Drug Database
EZ

ezetimibe + rosuvastatin (NVP1205 / NVP 1205)

✓ Approved

NVP Healthcare · HMGCR · Small Molecule

What is ezetimibe + rosuvastatin?

ezetimibe + rosuvastatin is a small molecule developed by NVP Healthcare. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesNVP1205, NVP 1205
CompanyNVP Healthcare
Drug ClassSmall Molecule
Molecular TargetHMGCR, NPC1L1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, NVP Healthcare

Mechanism of Action

Molecular Targets

ezetimibe + rosuvastatin acts on 2 molecular targets:

HMGCR3-hydroxy-3-methylglutaryl-CoA reductase (LDLCQ3, LGMDR28)
NPC1L1NPC1 like intracellular cholesterol transporter 1 (SLC65A2, LDLCQ7)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

ezetimibe + rosuvastatin is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Metabolism and nutrition disordersHyperlipidaemia✓ Approved

Related Research Articles

PubMedMedScience2026-07-17

CRISPR screening reveals NPC1L1 as a key driver of glioblastoma progression via cholesterol metabolic regulation.

Liu Xiao X, Yang Guangzhao G, Qin Haozhe H, Zhang Qi Q et al.

Glioblastoma (GBM), the most aggressive central nervous system (CNS) malignancy, currently lacks curative therapeutic options. While immunotherapy has revolutionized treatment for many cancers, GBM remains refractory to immune-based interventions due to the absence of effective immunotherapeutic targets. Here, through CRISPR screening, we identify Niemann-Pick C1-like 1 (NPC1L1) as a previously unrecognized key driver of GBM progression. Mechanistically, NPC1L1 modulates cholesterol metabolism to concurrently enhance tumor cell stemness and suppress CD8+ T-cell activation, thus inducing tumor progression. Notably, combined treatment with ezetimibe (NPC1L1 inhibitor) and anti-PD-1 antibody elicited potent antitumor activity in GBM orthotopic mouse models. Collectively, these findings establish NPC1L1 as a critical regulator of GBM pathogenesis, underscoring the translational potential of targeting NPC1L1-mediated cholesterol metabolism for developing novel GBM immunotherapies.

PMID 42467361
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PubMedEuropean heart journal2026-07-17

Peripheral artery disease: advances in medical therapy.

Garagoli Fernando F, Slipczuk Leandro L, Shapiro Michael D MD, Bonaca Marc P MP et al.

Peripheral artery disease (PAD) is a prevalent manifestation of systemic atherosclerosis, associated with elevated risks of major adverse cardiovascular events (MACE) and major adverse limb events (MALE). Despite its clinical significance, PAD remains underdiagnosed and undertreated, reflecting substantial gaps in guideline implementation. This review highlights advances in the medical management of PAD, focusing on strategies targeting the metabolic, lipid, immuno-inflammatory, and thrombotic drivers of disease to improve cardiovascular and limb outcomes. Optimal management requires intensive, multifaceted approaches that integrate lifestyle modification (including smoking cessation, a healthy diet, and physical activity), risk factor control, and pharmacologic interventions. Dual pathway antithrombotic therapy with low-dose rivaroxaban and aspirin has emerged as a superior strategy to mitigate both cardiovascular and limb events in patients with high ischaemic risk and non-high bleeding risk. Statins are the first-line lipid-lowering therapy for all patients with PAD, and if low-density lipoprotein cholesterol (LDL-C) goals are not achieved with maximally tolerated doses, adjunctive agents-such as ezetimibe, bempedoic acid, and proprotein convertase subtilisin/kexin type 9 inhibitors (PCSK9i)-should be added. Novel antidiabetic agents, particularly glucagon-like peptide-1 receptor agonists (GLP-1 RAs) and sodium-glucose cotransporter-2 inhibitors (SGLT2is), confer cardiovascular and renal benefits independent of glycaemic control, with emerging data suggesting that GLP-1 RAs may also reduce limb events. To date, semaglutide remains the only anti-obesity pharmacotherapy that has been demonstrated to reduce cardiovascular events in high-risk patients with overweight or obesity in the absence of diabetes. We propose a phenotype-driven approach to enable refined risk stratification across the PAD spectrum, supporting individualized and, when needed, more intensive management.

PMID 42466921
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PubMedBMJ open2026-07-16

Effects of China's National Volume-Based Procurement policy on utilisation and affordability of statins in children: an interrupted time series analysis.

Wu Yongyi Y, Bai Wei W, Liu Fanyu F, Fan Xiaohan X et al.

Statins are effective in lowering lipids and reducing cardiovascular risk. In recent decades, rising paediatric lipid levels, especially in low- and middle-income countries (LMICs), have led to growing demand for lipid-lowering drugs. However, access remains limited in LMICs due to financial constraints. To address this, China launched its National Volume-Based Procurement (NVBP) policy in 2019, significantly improving the price and affordability of statins. This study evaluates the policy's impact on statin use and expenditures in children. The study used interrupted time series regression to analyse all levels of children's hospitals across the country's monthly procurement records of statins, covering the period from January 2019 to December 2020. It investigated the fluctuations in monthly drug procurement quantity (measured in defined daily doses) and expenditures (affordability) at both the national level and across different tiers of child medical facilities. Following the implementation of the NVBP policy, the utilisation and affordability of statins across all children's hospitals nationwide exhibited a positive upward trend. After the NVBP policy, the affordability of atorvastatin in children's hospitals nationwide improved by at least 90.54% and the affordability of rosuvastatin in children's hospitals nationwide increased by no less than 89.85%. Both before and after the NVBP policy, the majority of utilisation and expenditure in statin was contributed by atorvastatin and rosuvastatin. After the NVBP policy, the utilisation of atorvastatin and rosuvastatin bid-winning generic has increased significantly, making bid-winning generic change from the variety occupying the least market to the variety occupying the most market in children's hospitals. The implementation of China's NVBP policy has resulted in a marked increase in the dosage of atorvastatin and rosuvastatin, while effectively reducing cost expenditure for children. This achievement has been realised without compromising the quality of healthcare services. China's NVBP policy provides a reference and path for the medical reform of all countries in the world especially LMICs.

PMID 42457426
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PubMedBJGP open2026-07-16

Understandability of statin patient information leaflets in the UK: a mixed-methods cross-sectional evaluation.

Rao Diya D, Dickson Jon M JM, Sudbury Mia M, Dixon William W et al.

Statins are the UK's most prescribed medicine and are used more in deprived populations. Patient Information Leaflets (PILs) included in medication packaging may support safe, effective use, but only if they are understandable. Guidance states PILs should have a reading age of ≤13-years, and regulators require that ≥80% of patients answer comprehension questions correctly on them when 'user tested'. To provide the first independent evaluation of the readability and comprehension of UK statin PILs. Study 1: Cross-sectional analysis of the reading age of 39/40 of the UK's approved statin PILs. Study 2: Cross-sectional survey with a representative sample of 517 UK adults aged 40-74. Study 1: Reading age was assessed using four readability formulas, with additional scores calculated after adjusting for potentially familiar technical terms. Study 2: Two PILs (atorvastatin [MSN] and rosuvastatin [Ranbaxy]) were randomly selected and user tested with participants. They answered eight comprehension questions per PIL; responses were double-scored. Study 1: No PIL met the recommended reading age. Median reading age was 15.9 years (15.0 after adjustment). Atorvastatin PILs were least readable. Study 2: Key messages were poorly understood; for atorvastatin, 5/8 items met the≥80% criterion; for rosuvastatin, 2/8 met it. Key safety and use messages were frequently misunderstood. UK statin PILs do not meet recommended readability or comprehension standards and are likely to be difficult to understand for many users. Improving clarity and usability is essential to support equitable understanding and safe, informed long-term statin use.

PMID 42457226
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PubMedEuropean journal of clinical investigation2026-07-16

High-Intensity Statin Treatment Is Associated With Reduced Growth Differentiation Factor-15 in Patients With Coronary Artery Disease.

Stępień Konrad K, Ząbczyk Michał M, Natorska Joanna J, Zalewski Jarosław J et al.

Growth differentiation factor-15 (GDF-15) is upregulated in coronary artery disease (CAD). The relationship of intensive statin therapy with circulating GDF-15 levels has not been explored yet. In the current secondary analysis of an observational cohort, we investigated whether high-intensity statin treatment is associated with GDF-15 in patients with advanced CAD. In 102 CAD patients we measured GDF-15 levels before and after median 7 [6-8] months from initiation atorvastatin 80 mg/day (n = 63, 61.8%) or rosuvastatin 40 mg/day (n = 39, 38.2%). At the two time points we also determined C-reactive protein (CRP), thrombin generation and fibrinolysis inhibitors. There was no concurrent control group. At baseline GDF-15 levels (median 942; interquartile range 639-1284 pg/mL) were associated solely with age (R = 0.567, p < 0.001) and CRP (R = 0.464, p < 0.001), but not with lipid profile. On high-intensity statin therapy GDF-15 reduction by 17.8% was observed (p = 0.006), which was associated with CRP lowering by 46.4% (R = 0.788, p < 0.001), but not with changes in total cholesterol (by 17.6%) and low-density lipoprotein cholesterol (LDL-C) (by 28.1%). However, GDF-15 levels were lower by 28.5% (p < 0.001) and 18.9% (p = 0.013) in 43 patients (42.2%) who achieved the target LDL-C < 1.8 mmol/L and 19 (18.6%) with LDL-C < 1.4 mmol/L, respectively, as compared to the remainder. The type of statin was not associated with follow-up GDF-15. Age (p = 0.029), baseline GDF-15 (p < 0.001) and CRP (p < 0.001), but not LDL-C, were independently associated with follow-up GDF-15. We demonstrated that high-dose statin therapy is associated with lower GDF-15 in CAD patients and this effect is largely related to the anti-inflammatory properties of statins.

PMID 42460854
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PubMedDrug development and industrial pharmacy2026-07-15

Rosuvastatin-Metformin Co-Processing: Enhanced Dissolution, Oral Bioavailability, and Therapeutic Efficacy through a Solvent-Minimized Approach.

El-Masry Soha M SM, Mostafa Shaimaa K SK, Khedr Shaimaa M SM, Abdelwahab Abeer E AE et al.

Rosuvastatin calcium (ROS) exhibits poor aqueous solubility and dissolution-limited oral absorption. This study aimed to develop an oral co-processed fixed-dose combination of ROS and metformin HCl (MET) to enhance ROS dissolution and oral bioavailability. This work highlights wet co-grinding as a simple, solvent-minimized approach for improving the biopharmaceutical performance of ROS while supporting fixed-dose combination development. Rosuvastatin/metformin (ROS/MET) co-processed systems were prepared using a solvent-minimized wet co-processing approach. The formulations were evaluated for drug content and characterized using Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), thermal analysis (DSC/TGA), and scanning electron microscopy (SEM). In vitro dissolution studies were performed to assess drug dissolution behavior. In vivo Comparative pharmacokinetic evaluation in rats (n = 3 per group) assessed oral bioavailability, In vitro-in vivo correlation (IVIVC) analysis and liver biodistribution, while anti-hyperlipidemic efficacy was assessed in hyperlipidemic rats (n = 6 per group) through biochemical and histopathological analyses. The co-processed mixtures significantly enhanced rosuvastatin dissolution, with the 20:500 ROS ratio (F2) showing the best performance. Across pH 1.2, 4.5, and 6.8, F2 achieved Q5 values of 73.6%, 82.5%, and 92.7%, respectively, compared with 12.4%, 19.9%, and 28.6% for unprocessed ROS. Correspondingly, dissolution efficiency increased from 21.3-42.6% for ROS to 76.2-90.4% for F2. Comparative pharmacokinetic evaluation revealed a 21.5% increase in relative bioavailability, a 1.34-fold increase in Cmax, and a more rapid onset of action compared to unprocessed rosuvastatin. Additionally, the co-processed F2 demonstrated improved liver drug distribution and superior anti-hyperlipidemic effects in poloxamer 407-induced hyperlipidemic rats. The co-processing of rosuvastatin with metformin presents a solvent-minimized and effective strategy to enhance the dissolution, bioavailability, and therapeutic efficacy of rosuvastatin. This approach holds promise for the clinical management of complex conditions such as dyslipidemia and type 2 diabetes mellitus.

PMID 42454697
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