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rosuvastatin + ezetimibe (ID 1805 / ID1805 / Droptop)

✓ Approved

Ildong Pharmaceutical · HMGCR · Small Molecule

What is rosuvastatin + ezetimibe?

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

Drug Profile

Brand NamesID 1805, ID1805, Droptop
CompanyIldong Pharmaceutical
Drug ClassSmall Molecule
Molecular TargetHMGCR, NPC1L1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Ildong Pharmaceutical

Mechanism of Action

Molecular Targets

rosuvastatin + ezetimibe 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

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

Therapeutic AreaConditionPhase
Metabolism and nutrition disordersHypercholesterolaemia✓ Approved

Related Research Articles

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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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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PubMedDrug delivery and translational research2026-09-17

Chitosan-TPP modification of SNEDDS enhances mucin interaction, apparent epithelial transport, and oral exposure of ezetimibe.

Lee Ju Young JY, Song Ji Ho JH, Cho Jung Hyun JH

Poor aqueous solubility limits the oral absorption of ezetimibe, and conventional self-nanoemulsifying drug delivery systems (SNEDDS) primarily address the solubilization barrier. In this study, ezetimibe-loaded SNEDDS were associated with a chitosan-tripolyphosphate (TPP) ionic network to generate chitosan-TPP-modified SNEDDS colloids (CS-SNEDDS) with additional mucin-interactive characteristics. The resulting CS-SNEDDS had a mean particle size of approximately 142 nm and a positive zeta potential, while retaining the apparent solubilization and rapid dispersion properties of the SNEDDS component. Compared with conventional SNEDDS, CS-SNEDDS showed markedly greater mucin association and increased apparent apical-to-basolateral transport across Caco-2 monolayers. Following oral administration to rats, CS-SNEDDS produced an AUC₀-₂₄h of 4715.62 ± 854.07 ng·h/mL, compared with 3647.39 ± 753.54 ng·h/mL for SNEDDS and 2176.84 ± 426.58 ng·h/mL for crystalline ezetimibe. The AUC₀-₂₄h of CS-SNEDDS was significantly higher than that of SNEDDS, whereas no significant difference in Cmax was detected between the two nanoformulations. These findings indicate that chitosan-TPP modification of ezetimibe-loaded SNEDDS introduced mucin-interactive cationic properties and was associated with an additional improvement in apparent epithelial transport and systemic exposure beyond that achieved by SNEDDS alone. This lipid-polymer interfacial modification strategy may provide a useful formulation approach for improving the oral delivery of poorly water-soluble drugs.

PMID 42749906
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PubMedJournal of controlled release : official journal of the Controlled Release Society2026-09-17

ROS-responsive bionanodrug for atherosclerosis therapy via regulating glycolipid metabolism and cell crosstalk.

Yu Jie J, Dong Xiaoyan X, Yu Feifei F, Wu Yizhou Y et al.

Atherosclerosis (AS) is a long-term inflammatory disorder marked by dysfunctional glycolipid metabolism, abnormal inflammatory response and intercellular crosstalk. Rosuvastatin (RSV), a first-line drug with lipid-lowering activity, fails to adequately modulate the inflammatory microenvironment of atherosclerotic plaques. The natural active ingredient shikonin (SKN) compensates for this limitation through inhibiting glycolysis and anti-inflammation. However, how to efficiently co-delivery them to the plaques remains challenging. In this, we engineered a ROS-responsive nanosystem (TK-MLP@SR NPs) containing SKN and RSV. This system enables drugs release in the plaque microenvironment with high ROS levels, prolongs circulation time, and achieves active lesion targeting. In vitro assay indicated the function of TK-MLP@SR NPs for inhibiting glycolysis and promoting fatty acid oxidation (FAO) in homocysteine-treated macrophages, thereby inhibiting foam cell formation and alleviating inflammation. Moreover, this nanosystem inhibited phenotype switch of vascular smooth muscle cell by restoring normal macrophage - smooth muscle cell crosstalk. In ApoE-/- mice, the accumulation of TK-MLP@SR NPs in the plaque reduced macrophage infiltration, thereby modulating the inflammatory microenvironment to restore smooth muscle cell function and improved the plaque stability, characterized by less lipid deposition, and increased collagen, along with smaller necrotic cores. Compared with free drugs, this strategy exhibited superior efficacy in regulating the plaque microenvironment by inhibiting lipid deposition. In summary, this work introduces a novel plaque environment-activated prodrug platform, providing valuable insights for clinical translation of AS therapy.

PMID 42753822
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PubMedAnnals of internal medicine2026-09-15

A Synopsis of the 2025 U.S. Department of Veterans Affairs and U.S. Department of Defense Clinical Practice Guideline for Lipid Management for Cardiovascular Disease Risk Reduction.

Arnold Michael J MJ, Spacek Lance L, Bush Kelvin N V KNV, Waring Ashley Arana AA et al.

In December 2025, the U.S. Department of Veterans Affairs (VA) and the U.S. Department of Defense (DoD) released a clinical practice guideline (CPG) update on lipid management for cardiovascular disease risk reduction in adults. This synopsis reviews the 2025 updates and describes the major recommendations. The VA/DoD guideline development team updated the 2020 VA/DoD lipid management CPG with clinical stakeholders. The guideline panel developed 12 key questions, systematically evaluated the literature (English-language publications from 16 May 2019 to 15 January 2025), and developed 24 evidence-based recommendations. The recommendations were graded using the GRADE (Grading of Recommendations Assessment, Development and Evaluation) system. This synopsis highlights key recommendations for lipid management that are new or differ from other guideline recommendations. This update recommends the Predicting Risk of Cardiovascular Disease EVENTs (PREVENT) calculator for risk estimation in primary prevention and removes a previous recommendation against routine lipid monitoring. Two new risk refinement strategies were added: Coronary artery calcium testing is suggested for patients with clinical uncertainty and intermediate-to-high calculated risk, and one-time lipoprotein(a) testing is recommended to identify patients with enhanced cardiovascular risk. For primary prevention, moderate-intensity statins remain the recommended treatment for those at higher risk and should be considered for those at intermediate risk. A new recommendation suggests moderate-intensity statins for adults living with HIV even when 10-year risk is low. This update shifts toward more intensive lipid-lowering therapy for secondary prevention. For very high-risk patients with atherosclerotic cardiovascular disease, the guideline now suggests combination therapy with high-intensity or maximally tolerated statins plus ezetimibe and/or proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors. For statin-intolerant patients, alternatives include bempedoic acid, ezetimibe, fibrates, or PCSK9 monoclonal antibody inhibitors.

PMID 42735406
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