JW Pharmaceutical · AGTR1 · 小分子
pitavastatin + valsartan 是一种小分子，由JW Pharmaceutical研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。
| 商品名 | Livalsartan, Livasartan |
| 公司 | JW Pharmaceutical |
| 药物类别 | 小分子 |
| 分子靶点 | AGTR1, HMGCR |
| 给药途径 | Oral (PO) |
| 状态 | Approved |
pitavastatin + valsartan 作用于 2 个分子靶点：
| AGTR1 | angiotensin II receptor type 1 (HAT1R, AT1) |
| HMGCR | 3-hydroxy-3-methylglutaryl-CoA reductase (LDLCQ3, LGMDR28) |
pitavastatin + valsartan 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 |
|---|---|---|
| Metabolism and nutrition disorders | Hypercholesterolaemia | ✓ Approved |
| Vascular disorders | Hypertension | ✓ Approved |
Steinberg Daniel I DI, ACP Journal Club Editorial Team at McMaster University
GIM/FP/GP: [Formula: see text] Cardiology: [Formula: see text].
Su Tong T, Jia Tiantian T, Xu Danping D
Ozaki Aya F AF, Nomura Hisanaga H, Terada Tomohiro T, Kato Eri T ET et al.
Sacubitril/valsartan (S/V) is an established therapy for heart failure that has been recently approved for hypertension in Japan. However, evidence regarding its use in combination with other antihypertensive agents in real-world practice is limited. To describe real-world prescribing patterns of S/V among patients with hypertension in Japan. A retrospective cohort study using a nationwide Japanese electronic health record database (August 2020 to October 2023) identified adults with hypertension (ICD-10: I10-I15) who were newly prescribed S/V. Patients with heart failure were excluded. Concomitant antihypertensive medications, S/V dosing, and discontinuation patterns were assessed over 90 days following initiation. Of the 9,486 patients (median age 79 years; 50.6% men), 63.6% received S/V with a calcium channel blocker (CCB), 22.5% as monotherapy, and 11.8% as triple therapy with CCB and thiazide. At day 90, 55.5% of patients received S/V plus a CCB, and 26.0% were on S/V monotherapy. The S/V discontinuation rate reached 11.8% by day 90. Approximately half of those on triple therapy discontinued the thiazide diuretic within 30 days. In Japanese patients with hypertension, S/V is most commonly used in combination with a CCB, although a notable proportion receive it as monotherapy. These findings highlight the need for further studies to evaluate the safety, efficacy, and cost-effectiveness of S/V-based combination regimens.
Nogi Kazutaka K, Tanaka Atsushi A, Imai Takumi T, Doi Shunichi S et al.
Sacubitril/valsartan (Sac/Val) reduces N-terminal pro-B-type natriuretic peptide (NT-proBNP) levels in acute heart failure (AHF), particularly in patients with reduced ejection fraction. However, whether estimated total blood volume (TBV), calculated using anthropometric equations, is associated with heterogeneity in biomarker response remains uncertain. This post hoc exploratory sub-analysis of the PREMIER randomized trial evaluated whether baseline estimated TBV was associated with heterogeneity in NT-proBNP reduction after Sac/Val compared with angiotensin-converting enzyme inhibitor/angiotensin receptor blocker (ACEI/ARB) therapy. Estimated TBV was calculated using validated anthropometric equations and dichotomized at the median (4.05 L). Patients were further stratified by left ventricular ejection fraction (LVEF <40% vs. ≥40%). The primary endpoint was the proportional change in NT-proBNP from baseline to Week 8. Among 376 patients, 372 with baseline estimated TBV data were analyzed. In the high TBV group, Sac/Val was associated with greater NT-proBNP reduction than ACEI/ARB (-56% vs. -32%; ratio of change, 0.67; 95% confidence interval, 0.53-0.84; P=0.001), whereas no significant difference was observed in the low TBV group (P for heterogeneity=0.063). In patients with LVEF <40%, Sac/Val was associated with greater NT-proBNP reduction in both TBV groups. In patients with LVEF ≥40%, Sac/Val was associated with greater NT-proBNP reduction in the high TBV group, whereas the point estimate in the low TBV group numerically favored ACEI/ARB. In this exploratory post hoc analysis, higher estimated TBV was associated with greater NT-proBNP reduction after Sac/Val, particularly among patients with LVEF ≥40%. These findings are hypothesis-generating and require external validation. ClinicalTrials.gov, NCT05164653; Japan Registry of Clinical Trials, jRCTs021210046.
Gharat Mithun M MM, Roy Pallavi T PT, Gosar Amit N AN, Shaikh Tabrez A TA et al.
For many years, it is known as Nitrosamines are responsible for carcinogenicity in human. These nitroso-impurities were found detected in plastics, food items, cigarette, insect killer, water and alcoholic beverages. In 2018 EMA and USFDA claimed the presence of N-nitrosodimethylamine in valsartan used for the treatment of hypertension. Consequently, to assess the adverse effects of nitrosamine generation during storage, in the course of production, or through contaminated supply chains, regulators have issued many guidelines. Hence, there is a crucial need for accurate evaluation technique to measure nitroso-impurities in pharmaceutical products. According to the Carcinogenic Potency Categorization Approach, the allowable intake is 400 ng/day, which translates to an allowable limit of 16 ppm for a 25 mg daily dose. A study was then performed at 1.5 ppm relative to sample concentration, which is less than 10% of this limit. The main aim of this development to optimize and prove suitability of a new liquid chromatography-tandem mass spectrometry method for quantitatively analyzing 3-amino-N-nitrosopiperidine (NTPA) in Alogliptin Benzoate (AGP), achieving detectable response of 0.03 ppm and quantifiable response value of 0.1 ppm relative to sample concentration. Current method was found to be linear with the coefficient of regression of 0.9979. Also, spiking study was performed by the calculating percentage spiked NTPA in the drug, which ranged from 96.67% to 100.14%. The results confirmed that the methodology was reliable, precise, robust and reproducible to quantify NTPA at 1.5 ppm in samples of 2.75 mg/mL concentration.
Dai Lu L, Chen Guanglei G, Yang Yinan Y, Yan Yiping Y et al.
Immunoglobulin A nephropathy (IgAN), the most common primary glomerular disease and a leading cause of end-stage kidney disease (ESKD), is associated with cardiovascular and metabolic abnormalities. To explore these genetic overlaps, we integrated large-scale GWAS data from IgAN, 21 pan-vascular diseases (PVDs), 13 metabolic traits, 11 immune cell phenotypes, and established IgAN risk factors. Cross-trait analyses (LDSC, GNOVA, SUPERGNOVA) revealed significant genetic correlations between IgAN and multiple PVDs, including coronary artery disease, heart failure, stroke, aortic aneurysm, and varicose veins. Multi-omics prioritization (TWAS, SMR, MAGMA, and fastBAT) identified shared variants and candidate genes associated with immune regulation, lipid transport, and cardiovascular function. Gene expression profiling demonstrated enrichment of these genes in endothelial cells, macrophages, spleen, lung, and blood. Drug repurposing analysis based on gene-drug matching scores (>0.5) identified promising therapeutic candidates, including immunosuppressants (prednisolone, cyclosporine, azathioprine), lipid-lowering agents (pitavastatin, fenofibrate), and the antiplatelet drug aspirin. These findings offer novel opportunities for precision medicine and drug repurposing in IgAN patients with cardiometabolic disorders.
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