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amlodipine besilate + irbesartan (DSP8153)

✓ Approved

Sumitomo Pharma Co., Ltd. · AGTR1 · 小分子

什么是 amlodipine besilate + irbesartan？

amlodipine besilate + irbesartan 是一种小分子，由Sumitomo Pharma Co., Ltd.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DSP8153
公司Sumitomo Pharma Co., Ltd.
药物类别小分子
分子靶点AGTR1, CACNA1C
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Sumitomo Pharma Co., Ltd.

作用机制

分子靶点

amlodipine besilate + irbesartan 作用于 2 个分子靶点：

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
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

amlodipine besilate + irbesartan 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedMedical sciences (Basel, Switzerland)2026-07-27

Real-World Pharmacotherapy-Driven Cardiovascular Risk Prediction Using Interpretable Machine Learning and Jordanian EHR Data.

Moshawih Said S, Gharaibeh Lobna L, Alfreahat Islam I, Shnoudeh Abeer Jabra AJ

Background: Cardiovascular disease (CVD) remains the leading cause of mortality worldwide, with over 75% of deaths occurring in low- and middle-income countries, where conventional risk models often demonstrate poor calibration and limited generalizability. Objective: This study aimed to develop an interpretable, pharmacotherapy-informed machine learning model for cardiovascular risk prediction using national electronic health record (EHR) data from Jordan. Methods: A retrospective cohort study was conducted using approximately 600,000 individuals from the national Hakeem EHR system (2018-2022). Demographic, clinical, blood pressure, laboratory, and medication data were integrated to construct three datasets reflecting varying levels of feature completeness. Multiple machine learning models were benchmarked, followed by optimization, hybrid modeling, and probability calibration. Model interpretability was assessed using SHAP analysis. Results: The national cohort demonstrated a high cardiometabolic burden, with prevalence of hypertension (50.2%), hyperlipidemia (54.9%), and diabetes (47.9%). Antihypertensive and lipid-lowering therapies were more frequently used among CVD patients (56.9% and 49.6%, respectively). Treatment patterns were dominated by amlodipine (19.9%) and atorvastatin (74.4%). The final calibrated seed-bagged gradient boosting model achieved robust performance (ROC-AUC 0.844; PR-AUC 0.813) with consistent generalization across datasets. Key predictors included antihyperlipidemic therapy, systolic blood pressure variability, age, and sex. Conclusions: This study presents JoRisk, a calibrated and interpretable machine learning framework that integrates pharmacotherapy and clinical data for short-term cardiovascular risk prediction. The model demonstrates strong performance using routinely available EHR variables and offers a scalable decision-support tool for risk stratification in resource-constrained healthcare systems.

PMID 42506312
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PubMedChannels (Austin, Tex.)2026-07-26

Research progress on the role and mechanism of STIM and Orai protein-mediated store-operated calcium entry in cardiovascular diseases.

Liao Xin X, Pan Chenglin C, Guo Xueqing X, Cheng Jun J

Store-operated calcium entry (SOCE) mediated by STIM and Orai proteins is a fundamental Ca2+ influx mechanism that critically regulates intracellular calcium homeostasis and participates in cardiovascular pathophysiology. Upon endoplasmic reticulum Ca2+ store depletion, STIM1/2 activate plasma membrane Orai1/3 channels, initiating Ca2+ entry that drives vasoconstriction, smooth muscle proliferation, platelet activation, and cardiac hypertrophy. Dysregulated SOCE is closely associated with hypertension, atherosclerosis, pulmonary hypertension, and thromboembolic disorders. However, SOCE is not a simple binary pathway but operates within a complex regulatory network. Beyond the core STIM-Orai axis, auxiliary proteins including transient receptor potential canonical 1 (TRPC1), tetraspanin 18 (Tspan18), tropomyosin 3 (TPM3), SOCE-associated regulatory factor (SARAF), and A-kinase anchoring protein 79/150 (AKAP79/150) modulate SOCE amplitude, kinetics, and downstream signaling in a cell- and context-dependent manner. Moreover, the functional consequences of SOCE are highly heterogeneous: Orai1 protects adult cardiomyocytes but promotes pathological hypertrophy in neonatal cells, posing a therapeutic dilemma. Although preclinical studies have shown efficacy of SOCE inhibitors, clinical translation remains hindered by poor isoform selectivity, suboptimal pharmacokinetics, lack of tissue-specific delivery, disease-stage-dependent effects, and absence of validated biomarkers. Importantly, recent evidence has definitively ruled out amlodipine-induced CRAC channel activation at therapeutic concentrations, confirming it as an experimental artifact. This review systematically summarizes the molecular complexity, functional diversity, and translational barriers of STIM/Orai-mediated SOCE, aiming to inform precision therapeutic strategies for cardiovascular diseases.

PMID 42503223
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PubMedJournal of clinical hypertension (Greenwich, Conn.)2026-07-25

Serum Uric Acid Changes in Relation to Nighttime Blood Pressure Dipping Status in Patients on Antihypertensive Therapy.

Zhang Di D, Huang Qi-Fang QF, Li Yan Y, Wang Ji-Guang JG

We performed a post hoc exploratory secondary analysis to investigate whether baseline circadian blood pressure (BP) pattern was associated with changes in serum uric acid (SUA) during 8-week antihypertensive therapy. Of the 494 hypertensive patients who received amlodipine (5-10 mg) or nifedipine GITS (30-60 mg) for 8 weeks, 369 patients with available laboratory data and valid follow-up ambulatory BP monitoring data were included in the present analysis, including 221 dippers (nocturnal systolic BP decline ≥ 10%) and 148 non-dippers (nocturnal systolic BP decline < 10%). Analysis of covariance was used to estimate least square mean changes in SUA according to baseline dipping pattern. After 8-week antihypertensive treatment, SUA decreased significantly in dippers (-12.4 ± 3.4 µmol/L, p = 0.0004) but not in non-dippers (-3.3 ± 4.2 µmol/L, p = 0.44). In the repeated-measures analysis, SUA levels decreased significantly over time (p = 0.002), whereas no significant time-by-dipping interaction was observed (p = 0.23). Baseline BP dipping pattern may be modestly associated with short-term SUA changes during antihypertensive therapy. However, the absence of a significant time-by-dipping interaction suggests that these findings should be interpreted cautiously and require further confirmation.

PMID 42501048
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PubMedAnalytical science advances2026-07-23

Design-Assisted Chemometric UV Spectrophotometric Determination of Candesartan Cilexetil, Chlorthalidone and Amlodipine Using Principal Component Regression, Partial Least Squares and Genetic Algorithm-Partial Least Squares Models.

Amin Khanda F M KFM, Elagamy Samar H SH, Obaydo Reem H RH, Lotfy Hayam M HM

This study presents a sustainable chemometric-assisted UV spectrophotometric strategy for the simultaneous determination of candesartan cilexetil (CAN), chlorthalidone (CTL) and amlodipine (AML) in laboratory-prepared mixtures and commercial pharmaceutical formulations. Owing to the extensive spectral overlap of the three drugs in the UV region, conventional spectrophotometric methods are inadequate for their direct simultaneous analysis. To address this challenge, multivariate calibration models based on principal component regression (PCR), partial least squares (PLS) and genetic algorithm-optimized partial least squares (GA-PLS) were developed, enabling accurate quantification without prior separation or complex sample preparation. A design of experiments (DoE) approach was employed to construct the calibration set, while an independent validation set was generated using orthogonal array-based Latin hypercube sampling (OALHS) to ensure robust external validation across the concentration domain. The GA-PLS model enhanced predictive performance through effective wavelength selection, reducing spectral redundancy and improving model robustness. Furthermore, variable importance in projection (VIP) analysis was employed to identify the most influential spectral variables and provide insight into the spectral regions contributing to analyte quantification. The developed models exhibited excellent analytical performance, characterized by low calibration errors (root mean square error of calibration [RMSEC] < 0.30), strong predictive ability and satisfactory external validation results (RMSEP = 0.2278-0.4419; RRMSEP = 0.1558-0.3978), with recoveries ranging from 99.0% to 100.0%. The sustainability of the proposed methodology was assessed using the multi-colour assessment (MA) tool according to white analytical chemistry principles, yielding a high whiteness score and demonstrating superior environmental performance compared with conventional chromatographic methods. In addition, the graphical layout tool for analytical chemistry evaluation (GLANCE) visualization framework provided a comprehensive graphical assessment of analytical performance and sustainability metrics. The proposed chemometric strategy offers a rapid, reliable, cost-effective and environmentally friendly alternative for routine quality control of multicomponent pharmaceutical formulations.

PMID 42487652
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PubMedKidney international supplements2026-07-22

Approved therapies in the IgA nephropathy armamentarium: a summary of the evidence.

Norouzi Sayna S, Lafayette Richard A RA

Historically, IgA nephropathy (IgAN) was managed using supportive care, with a suggested 6 months of immunosuppressive therapy considered for patients at high risk of progressive kidney function decline (proteinuria, >0.75-1 g/d) despite ≥90 days of optimized supportive care. The evolving treatment landscape includes agents that target immunologic aspects of IgAN or better preserve kidney function, or both. Recent approvals include Nefecon, sparsentan, iptacopan, atrasentan, and sibeprenlimab. Nefecon, a targeted-release formulation of budesonide, is the only US Food and Drug Administration and European Medicines Agency fully approved agent that is designed to target the primary source of IgAN: galactose-deficient IgA1 production in the gut mucosa. Phase 3 data showed that Nefecon slowed estimated glomerular filtration rate decline and decreased proteinuria versus placebo, with an acceptable safety profile. Sparsentan, a fully US Food and Drug Administration- and European Medicines Agency-approved dual endothelin A/angiotensin II receptor antagonist, affects the generic responses to IgAN-induced nephron loss, potentially including glomerular inflammation and fibrosis. Sparsentan demonstrated a significant reduction in proteinuria and estimated glomerular filtration rate decline compared with irbesartan. Iptacopan inhibits complement factor B and has received accelerated US Food and Drug Administration approval. Interim phase 3 study data have shown that iptacopan significantly reduces proteinuria when compared with placebo. The endothelin A receptor antagonist atrasentan and A proliferation binding ligand inhibitor sibeprenlimab have also received accelerated US Food and Drug Administration approval, based on interim phase 3 results showing significant proteinuria reduction versus placebo in patients with IgAN. This expanded clinical armamentarium offers clinicians and patients greater choice and improved disease control in IgAN management.

PMID 42483539
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PubMedClinical cardiology2026-07-21

Clinical Presentation and Treatment Response in Women With Acetylcholine-Confirmed Coronary Spasm: A Single-Center Observational Study.

Sikulu Josephine J, Kubini Ralf R, Turkman Muath M, Immohr Moritz Benjamin MB et al.

Coronary vasomotor disorders are frequently underdiagnosed in women with angina and non-obstructive coronary arteries. We investigated clinical presentation, diagnostic delay, spasm subtype, and patient-reported treatment response in women with acetylcholine-confirmed coronary spasm. This single-center observational study included women with a positive intracoronary acetylcholine provocation test who completed a locally developed questionnaire on symptoms, triggers, comorbidities, medication tolerance, and treatment response. Epicardial spasm was defined as ≥ 90% epicardial diameter reduction with symptom reproduction and ischemic ECG changes; microvascular spasm as symptoms and ischemic ECG changes with < 90% epicardial vasoconstriction. Diltiazem was initiated as first-line therapy, with amlodipine as an alternative. Regression analyses exploring therapeutic failure were considered exploratory because of the low event count. A total of 194 women were included (median age 60 years [IQR 52-67]). Chest pain/tightness was reported by 163/190 (85.8%), dyspnea by 70/135 (51.9%), and palpitations by 74/136 (54.1%). Epicardial/microvascular spasm was present in 110/187 (58.8%) and 77/187 (41.2%). Median symptom-to-diagnosis time was 24 months [IQR 8-90]. Diltiazem was prescribed in 162/194 (83.5%). Among respondents with follow-up data, symptom frequency decreased in 103/128 (80.5%), episode duration decreased in 91/118 (77.1%), and pain intensity decreased/resolved in 92/115 (80.0%). Therapeutic failure occurred in 8/106 (7.5%). Residual symptom burden remained common, with CCS class > II at follow-up in 65/124 (52.4%) and persistent complaints in 53/107 (49.5%). In women with acetylcholine-confirmed coronary spasm, symptom burden and diagnostic delay were substantial. Calcium-channel blocker therapy was associated with patient-reported symptom improvement among respondents with available follow-up data.

PMID 42478585
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