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atorvastatin + ezetimibe (CKD 391 / CKD391)

✓ Approved

Chong Kun Dang Pharmaceutical · HMGCR · 小分子

什么是 atorvastatin + ezetimibe？

atorvastatin + ezetimibe 是一种小分子，由Chong Kun Dang Pharmaceutical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CKD 391, CKD391
公司Chong Kun Dang Pharmaceutical
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, Chong Kun Dang Pharmaceutical

作用机制

分子靶点

atorvastatin + ezetimibe 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

atorvastatin + ezetimibe 针对 2 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 disordersHypercholesterolaemia✓ Approved
Metabolism and nutrition disordersHyperlipidaemia✓ Approved

相关研究文献

PubMedRomanian journal of internal medicine = Revue roumaine de medecine interne2026-10-26

Achieving Risk-Specific Absolute LDL-C Threshold with PCSK9 Inhibitors: A Real-World, Single-Center Analysis.

Ciobanu Dana Mihaela DM, Berchișan Antonia A, Mălan Cosmina C, Rusu Adriana A et al.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors emerged as an effective treatment for hypercholesterolemia in clinical trials, however real-world evidence shows considerable heterogeneity. We aimed to assess the effectiveness and safety of injectable PCSK9 inhibitors in real-world patients. Our retrospective analysis included 45 consecutive adults, 18 (40%) men, mean age 57.4 years, inadequately controlled on, or intolerant to, statins and/or ezetimibe, and newly initiated on alirocumab 75 mg or 150 mg, evolocumab 140 mg, or inclisiran 284 mg. Biochemical parameters and adverse events were recorded at baseline and when LDL-C reached the risk-specific absolute threshold or the lowest LDL-C closest to it after starting PCSK9 inhibitors (<55 mg/dL very high, <70 mg/dL high cardiovascular risk, per European Society of Cardiology). LDL-C was also assessed at standardized time points (3, 6, 12, 18, 24 months). At 3 and 6 months, LDL-C decreased by a median of 54.4% and 59.2% (both p < 0.001), with 52.4% and 50.0% of patients below threshold. The best LDL-C reduction was 66.9% (from 145 mg/dL to 50 mg/dL; p < 0.001) at a median time to first documented threshold attainment of 5 months. In an exploratory analysis, no significant association was detected between LDL-C reduction and sex, diabetes, statin intensity or ezetimibe use. No clinically relevant hepatic or muscular toxicity was attributed to PCSK9 inhibitors. In real-world patients aiming to achieve the absolute LDL-C threshold on PCSK9 inhibitors, treatment was associated with marked LDL-C reduction after a median of 5 months.

PMID 42928644
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PubMedPeerJ2026-10-25

Effectiveness and safety of atorvastatin/ ezetimibe fixed-dose combination in hypercholesterolemia: a systematic review and network meta-analysis.

Qian Juying J, Zhang Xingxin X, Li Qing Q, Chen Sisi S

Many patients fail to achieve low-density lipoprotein cholesterol (LDL-C) targets with statin monotherapy, calling for a combination of statins and ezetimibe. This systematic review and network meta-analysis evaluated the comparative effectiveness and safety of atorvastatin monotherapy, atorvastatin/ezetimibe free-equivalent combination (AS/EZ FEC), and fixed-dose combination (AS/EZ FDC) in patients with hypercholesterolemia. Randomized controlled trials were retrieved from electronic databases. Primary outcomes were the percentage change in LDL-C from baseline and LDL-C goal attainment, analyzed using mean difference (MD) and risk ratio (RR) with 95% confidence intervals (CI). Treatments were ranked via surface under the cumulative ranking curve (SUCRA). The two combination therapies were compared to AS alone for their safety profiles and tolerability. Forty-six trials (n = 10,567) were included. AS/EZ FDC reduced LDL-C more than AS alone (MD -13.94%, 95% CI [-18.90% to -9.10%]), with similar results for AS/EZ FEC (MD -12.41%, 95% CI [-14.61% to -10.22%]). SUCRA rankings for LDL-C reduction were FDC (86.2%), FEC (63.8%), and AS (0.0%). For LDL-C goal attainment, the RR was 1.87 (95% CI [1.47-2.39]) for FEC vs. monotherapy, 1.80 (95% CI [0.85-3.81]) for FDC vs. monotherapy. No significant differences in safety profiles were observed between treatments. AS/EZ combination therapies provide greater improvements in LDL-C reduction and goal attainment compared with AS monotherapy, with FDC ranking highest in LDL-C reduction. Treatment with AS/EZ FEC or FDC did not increase the risk of adverse events compared to AS monotherapy and was well tolerated. These findings support FDC use when intensive LDL-C lowering is required.

PMID 42927391
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PubMedDaru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences2026-10-25

Association between perioperative statin-ezetimibe therapy and reoperation following arthroscopic rotator cuff repair: A TriNetX database study.

Mahatme Ronak R, Gangavaram Anish A, Muthusamy Nishanth N, Moore Shawn S et al.

Hyperlipidemia (HLD) impairs tendon healing and is associated with increased revision risk following arthroscopic rotator cuff repair (ARCR). While statins may partially mitigate this effect, residual dyslipidemia may impair healing. Ezetimibe, through inhibition of intestinal cholesterol absorption, has demonstrated favorable effects on tendon healing in preclinical studies. This study evaluated whether perioperative statin-ezetimibe therapy is associated with improved postoperative outcomes following ARCR compared with statin monotherapy and patients without HLD. A retrospective cohort study was conducted using the TriNetX Research Network. Adult patients undergoing ARCR were stratified into three cohorts based on HLD status and perioperative (± 6 months) lipid-lowering therapy: (1) documented HLD treated with statin-ezetimibe prescriptions, (2) patients without documented HLD or lipid-lowering therapy prescriptions, and (3) documented HLD treated with statin monotherapy prescriptions. Primary comparisons were predefined between cohort 1 and cohorts 2 and 3. Propensity score matching (1:1) adjusted for demographics and comorbidities. Tear size and presence of fatty atrophy and fatty infiltration were not adjusted for. Outcomes occurring within 5 years included revision rotator cuff repair (RCR), conversion to shoulder arthroplasty, and secondary shoulder arthroscopy. After matching, 1,066 patients were included in cohorts 1 and 2 and 1,114 patients in cohorts 1 and 3. Compared with patients without HLD, statin-ezetimibe therapy demonstrated similar rates of revision RCR (5.4% vs. 6.4%; RR 0.853; p = 0.358), conversion to shoulder arthroplasty (RR 1.227; p = 0.470), and secondary arthroscopy (RR 0.846; p = 0.260). Compared with statin monotherapy, statin-ezetimibe therapy was associated with lower rates of revision RCR (5.6% vs. 8.0%; RR 0.697; p = 0.023) and secondary shoulder arthroscopy (7.3% vs. 9.6%; RR 0.757; p = 0.048), while arthroplasty rates remained similar (RR 1.261; p = 0.400). Among patients with HLD undergoing ARCR, perioperative statin-ezetimibe therapy was associated with lower reoperation rates compared with statin monotherapy and postoperative outcomes comparable to patients without HLD. These findings support further investigation of intensified lipid-lowering therapy, while accounting for tear size and fatty infiltration.

PMID 42927533
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PubMedDrug design, development and therapy2026-10-25

Steady-State Pharmacokinetic Drug-Drug Interaction Study of Zastaprazan, a Novel Potassium-Competitive Acid Blocker, and Atorvastatin in Healthy Participants.

Yang A-Young AY, Kim Hongsock H, Yoo Hyounggyoon H, Lee Yil-Seob YS et al.

Zastaprazan is a novel potassium-competitive acid blocker with CYP3A-mediated metabolism, whereas atorvastatin undergoes CYP3A4- and transporter-mediated disposition. Because these drugs may be co-administered and their net interaction cannot be inferred from shared metabolic pathways alone, this study evaluated their steady-state pharmacokinetic drug-drug interaction. This open-label, fixed-sequence, three-period, multiple-dose study included healthy Korean men. Participants received atorvastatin 40 mg once daily, zastaprazan 20 mg once daily, and concomitant atorvastatin and zastaprazan, each for 5 consecutive days, under steady-state conditions. Plasma concentrations of zastaprazan, atorvastatin, and 2-hydroxyatorvastatin were measured, and geometric mean ratios (GMRs) with 90% confidence intervals (CIs) were calculated for C max,ss and AUC τ,ss. Twenty-four healthy Korean men received at least one dose of a study drug, and 22 were included in the pharmacokinetic analysis. Atorvastatin decreased zastaprazan C max,ss by approximately 26% (GMR, 0.740; 90% CI, 0.655-0.836), whereas AUC τ,ss was preserved (GMR, 1.054; 90% CI, 0.927-1.198). Zastaprazan did not meaningfully alter atorvastatin exposure (C max,ss GMR, 0.982; 90% CI, 0.806-1.195; AUC τ,ss GMR, 1.029; 90% CI, 0.944-1.122). The AUC τ,ss of 2-hydroxyatorvastatin showed a modest decrease (GMR, 0.940; 90% CI, 0.889-0.994) that remained within the predefined conventional reference range. Co-administration was generally well tolerated, with no serious adverse events or adverse event-related discontinuations. Zastaprazan did not meaningfully alter atorvastatin C max,ss or AUC τ,ss under the studied conditions. Although atorvastatin reduced zastaprazan C max,ss, total exposure was preserved, a pattern consistent with altered absorption kinetics without establishing a specific mechanism. The pharmacodynamic significance of the lower zastaprazan C max,ss remains uncertain because intragastric pH was not measured. These pharmacokinetic findings do not suggest a need for atorvastatin dose adjustment under the studied conditions.

PMID 42921573
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PubMedNutrition, metabolism, and cardiovascular diseases : NMCD2026-10-25

Extreme cardiovascular risk as a major barrier to LDL-C target achievement: insights from ITACARE-P registry.

Giallauria Francesco F, Cuomo Gianluigi G, Faggiano Andrea A, Vallefuoco Giuseppe G et al.

Achieving low-density lipoprotein cholesterol (LDL-C) targets remains challenging in secondary cardiovascular prevention despite the availability of effective lipid-lowering therapies. The 2025 ESC/EAS dyslipidaemia guidelines introduced an "extreme cardiovascular risk" category requiring LDL-C levels <40 mg/dL, potentially increasing the difficulty of target attainment. We aimed to identify clinical and therapeutic predictors of LDL-C target achievement according to the 2025 ESC/EAS recommendations and estimate the probability of goal attainment across different risk categories and treatment strategies. This sub-analysis of the multicentre ITACARE-P registry included 1904 outpatients with established atherosclerotic cardiovascular disease. Missing data were handled using multiple imputation, and stable predictors were selected through Elastic Net regularization across 20 imputed datasets. A multivariable generalized linear mixed-effects model was internally validated using 1000 bootstrap resamples. Overall, 38% of patients achieved guideline-recommended LDL-C targets. Independent predictors of target attainment included PCSK9 inhibitor therapy (OR = 7.65), high-intensity statins (OR = 4.73), ezetimibe (OR = 2.64), male sex (OR = 1.99), diabetes mellitus (OR = 1.99), coronary artery disease (OR = 2.73), participation in cardiac rehabilitation (OR = 1.81), and high physical activity (O = 1.54). Current smoking, prior dyslipidaemia, and longer disease duration were associated with lower odds of achievement. Very-high-risk patients were more likely to achieve LDL-C targets than extreme-risk patients (OR = 5.66). Predicted target attainment ranged from 9.8% to 88.6% according to treatment intensity and risk category. Model discrimination was good (optimism-corrected AUC = 0.782). LDL-C target attainment under the 2025 ESC/EAS guidelines remains suboptimal, particularly among extreme-risk patients. Earlier therapeutic intensification and individualized lipid-lowering strategies may be necessary to improve real-world goal achievement.

PMID 42928029
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PubMedJournal of molecular histology2026-10-23

Comprehensive insight into the anti-dyslipidemic and pancreatic lipase inhibition activities of Clematis flammula L. and Fraxinus angustifolia Vahl. extracts using two animal models.

Zaidi Adlane A, Atmani-Kilani Dina D, Atmani Djebbar D, Moulaoui Kenza K et al.

Clematis flammula and Fraxinus angustifolia leaves are commonly used in Algeria to treat inflammatory diseases, with potential hypolipidemic effects that have not been investigated so far. The present study explored the in vitro, ex vivo, and in vivo hypolipidemic effects of ethanolic leaf extracts from both plants using two animal models (mice and rabbits) with distinct lipid metabolism. Dyslipidemia was induced by oral administration of Triton X-100, once daily for three consecutive days. Immediately after each Triton X-100 administration, animals received plant extracts (100 and 200 mg/kg bw) or atorvastatin (10 mg/kg bw). Anti-lipase and anti-HMG-CoA reductase activities were evaluated using in vitro and ex vivo assays. Triton X-100 induced marked alterations in serum lipid profiles, characterized by increased LDL-C, VLDL-C, and total cholesterol levels, which were improved by C. flammula and F. angustifolia extracts, particularly at 200 mg/kg bw. While F. angustifolia exhibited greater hypolipidemic efficacy, the lack of improvement in total cholesterol in mice treated with C. flammula, in contrast to rabbits, may suggest species-dependent differences in lipid metabolism, potentially involving CETP-mediated cholesterol transport, which requires further experimental confirmation. In vitro anti-lipase assays showed greater inhibitory potency for F. angustifolia (IC50 = 3.55 µg/mL) than C. flammula (IC50 = 12.10 µg/mL). Both extracts inhibited HMG-CoA reductase activity by over 60% in vitro and ex vivo, with IC50 values of 90.06 and 96.57 µg/mL for F. angustifolia and C. flammula, respectively. Histological examination further supported the hypolipidemic effects of both extracts. Overall, these findings highlight C. flammula and F. angustifolia as promising natural sources of bioactive compounds with potential applications in managing hypercholesterolemia and dyslipidemia.

PMID 42918911
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