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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

PubMedInternational journal of clinical pharmacology and therapeutics2026-08-03

Acquired apparent mineralocorticoid excess induced by compound glycyrrhizin tablets: A case report and literature review.

Li Yu Y, Du Juan J, Ma Guojie G

Compound glycyrrhizin tablets, derived from licorice root, are widely used for their anti-inflammatory and hepatoprotective properties. However, their active metabolite, glycyrrhetinic acid, can induce acquired apparent mineralocorticoid excess (AME) - a clinical syndrome where cortisol abnormally activates mineralocorticoid receptors due to the inhibition of 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), mimicking primary aldosteronism. We report a case of a 57-year-old male who developed severe hypertension and hypokalemia after 30 days of treatment with compound glycyrrhizin (150 mg, t.i.d.). Laboratory investigations revealed profound hypokalemia (2.03 mmol/L) and metabolic alkalosis. Critically, both plasma renin activity (< 0.5 μIU/mL) and aldosterone levels (2.4 - 2.7 ng/dL) were significantly suppressed, effectively ruling out primary and secondary hyperaldosteronism. A diagnosis of acquired AME was established based on the temporal relationship with glycyrrhizin intake, the "double-low" hormonal profile, and the exclusion of Cushing's syndrome. Following treatment with amlodipine and potassium supplementation, the patient's symptoms resolved. At the 2-week post-discharge follow-up, after discontinuing all medications, his blood pressure remained stable (< 140/90 mmHg) and serum potassium normalized to 4.55 mmol/L, confirming the reversible nature of acquired AME.

PMID 42544526
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PubMedHigh blood pressure & cardiovascular prevention : the official journal of the Italian Society of Hypertension2026-08-01

Efficacy and Safety of the Extemporaneous Combination Nebivolol/Amlodipine in Patients with Hypertension Uncontrolled on Monotherapy: The BOTTICELLI Study.

Volpe Massimo M, Desideri Giovambattista G, Dechend Ralf R, Van De Borne Philippe P et al.

Hypertension is the leading cause of cardiovascular disease, and its complications are preventable with blood pressure (BP)-lowering treatment. Combination treatment with 2 or more antihypertensive agents achieves sustained BP reductions. Nebivolol (NEB), a highly β1-selective beta-blocker with vasodilating properties, and amlodipine (AML), a dihydropyridine calcium channel blocker, are widely prescribed as monotherapies or in combination. To evaluate efficacy and safety of extemporaneous combination at fixed doses of NEB/AML in adults with hypertension uncontrolled on monotherapy. This phase 4, open-label, multicentre study enrolled adults with hypertension uncontrolled on monotherapy. After 4-week run-in on NEB 5 mg or AML 5 mg, patients with uncontrolled BP initiated NEB/AML 5/5 mg. Those still uncontrolled after 4 weeks were up-titrated to NEB/AML 5/10 mg, while controlled patients continued NEB/AML 5/5 mg for the full 8-week period. The primary endpoint was the change from baseline in mean sitting DBP after 8 weeks of treatment. Secondary endpoints included the change from baseline in mean sitting SBP, the proportion of patients achieving guideline-recommended BP targets, and safety. A total of 301 patients, mean age 52.1 (± 8.5) years, entered the run-in period; of these, 276 completed the study, with 182 achieving goal BP on NEB/AML 5/5 mg and 94 up-titrated to NEB/AML 5/10 mg. Overall, mean sitting DBP decreased by -15.2 (± 8.3) mmHg and SBP by -24.2 (± 11.8) mmHg (both p<0.001) over the treatment period. At study end, 63.0% of patients achieved BP <130/80 mmHg. NEB/AML dose regimens were well tolerated, and no serious treatment-emergent adverse events were reported. This study adds to the existing evidence supporting the efficacy and safety of the NEB/AML combination at two dose levels in managing hypertension and bringing patients at target goal.

PMID 42538498
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PubMedPharmaceuticals (Basel, Switzerland)2026-07-28

Bisoprolol and Amlodipine Co-Administration with Glimepiride in a Diabetic Rat Model: A Statistical and Machine Learning Analysis.

Hailat Mohammad M, Hailat Zeyad Z, Ifraitekh Mo'ath M, Zakaraya Zainab Z et al.

Background/Objectives: Diabetes mellitus type 2 (T2DM) is often associated with hypertension, necessitating treatment with combinations of medications that address both glycemic control and blood pressure. Whether commonly co-prescribed antihypertensives modify the glycemic efficacy of a sulfonylurea remains insufficiently characterized in controlled preclinical models. Methods: One hundred adult male Wistar rats were allocated to ten parallel groups (n = 10): healthy and diabetic untreated controls; glimepiride, bisoprolol or amlodipine monotherapy (in healthy and diabetic animals); and the diabetic combinations glimepiride+bisoprolol and glimepiride+amlodipine. T2DM was induced with a high-fat diet plus low-dose streptozotocin (35 mg/kg, i.p.) and confirmed by fasting blood glucose ≥ 200 mg/dL. Glycated hemoglobin (HbA1c) was measured weekly for 11 weeks. Non-parametric inference (Kruskal-Wallis, Dunn's with Bonferroni correction, Mann-Whitney U, Wilcoxon signed-rank) was complemented by Random Forest regression and PCA/K-means clustering. Results: Week-11 HbA1c differed markedly across groups (Kruskal-Wallis H = 94.3, p < 0.001). Glimepiride + bisoprolol achieved near-normal control (4.37% ± 0.15), statistically indistinguishable from healthy groups (p ≥ 0.33), and was the only diabetic regimen with a declining trajectory (-0.66 percentage points; Wilcoxon p = 0.004). Adding either antihypertensive to glimepiride did not worsen glycemic control. Amlodipine monotherapy did not attenuate hyperglycemia (8.47% ± 0.20), approaching that of untreated diabetic controls (9.31% ± 0.18), consistent with the absence of intrinsic glucose-lowering activity. All agents showed pronounced disease-state dependence (healthy-diabetic divergence 2.33-3.13 points). Random Forest prediction was accurate (R2 = 0.985), and unsupervised clustering separated effective from ineffective regimens, corroborating the statistical findings. Conclusions: In this model, bisoprolol co-administration enhanced and amlodipine co-administration preserved glimepiride-mediated glycemic control. Glimepiride+bisoprolol emerged as the most effective regimen, supporting cardioselective β-blockade as a metabolically favorable antihypertensive partner for sulfonylurea therapy and warranting clinical confirmation. More broadly, these results provide a preclinical, evidence-based rationale for selecting metabolically favorable antihypertensives in patients with coexisting T2DM and hypertension, with the potential to improve glycemic outcomes and reduce the risk of adverse drug-disease interactions during combination therapy.

PMID 42515745
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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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