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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

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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PubMedAAPS PharmSciTech2026-09-10

Direct Powder Extrusion of Atorvastatin 3D-Printed Tablets for Immediate-Release: Solid-State Characterization and Dissolution Performance.

Anekalla Thirupathi Reddy TR, Bashetty Sujith Raj SR, Nalajala Navya N, Narala Nagarjuna N et al.

Thermal extrusion is a well-established approach for producing amorphous solid dispersions (ASDs) to enhance the solubility, dissolution, and bioavailability of poorly water-soluble drugs. Atorvastatin calcium trihydrate (ACT), a BCS class II lipid-lowering agent, exhibits low aqueous solubility, limited oral bioavailability, and variable absorption. The present study investigated the feasibility of fabricating immediate-release ACT tablets using a direct powder extrusion (DPE) three-dimensional (3D) printing technique, thereby enabling in situ drug amorphization and tablet fabrication in a single step. Critical process parameters (CPPs), including nozzle speed, printhead temperature, infill density, and extrusion pressure, were systematically optimized to achieve reproducible oval-shaped tablets with acceptable mechanical integrity and structural fidelity. Among the evaluated polymeric systems for improved dissolution, a combination of 25% (w/w) polyethylene glycol (PEG), 25% (w/w) polyethylene oxide (PEO), 15% (w/w) Pluronic F127, and 15% (w/w) sorbitol yielded consistent DPE printing at a 25% infill density, which has been shown to improve dissolution. The 3D-printed tablets, characterized by physicochemical, structural, and thermal analyses, confirmed successful drug amorphization. In vitro dissolution testing in phosphate buffer (PBS, pH 6.8) demonstrated rapid tablet disintegration and immediate drug release, with ~86% of ACT released within 30 min, meeting United States Pharmacopeia (USP) specifications for immediate-release ACT tablets. Accelerated stability studies (40°C/75% RH) for 3 months showed retention of the amorphous state, as confirmed from DSC and pXRD, with dissolution profiles comparable to initial results. Overall, the findings demonstrated that DPE-based thermal extrusion 3D printing enables single-step fabrication of amorphous ACT tablets with improved dissolution performance and stability, highlighting its potential as a single-step, flexible, patient-centric manufacturing platform at the point of service.

PMID 42717140
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PubMedFrontiers in medicine2026-09-10

Case Report: Balancing immunosuppression and infection-intravenous immunoglobulin in anti-HMGCR immune-mediated necrotizing myopathy complicated by severe pneumonia.

Fu Jing J, Zhao Qiong Q, Lou Jing-Bo JB, Tang Gui-Hua GH et al.

A 65-year-old male with a 3-year history of atorvastatin use presented with progressive proximal muscle weakness, dysphagia, and markedly elevated creatine kinase (2,277 U/L). Initially misdiagnosed with polymyositis, he deteriorated with severe pneumonia, septicemia, and type I respiratory failure requiring mechanical ventilation. Interleukin-6 rose from 12.83 to 610.9 pg/mL during sepsis. After confirmation of anti-HMGCR antibody positivity (18 arbitrary units [AU], cutoff >10 AU) via line blot assay, we discontinued methotrexate, maintained methylprednisolone at 40 mg, and initiated intravenous immunoglobulin (IVIG) 0.4 g/kg/day for 5 days with broad-spectrum antibiotics. Within two weeks, proximal muscle strength (MRC scale) improved from 2/5 to 4/5, IL-6 normalized to 8.56 pg/mL, and respiratory failure resolved. This case suggests that IVIG may serve as a safe immunomodulatory bridge in critically ill IMNM patients with severe infections.

PMID 42718719
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PubMedIranian journal of pharmaceutical research : IJPR2026-09-09

Synthesis and Evaluation of the Effects of Nanoparticles of Atorvastatin and Atorvastatin on Cuprizone-Induced Demyelination: Modulation of the Nrf2/NF-kB Signaling Pathway.

Shirooie Samira S, Heidarizade Niloofar N, Noori Tayebeh T, Sureda Antoni A et al.

Multiple sclerosis (MS) is a chronic inflammatory disease of the central nervous system (CNS) characterized by damage to the myelin sheath and, over time, by progressive neurological disability. Statins have attracted attention in MS research owing to their anti-inflammatory and neuroprotective effects. This study assessed whether atorvastatin could ameliorate cuprizone-induced behavioral and histopathological changes in the brains of male C57BL/6 mice. All groups of mice, except the control group, which received a normal diet, were fed 0.2% cuprizone (CPZ) in their daily diet for 6 weeks to induce demyelination. The treatment groups received atorvastatin (1, 2, or 4 mg/kg/day, i.p.) or nano-atorvastatin (2 mg/kg/day, i.p.) during the final 2 weeks of the study. At the end of the study, behavioral tests were conducted, and immunofluorescence assessment of NF-kB p65 and Nrf2 in the corpus callosum was conducted. CPZ caused progressive weight loss by the end of the study compared with the control group; this effect was reversed by treatment with atorvastatin and nano-atorvastatin. All behavioral tests showed reduced motor coordination in the CPZ group (P < 0.001) compared with the control group. Administration of atorvastatin and nano-atorvastatin during the last 2 weeks reversed these motor deficits. Histopathological examination showed significant demyelination in the CPZ group, which was reversed by atorvastatin injections. Furthermore, CPZ significantly decreased Nrf2 levels (P < 0.001) and increased NF-kB p65 levels (P < 0.001) in the corpus callosum; these changes were stabilized in the atorvastatin and nano-atorvastatin groups. Atorvastatin may attenuate CPZ-induced toxicity by reducing demyelination and modulating the NF-kB p65 and Nrf2 signaling pathways.

PMID 42713419
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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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PubMedNeurotoxicity research2026-09-09

Atorvastatin Shows Limited Disease-Modifying Effects in an A53T α-Synuclein Mouse Model of Parkinson's Disease.

Wei Lijian L, Hua Junkai J, Tang Shuangfeng S, Lei Jianming J et al.

Neuroprotective effects of statins in Parkinson's disease (PD) remain uncertain, and their activity in genetic α-synuclein (αSyn) disease models has been insufficiently characterized. We evaluated atorvastatin (ATO) in a mouse model with nigral overexpression of human A53T-mutant αSyn. Mice received ATO by oral gavage at 10 mg/kg/day for 5 weeks and were assessed using behavioral testing, neuropathological assessment, brain transcriptomics, and molecular docking. ATO inhibited cholesterol biosynthesis-related transcriptional programs and broadly remodeled lipid metabolism-associated networks, but did not lead to functional or histopathological benefit. ATO did not ameliorate motor deficits, restore dopaminergic markers, or reduce αSyn protein levels or pSer129-αSyn immunoreactivity. Transcriptomic analysis further showed that ATO failed to reverse the core disease-associated signature induced by A53T αSyn overexpression and instead increased SNCA mRNA. Targeted RNA-seq and western blot analyses showed no parallel increase in Prkn, Gba1, or Lamp2 transcript abundance or in PARKIN, GBA1, or LAMP2A protein expression. Molecular docking, used here as an exploratory structural comparison, suggested a relatively weak predicted interaction between ATO and αSyn when compared with several other statins and provided supportive context for the lack of efficacy. Overall, our findings indicate limited efficacy of ATO in this αSyn-driven setting and support further comparative evaluation of individual statins across complementary PD models.

PMID 42714756
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