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

PubMedJournal of medical economics2026-06-09

Cost-effectiveness and budget impact of ezetimibe-atorvastatin single-pill combination versus free combination in Chinese adults with hypercholesterolemia.

Xing Qian Q, Cheng Wendi W, Wang Wei W, Ren Weiwei W et al.

Hypercholesterolemia imposes a growing cardiovascular burden in China, yet low-density lipoprotein cholesterol (LDL-C) target attainment remains low. The single-pill combination (SPC) of ezetimibe and atorvastatin (E/A SPC) was approved in China in 2023 and added to the National Reimbursement Drug List (NRDL) in 2024. Compared with free combination therapy (E/A FCT), E/A SPC may improve adherence and LDL-C reduction, but its economic value has not been assessed in the Chinese context. To evaluate the cost-effectiveness of E/A SPC versus E/A FCT in Chinese adults with hypercholesterolemia inadequately controlled on statin monotherapy, and to estimate the 5-year budget impact of E/A SPC adoption. An 11-state Markov model was developed from the Chinese healthcare system perspective, projecting 20-year costs and health outcomes in patients aged 69 years with uncontrolled LDL-C (>70 mg/dL) after statin therapy. Clinical efficacy inputs were derived from a large real-world German head-to-head study (n = 311,242). Subgroup analyses were conducted by age, sex, and cardiovascular risk. A 5-year budget impact analysis estimated the financial consequences of increasing E/A SPC uptake. Costs and outcomes were discounted at 5% annually. E/A SPC generated 0.06 additional quality-adjusted life years (QALYs) at an incremental cost of USD 250.12, yielding an incremental cost effectiveness ratio (ICER) of USD 4,070/QALY, well below the willingness-to-pay threshold of USD 14,423. The probability of cost-effectiveness was 91%. Subgroup analyses consistently favored E/A SPC, with the most favorable ICERs observed in very high-risk patients and middle-aged patients. Over 5 years, E/A SPC was associated with incremental drug spending of USD 372.5 million, partly offset by USD 292.0 million in avoided cardiovascular event costs. E/A SPC is a cost-effective strategy for Chinese adults with hypercholesterolemia inadequately controlled on statin monotherapy, supporting its NRDL inclusion. The study findings should be further validated using larger-scale real-world data from China.

PMID 42262268
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PubMedJournal of the American Heart Association2026-06-09

Electronic Health Record Alerts to Improve Lipid Lowering After a Recent Myocardial Infarction.

Karalis Dean G DG, Richter Benjamin B, Hessen Scott S, Moeller Patrick P et al.

This observational, quality initiative evaluated the impact of changing from a passive (dismissible) to an active (nondismissible without action) electronic health record alert on guideline-recommended lipid-lowering therapy (LLT) prescriptions in patients with recent myocardial infarction at risk for secondary events. We sequentially recruited a retrospective passive-alert (February 2018-July 2019; n=733) and a prospective active-alert (August 2020-January 2022; n=587) cohort of patients who triggered an alert to intensify LLT or order a low-density lipoprotein-cholesterol (LDL-C) test if they had a recent myocardial infarction (within 12 months) and elevated (≥70 mg/dL) or missing LDL-C. Prescribed LLTs and cumulative percentages of patients with missing or LDL-C <70 and <55 mg/dL were assessed in 6-month periods up to 24 months. Reasons for not intensifying LLTs were recorded with the active alert. During 24 months, statin and high-intensity statin use increased from 59% to 87% and from 39% to 69%, respectively, in the passive-alert cohort. In the active-alert cohort, statin and high-intensity statin use were high and changed minimally (79% to 80% and 70% to 73%), but ezetimibe and proprotein convertase subtilisin/kexin type 9 inhibitor use increased from 12% to 35% and from 2% to 8% (odds ratio, 4.69 [95% CI, 3.22-6.96] and 4.07 [95% CI, 1.92-9.46]), respectively. LDL-C testing and LDL-C goal attainment improved in both cohorts. LDL-C not current (41.7%) was the most common reason for not intensifying LLT. Continued efforts are needed to encourage guideline-directed LLT intensification for patients with a recent myocardial infarction who are at risk of another cardiac event.

PMID 42261954
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PubMedNutrition, metabolism, and cardiovascular diseases : NMCD2026-06-07

Effect of add-on PCSK9 inhibitors on endocan and arterial stiffness in heterozygous familial hypercholesterolemia: a two-lipid center real-world study.

Toscano Arianna A, Bosco Giosiana G, Di Giacomo Barbagallo Francesco F, Di Marco Maurizio M et al.

Endothelial dysfunction (ED) represents an early key event in atherogenesis. Our aim was to evaluate the efficacy of six months add-on PCSK9 monoclonal antibodies (mAbs) on endothelial function assessed by endocan plasma levels and PWV in a cohort of HeFH subjects; furthermore, we investigated the association of endocan lowering and PWV variation. In this prospective observational study, we evaluated 30 FH subjects on high-intensity statins plus ezetimibe and with an off-target LDL-C. All patients received PCSK9 mAbs therapy and obtained biochemical analysis as well as endocan measurement and PWV evaluation at baseline and after six months of PCSK9 mAbs. After six months of add-on PCSK9 mAbs therapy, a significant reduction of TC, LDL-C, Non-HDL-C, TG, Lp(a) and ApoB was observed; moreover, both PWV and endocan significantly improved after six months of treatment. Finally, univariate linear regression analysis showed that ΔPWV was significantly associated with ΔEndocan (p value < 0.001). PCSK9 inhibition was associated with significant improved endocan levels and PWV in a cohort of HeFH subjects. ΔEndocan was significantly associated with ΔPWV. Our exploratory findings demonstrate endothelial benefits of PCSK9 mAbs in addition to LDL-C lowering and support endocan and PWV as complementary markers of vascular response in FH.

PMID 42250972
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PubMedComparative biochemistry and physiology. Toxicology & pharmacology : CBP2026-06-06

Rosuvastatin calcium and pravastatin sodium regulate the antioxidant system in zebrafish liver through the PI3K/Nrf2/ARE signaling pathway.

Xie Y I N G YING, Wang X I A N R U I XIANRUI, Mu Q U A N L I N G QUANLING, Ding C U N B A O CUNBAO

Rosuvastatin calcium (ROV) and pravastatin sodium (PRA) are common drugs used for the treatment and prevention of cardiovascular diseases. They have been frequently detected in the global aquatic environment, but their toxic effects and molecular mechanisms on the antioxidant system of fish remain unclear. In this study, zebrafish were exposed to ROV or PRA for 48 h to investigate their effects on the hepatic antioxidant response system of zebrafish and the possible underlying molecular mechanisms. The results showed that after exposure to the two drugs, the levels of reactive oxygen species (ROS), glutathione (GSH), and malondialdehyde (MDA) increased, while the activities of catalase (CAT) and superoxide dismutase (SOD) were inhibited. Exposure to ROV (5 mg/L) upregulated the activities of glutathione peroxidase (GPx) and glutathione S-transferase (GST), as well as the mRNA levels of phosphatidylinositol 3-kinase (PI3K) and CAT. However, the protein levels of nuclear factor erythroid 2-like protein (Nrf2) and SOD were suppressed. Exposure to PRA (10 mg/L) also increased the mRNA levels of PI3K, CAT, and GPx, while inhibiting Nrf2 and SOD proteins. The inhibitory effects on Nrf2 and SOD proteins were reversed after the addition of the PI3K activator 740YP. Molecular docking showed that both ROV and PRA could bind stably to PI3K. In conclusion, both ROV and PRA can induce hepatic oxidative damage in zebrafish, and the mechanism may be related to the disruption of the PI3K-mediated Nrf2/ARE pathway.

PMID 42248540
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PubMedAnnals of the Academy of Medicine, Singapore2026-06-06

Singapore expert consensus on optimising lipid-lowering strategies in acute coronary syndrome: A modified Delphi study.

Tan Ru San RS, Yap Jonathan J, Yeo Colin C, Poh Kian Keong KK et al.

Acute coronary syndrome (ACS) carries a high early risk of recurrent events, yet time-to-target low-density lipoprotein cholesterol (LDL-C) is often prolonged, and goal attainment is suboptimal in real-world practice. The authors aimed to develop expert consensus recommendations for post-ACS lipid management in Singapore, focusing on LDL-C targets, pharmacotherapy, escalation strategies, and implementation tools to improve adherence and reduce therapeutic inertia. A modified Delphi methodology was employed with a panel of 10 members. Evidence was synthesised from guidelines, randomised trials, metaanalyses, and observational studies. Thirty-two statements were drafted across 5 domains (LDL-C targets; timing/ monitoring; pharmacotherapy; special populations; implementation/adherence/health-system strategies) and rated anonymously on a 5-point Likert scale. Consensus thresholds were defined as high (≥75% concordant), moderate (55-74%), and low (<55%). After the final round, 30 of 32 statements achieved high consensus, and 2 received low consensus. Key agreements included measuring lipids within 24 hours of admission and retesting at 4-6 weeks, early initiation of high-intensity statins, and upfront combination therapy with statin + ezetimibe when monotherapy is unlikely to achieve the goals. Consideration of a proprotein convertase subtilisin/kexin type 9 inhibitor at discharge was recommended if LDL-C remained >1.4 mmol/L. Special considerations included older adults, familial hypercholesterolaemia, lower statin adherence among women, and the role of lipoprotein(a). The panel recommended adopting objective metrics, integrating electronic health record prompts, and developing localised pathways to harmonise care transitions. The consensus recommendations provide a tailored approach for Singapore, emphasising early action, proactive escalation, and systems-level interventions to improve post-ACS outcomes.

PMID 42249756
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PubMedClinica e investigacion en arteriosclerosis : publicacion oficial de la Sociedad Espanola de Arteriosclerosis2026-06-06

Inclisiran for LDL-C reduction in secondary prevention: Real-world evidence from a homogeneous Spanish cohort with subgroup insights.

Piro Victoria V, Fuente Elena E, Romano Francisco F, Galván Mario M et al.

Inclisiran produces sustained LDL-C lowering in clinical trials. Real-world evidence in homogeneous secondary prevention populations is limited. To evaluate the early effect of inclisiran on LDL-C in a homogeneous secondary prevention cohort with coronary artery disease. We conducted a retrospective, observational study of 120 adults with established atherosclerotic cardiovascular disease treated with inclisiran between December 2023 and August 2025 at a tertiary care center in Spain. Baseline and 90-day lipid profiles were compared. Subgroup analyses examined LDL-C reduction by sex, type 2 diabetes, statin, ezetimibe, and bempedoic acid use, as well as Lp(a) and remnant cholesterol (RC) levels. Mean baseline LDL-C was 126.1±34.7mg/dL (3.26±0.90mmol/L), decreasing to 45.3±28.3mg/dL (1.17±0.73mmol/L) at 90 days (absolute change -80.9mg/dL; -2.09mmol/L, -63.8%). The therapeutic target, <55mg/dL (<1.4mmol/L), was achieved by 64.5%. Statin users had significantly greater reductions (p<0.01). LDL-C lowering was similar across sexes despite higher baseline levels in women, and slightly greater in patients with diabetes (p=0.48). Elevated Lp(a) showed a weak inverse correlation with LDL-C change although a trend was shown (r=-0.18). RC fell by 16.6% (p=0.008). Bempedoic acid users (n=16) had numerically greater reductions, though not statistically significant probably due to the low n of patients. Inclisiran was well tolerated in this cohort, with no significant adverse events reported. Inclisiran achieved marked LDL-C reductions at 90 days in real-world secondary prevention, especially with the concurrent use of statins. Its twice-yearly dosing and favorable safety profile, in the term observed, support integration into guideline-directed therapy. Larger, longer-term studies should assess durability of effect, long term adherence and the impact on cardiovascular outcomes.

PMID 42248700
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