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fimasartan + rosuvastatin (Tubero / Tuvero)

✓ Approved

Boryung · AGTR1 · 小分子

什么是 fimasartan + rosuvastatin？

fimasartan + rosuvastatin 是一种小分子，由Boryung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Tubero, Tuvero
公司Boryung
药物类别小分子
分子靶点AGTR1, HMGCR
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Boryung

作用机制

分子靶点

fimasartan + rosuvastatin 作用于 2 个分子靶点：

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
HMGCR3-hydroxy-3-methylglutaryl-CoA reductase (LDLCQ3, LGMDR28)
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

fimasartan + rosuvastatin 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Vascular disordersHypertension✓ Approved
Metabolism and nutrition disordersHyperlipidaemiaPhase III

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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PubMedJournal of clinical lipidology2026-09-08

Efficacy and safety of add-on bempedoic acid on maximal dose of rosuvastatin and ezetimibe in patients with established coronary artery disease (ADDBEMPERE study).

Garg Naveen N, Jaiswal Amit A, Kapoor Aditya A, Tewari Satendra S et al.

Bempedoic acid (BA) has emerged as an add-on therapy to statin and ezetimibe combination to achieve low-density lipoprotein cholesterol (LDL-C) targets. Data are limited regarding the efficacy and safety of adding BA in patients who are receiving the maximal dose of rosuvastatin in combination with ezetimibe. This study evaluated the efficacy and safety of adding bempedoic acid on the maximal dose of rosuvastatin with ezetimibe to achieve LDL cholesterol target in patients with established CAD. Postcoronary angioplasty patients having LDL >70 mg/dL despite being on a stable dose of ezetimibe and rosuvastatin (40 mg) combination were initiated on BA. Follow-up was done at 12, 24, and 48 weeks. Efficacy of BA was assessed by changes in lipid parameters. Safety assessments included clinical adverse events and changes in laboratory parameters. Adverse events of special interest included musculoskeletal safety, uric acid levels, hepatic and renal safety, and new-onset diabetes. The study involved 322 patients. Baseline LDL-C was 82.1 ± 15.6 mg/dL (mean ± SD) and was reduced to 57.6 ± 32.0 (-29.8%) at 12 weeks (P < .001) without any further significant reduction. LDL-C levels of <70 and <55 mg/dL were achieved in 84.8% and 69.6% patients, respectively, at 48 weeks. However, LDL-C levels of <30 mg/dL were achieved only in 14.6% patients. A significant reduction in high-sensitivity C-reactive protein was observed. A significant increase in uric acid was noted. However, clinical gout occurred in only 3 patients. None of our patients developed myopathy, new-onset diabetes, hepatic or renal impairment. Addition of BA to the full dose of rosuvastatin and ezetimibe leads to a significant reduction in LDL-C. Benefits start early and are sustained. Therapy is well tolerated.

PMID 42711169
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PubMedCardiovascular drugs and therapy2026-09-07

Efficacy and Safety of Fixed-Dose Combination Therapy with Cilostazol and Rosuvastatin in Patients with Symptomatic Lower Extremity Peripheral Artery Disease: A Multicenter Randomized Controlled Trial.

Kemalasari Adelin Dhivi AD, Suh Dong Woo DW, Jin In Tae IT, Lee Seung-Jun SJ et al.

To evaluate whether combined cilostazol and rosuvastatin therapy improves health-related quality of life, walking performance, and lipid profiles compared with rosuvastatin alone in patients with symptomatic lower extremity peripheral artery disease (PAD). This multicenter, double-blind, randomized placebo-controlled trial enrolled 260 patients with chronic lower extremity PAD (Rutherford category 2 or 3) at 52 sites in Korea. Participants were randomly assigned (1:1) to receive cilostazol 200 mg plus rosuvastatin or a matching placebo plus rosuvastatin for 24 weeks. The primary endpoint was the change in the Korean Peripheral Artery Questionnaire (KPAQ) summary score from baseline to week 24. A total of 257 patients were included in the full analysis set. The combination therapy group showed significantly greater improvement in the KPAQ summary score than in the rosuvastatin monotherapy group (least-squares mean change: 15.4 vs. 10.3 points; between-group difference 5.1 points, 95% confidence interval 1.5-8.7; P = 0.005). The treatment effect became statistically significant at week 12 and continued to increase through week 24. Treadmill walking distances improved in both groups; improvements were numerically greater with combination therapy but between-group differences were not significant at weeks 12 or 24. Compared with rosuvastatin monotherapy, combination therapy resulted in greater reductions in triglycerides and smaller increases in ApoB, together with greater increases in HDL cholesterol. Adverse events, adverse drug reactions, and discontinuations due to adverse events were numerically more frequent in the combination therapy group. Diarrhea was the only adverse event that occurred significantly more frequently, whereas no unexpected safety signals were observed. In patients with symptomatic PAD, the addition of cilostazol to rosuvastatin significantly improved patient-reported health status and provided additional favorable effects on atherogenic lipid profiles beyond rosuvastatin therapy alone. ClinicalTrials.gov, NCT07600385.

PMID 42704575
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PubMedEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2026-09-07

Novel inhibitors of BCRP found among drugs used in the treatment of cancer.

Timonen Martina M, Filppula Anne M AM, Hirvensalo Päivi P, Tornio Aleksi A et al.

Breast cancer resistance protein (BCRP) is an ATP-binding cassette transporter involved in clinically relevant drug-drug interactions. We aimed to identify new BCRP inhibitors among drugs used in cancer treatment. Accordingly, 133 drugs were screened at 50 µM for inhibition of BCRP using vesicular transport assay. Half-maximal inhibitory concentrations (IC50) were predicted, and compounds showing the highest inhibitory potencies relative to their systemic (I1) or intestinal (I2) concentrations were selected for experimental IC50 determination. A mechanistic static model was used to predict potential interactions with the BCRP substrate rosuvastatin in humans. Food and Drug Administration Adverse Event Reporting System (FAERS) was searched for signals of rosuvastatin-induced rhabdomyolysis during co-administration with the investigated drugs. Of the 133 drugs screened, 42 had a predicted IC50 value over 0.1×I₁ and 61 over 10×I₂, suggesting potential inhibition in humans. IC50 values were experimentally determined for 24 selected drugs. Cabozantinib and midostaurin were the strongest inhibitors, with IC50 values of 0.65 and 0.69 µM, respectively. Moreover, the model suggested that midostaurin, cabozantinib, and alpelisib could almost fully inhibit intestinal BCRP, nearly doubling rosuvastatin exposure (1.83- to 1.94-fold). Entrectinib, alpelisib, flutamide, abiraterone, and capecitabine were predicted to increase rosuvastatin exposure by 1.45- to 1.63-fold through BCRP inhibition. FAERS analysis indicated a higher frequency of rhabdomyolysis reports when abiraterone was co-administered with rosuvastatin compared with all reports without abiraterone, with a reporting odds ratio of 17.3. This study identified multiple previously unrecognized BCRP inhibitors, highlighting the potential for clinically relevant BCRP‑mediated drug-drug interactions in oncology patients.

PMID 42705394
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PubMedInternational immunopharmacology2026-09-06

Targeted drug delivery of rosuvastatin via nanoemulgel: A step towards more effective rheumatoid arthritis therapy.

Pathade Vrushali V, Nene Shweta S, Ratnam Shreya S, Tryphena Kamatham Pushpa KP et al.

The intent of the current study was the repurposing of rosuvastatin (RSV), an anti-hyperlipidemic drug, for the management of rheumatoid arthritis (RA). Transdermal delivery of RSV, a repurposed drug, loaded in nanoemulgel (NEG) improves the permeation of the drug through the skin and reaches the desired site of action. This thereby enhances the concentration of the drug at the site of action, reducing the side effects associated with other routes of delivery, further showing anti-inflammatory potential in the management of RA. Nanoemulsion (NE) was prepared by the spontaneous emulsification method. The globule size and polydispersity index of the developed NE were evaluated by Malvern ZetaSizer. Furthermore, RSV-NEG has been developed and characterized. In vivo efficacy of RSV-NEG was evaluated in complete Freund's adjuvant-induced RA in rats. Pro-inflammatory cytokine concentrations in rat serum were quantified by enzyme-linked immunosorbent assay. The globule size and polydispersity index of 0.4% w/w RSV NE were found to be 8.96 ± 0.19 nm and < 0.3, respectively. The developed NEG showed pseudoplastic shear thinning behavior and an average drug content of 97.54 ± 0.36%. The RSV demonstrated 28-fold higher permeation from RSV-NEG compared to free RSV gel. The animals treated with RSV-NEG exhibited anti-inflammatory potential along with significantly reduced (****p < 0.0001) paw thickness and arthritis scores compared to the negative control group. The promising findings with permeability after topical application and anti-inflammatory potential emphasize the ability of RSV-NEG to manage RA effectively.

PMID 42700513
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PubMedGenes to cells : devoted to molecular & cellular mechanisms2026-09-01

The HMG-CoA Reductase Inhibitor Fluvastatin Promotes Th2-Skewed Immune Responses by Modulating Dendritic Cell Differentiation.

Ishikawa Satoshi S, Mizuno Haruka H, Murase Kanon K, Sasano Kazuki K et al.

Statins, inhibitors of HMG-CoA reductase, exert immunomodulatory effects beyond lipid lowering, yet how they regulate T helper (Th) cell differentiation remains poorly understood. We show that fluvastatin administration to C57BL/6 mice for 7 days suppressed interferon-γ and elevated interleukin-4 production by splenic CD4+ T cells, shifting the immune balance toward Th2 without altering splenocyte numbers or major immune cell subset proportions. This effect was not shared by rosuvastatin, suggesting that lipophilicity-dependent cellular uptake influences immunomodulatory potency. In vitro experiments confirmed a direct Th2-promoting action of fluvastatin on CD4+ T cells. Basophils were excluded as mediating cells, as fluvastatin suppressed rather than enhanced basophil interleukin-4 production. Continuous fluvastatin exposure during granulocyte-macrophage colony-stimulating factor (GM-CSF)-driven dendritic cell (DC) differentiation altered the phenotype of the resulting DCs and markedly enhanced their Th2-polarizing capacity in co-cultures with antigen-specific CD4+ T cells. These functional changes were accompanied by alterations in DC surface molecule expression, although their causal contribution remains to be established. These findings indicate that continuous fluvastatin exposure during DC differentiation is associated with an altered DC phenotype and enhanced Th2-polarizing capacity.

PMID 42680200
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