between 2018 and 2023. We assessed baseline LLT use, LDL-C levels, and prevalence of uncontrolled cardiovascular risk factors, defined as blood pressure ≥130/80 mmHg, hemoglobin A1c ≥ 7%, waist-height ratio (WHtR) ≥ 0.5, and current smoking. Among patients with LDL-C >70 mg/dL, we visualized risk factor intersections using Euler diagrams. Despite high statin use across all cohorts (81% CAD, 82% PAD, 83% CAS, 93% Polyvascular), only 36-47% achieved LDL-C <70 mg/dL and 22-31% had LDL-C ≥100 mg/dL. Combination LLT was markedly underutilized (10-21%), with ezetimibe prescribed in 10-20% and PCSK9 inhibitors in only 1-3% of patients. Among those with LDL-C ≥70 mg/dL, central obesity was ubiquitous (86-89%), more than half had uncontrolled blood pressure (59-63%), 16-26% had hemoglobin A1c ≥ 7%, and 14-20% were active smokers. Patients with polyvascular disease had higher LLT use and LDL-C control but lower risk factor control. Uncontrolled risk factors frequently co-occurred: 29-31% had concurrent obesity and uncontrolled hypertension, and 7-9% harbored the triad of obesity, poor glycemic control, and uncontrolled hypertension. In this large, diverse cohort of patients with ASCVD, substantial gaps persist in achieving guideline-recommended LDL-C targets and controlling cardiovascular risk factors. The marked underutilization of combination LLT and the high coexistence of metabolic risk factors represent significant opportunities for treatment intensification and comprehensive risk factor management.

PMID 42270564
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