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

PubMedLipids in health and disease2026-09-20

Real-world use of bempedoic acid for hypercholesterolaemia: a German multicentre, retrospective, cohort study.

Haberbosch Linus L, Baessler Andrea A, de Ruiter Ulrike U, Sinning David D et al.

Dyslipidaemia remains a leading cause of death in Germany despite an improving therapeutic landscape, with many patients not achieving guideline-recommended low-density lipoprotein cholesterol (LDL-C) goals. Bempedoic acid, an adenosine triphosphate citrate lyase inhibitor, is a recent addition to the therapeutic landscape with proven efficacy in randomised controlled trials; however, its use varies between centres. We aimed to assess the short-term, real-world effectiveness of bempedoic acid in lowering LDL-C levels in patients in Germany. This retrospective, observational study was conducted using data from patients with primary hypercholesterolaemia or mixed dyslipidaemia, collected before and approximately 3 months after initiating bempedoic acid in 7 specialised lipid outpatient clinics in Germany. Data were analysed from a total of 641 patients, with a mean age (standard deviation [SD]) of 63.2 (11.3) years. The addition of bempedoic acid significantly reduced LDL-C levels from a mean of 133.6 mg/dL at baseline to 101.8 mg/dL after 3 months (p < 0.001). The mean within-patient LDL-C reduction was 31.8 mg/dL and the mean patient-level percentage change was -17.5%. Mean patient-level changes were -4.9% for HDL-C and -12.0% for total cholesterol; triglycerides did not change significantly. At 3 months, patients not receiving any lipid-lowering therapy (LLT) other than bempedoic acid had a mean patient-level LDL-C reduction of 27.1%; corresponding mean reductions were 23.7% with ezetimibe, 20.3% with PCSK9 inhibitor therapy, 9.0% with statin therapy and 6.1% with statin plus ezetimibe. Suspected adverse events were documented in 218/641 patients (34.0%), and 171/641 (26.7%) had discontinued bempedoic acid by follow-up. Myalgia was the most commonly reported adverse event in patients discontinuing treatment (75 cases). Findings from this real-world, multicentre study conducted in Germany show that bempedoic acid may present an effective treatment option for patients with hypercholesterolaemia who are already receiving LLT, in addition to being an effective option for patients not receiving/tolerating other LLTs. The magnitude of LDL-C reduction differed across background treatment strategies, while suspected adverse events and treatment discontinuation were common in this specialist-care cohort.

PMID 42763399
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PubMedJournal of geriatric cardiology : JGC2026-09-19

Safety and efficacy of low-density lipoprotein-lowering drugs in the elderly: a network meta-analysis of randomized controlled trials.

Niaga Karmenia Jessica Kurnia KJK, Supinto Pedro Arruda PA, Tjandra Kevin Christian KC, Martin Alfianto A et al.

Balancing the efficacy of low-density lipoprotein (LDL) reduction with safety presents a significant challenge in the elderly care. While guidelines recommended high-intensity statins as the optimal strategy to lower LDL in high-risk individuals, there are prevailing concerns regarding its side effects and subsequent fatality rate. The effectiveness of different LDL-lowering therapies in this population is also unclear. This study aims to compare the safety and efficacy of various LDL-lowering strategies in elderly population. A systematic search was conducted through six databases until March 2025. Randomized controlled trials (RCTs) that evaluate LDL-lowering agents were included. The primary outcome was adverse effects, while secondary outcomes included composite cardiovascular disease (CVD) events, CVD related mortality, all-cause mortality, and LDL level reduction. Risk of bias was assessed using the RoB-2 tool. A network meta-analyses were performed to compare the safety and efficacy with subgroup analysis based on underlying CVD under the cumulative ranking values. Sixteen RCTs (n = 43,625) with low to moderate risk of bias were included. Among interventions evaluated for adverse events, moderate-intensity pitavastatin had the highest probability of being the safest. Ezetimibe demonstrated the most favorable safety profile for reducing CVD mortality, while evolocumab was most effective in lowering all-cause mortality. For LDL reduction, the combination of moderate-intensity pitavastatin and ezetimibe was the most effective, followed by moderate-intensity rosuvastatin plus ezetimibe. Subgroup analyses revealed significant differences between CVD and non-CVD populations in CVD mortality (P = 0.0059), CVD events (P = 0.0096), and LDL reduction (P = 0.0100), with more pronounced effects in the non-CVD group, suggesting greater efficacy in primary prevention. Moderate-intensity pitavastatin showed the highest safety profile, while its combination with ezetimibe was the most effective for LDL reduction.

PMID 42760936
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PubMedSeminars in oncology2026-09-19

Rhabdomyolysis resulting from the interaction of rosuvastatin and abiraterone: A case study.

Blagojevic Christina C, Kim Richard B RB, Juurlink David N DN, Zipursky Jonathan S JS

Abiraterone is a first-line therapy for metastatic castrate-resistant prostate cancer. In vitro, abiraterone metabolites inhibit OATP1B1, the primary hepatic uptake transporter for several substrates, including statins. We describe the case of a 70-year-old man taking rosuvastatin who commenced treatment with abiraterone for metastatic castrate-resistant prostate cancer. Two months later, he presented to hospital with nonspecific symptoms including fatigue and diffuse myalgias with laboratory evidence of rhabdomyolysis and associated acute kidney injury. Plasma rosuvastatin concentrations were more than 40-fold higher than expected for the dose. Subsequent pharmacogenetic testing showed the patient was heterozygous for SLCO1B1*15, a variant of the SLCO1B1 gene encoding OATP1B1, which results in moderately reduced OATP1B1 transport activity. Considering the high frequency of statin prescribing, clinicians should be aware of the possible drug-drug interactions between statins and abiraterone and the associated risk of rhabdomyolysis, which is also affected by genetic differences.

PMID 42762808
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PubMedMethodist DeBakey cardiovascular journal2026-09-19

Familial Hypercholesterolemia.

Iatan Iulia I, Genest Jacques J

Familial hypercholesterolemia (FH) is a semi-dominant, autosomal, monogenic lipoprotein disorder characterized by severe elevations in low-density lipoprotein cholesterol (LDL-C) and premature atherosclerotic cardiovascular disease (ASCVD). The most common form, heterozygous FH, has an estimated prevalence of approximately 1 per 311 individuals, making it one of the most common hereditary disorders in medicine. FH is caused by pathogenic variants in the LDL receptor (LDLR) gene, or in genes encoding proteins involved in receptor-mediated LDL particle uptake, including apolipoprotein B (APOB) and proprotein convertase subtilisin/kexin type 9 (PCSK9). Other genes account for a minority of cases. Diagnosis is based on LDL-C levels, a family history of elevated LDL-C or premature ASCVD, supportive physical findings such as tendinous xanthomas, and, when available, molecular confirmation of a pathogenic FH-causing variant. Prompt recognition and treatment with statins, often combined with ezetimibe, modifies the natural course of the disease. Sex differences in FH diagnosis and treatment are widely reported, with women diagnosed later and treated less intensively than men. PCSK9 inhibitors are often required in patients with FH who meet criteria for treatment intensification. In statin-intolerant patients, bempedoic acid may provide additional therapeutic options. The most severe form, homozygous FH (HoFH), has an estimated prevalence of ~1 in 367,000 individuals and is associated with ASCVD in youth, calcific aortic stenosis, and a markedly reduced life expectancy. Patients with HoFH require specialized care and may need LDL apheresis and specific orphan drugs such as lomitapide or evinacumab.

PMID 42761917
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PubMedCJC open2026-09-18

Rationale and Design of the Canadian Lipoprotein(a) Registry.

Kramer Adam I AI, Abdel-Qadir Husam H, Abramson Beth L BL, Baass Alexis A et al.

Lipoprotein(a) [Lp(a)] is an independent, heritable risk factor for atherosclerotic cardiovascular disease. Guidelines recommend Lp(a) testing once in a lifetime and recognize it as a risk-enhancing factor. However, management of elevated Lp(a) in real-world clinical practice is not well described. Here we describe the rationale, design, and preliminary baseline characteristics of the Canadian Lp(a) Registry, a prospective, longitudinal observational study of patients with Lp(a) ≥ 100 nmol/L (≥ 50 mg/dL). Patient demographics, cardiovascular risk factors, laboratory results, and clinical outcomes are collected at baseline and at annual follow-up. The primary objective is to evaluate the clinical management and outcomes of patients with elevated Lp(a). From April 2024 to April 2025, 127 patients (mean age 57.5 ± 12.7 years, 48.8% female) were enrolled with a median Lp(a) level of 225 nmol/L (interquartile range 186-346 nmol/L), and 51.2% had multiple Lp(a) levels obtained. The most recent mean low-density lipoprotein cholesterol (LDL-C) was 2.49 ± 1.74 mmol/L. At the time of registry entry, 104 (81.9%) patients were receiving lipid-lowering therapies, including statins (74.8%), ezetimibe (48.0%), and proprotein convertase subtilisin/kexin type 9 inhibitors (27.6%), whereas 18.1% were not taking prescription lipid-lowering therapy. There were 66 (52.0%) patients with an LDL-C < 2.0 mmol/L. The Canadian Lp(a) Registry is an ongoing prospective, observational study designed to evaluate the clinical management, cardiovascular risk profile, and outcomes for patients with elevated Lp(a). It is expected to improve our understanding of how elevated Lp(a) is managed in contemporary clinical practice and to identify opportunities to improve care.

PMID 42756755
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PubMedInternational journal of cardiology. Cardiovascular risk and prevention2026-09-17

Real-world patterns in lipid profile testing and lipid-lowering therapy in hospitalized patients: The Jurasz Lipid Study.

Ostrowska Małgorzata M, Ratajczak Jakub J, Ziółkowski Marcin M, Adamski Piotr P et al.

The aim of the Jurasz Lipid Study was to provide real-world evidence on lipid profile testing, as well as the prevalence of lipid-lowering therapy (LLT) in consecutive patients hospitalized in a tertiary multi-specialist hospital in Poland. A total of 40,646 patients were hospitalized across all analyzed departments. The majority of patients hospitalized in the cardiology and neurology departments underwent lipid profile evaluation (93.6% and 95.0%, respectively), while it was rarely performed in surgical department (14.9%). Patients receiving LLT, compared with untreated patients, more frequently had a history of atherosclerotic cardiovascular disease (ASCVD) and lipid profile testing. The prevalence of LLT use ranged from 0.1% in pediatrics to 35.1% in vascular surgery, 37.1% in neurology, up to 65.7% in cardiology and 69.1% in the cardiac surgery department. Statin monotherapy remained the standard of care, with atorvastatin and rosuvastatin being the most frequently used agents. The proportion of patients receiving high-intensity statin therapy ranged from 29.2% in neurology to 71.7% among ASCVD patients in cardiology. The combination of a statin with ezetimibe was used in up to 36.1% of ASCVD patients hospitalized in cardiology. Other LLT combinations were rarely observed. Lipid profile evaluation was routinely performed by cardiologists and neurologists, but rarely ordered by surgeons. The majority of patients with ASCVD were treated with LLT, but only up to 29.4% achieve treatment goals. Statin monotherapy remained the cornerstone of LLT. Statin with ezetimibe was the most common therapeutic combination.

PMID 42751564
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