若生智能
Drug Database
AM

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

PubMedJournal of clinical medicine2026-06-12

Sparsentan for the Treatment of Immunoglobulin A Nephropathy: An Innovative Concept for Economic Modelling.

Baxter Garth G, Ramirez de Arellano Antonio A, Edmonds Tom T

Background/Objectives: Immunoglobulin A nephropathy (IgAN) is a type of chronic kidney disease (CKD) and the most common cause of kidney failure in patients <40 years of age. Previous economic models in CKD have generally defined health states solely by the progression of CKD. This manuscript presents an alternative method which also considers the level of proteinuria in a CKD patient. Methods: A cohort-level state transition model was developed, comparing the health benefits of sparsentan, a dual endothelin angiotensin receptor antagonist, to irbesartan, an angiotensin receptor blocker, in IgAN. Within four UP/C (proteinuria) states, patients are assigned to three sub-health states according to CKD stage. Patients with end-stage renal disease are grouped together, irrespective of UP/C, and are stratified instead by renal replacement therapy modality. Transition matrices are derived from a combination of data from PROTECT, a clinical trial comparing sparsentan to irbesartan, and the UK RaDaR registry. Health-related quality of life data from a general CKD population is used as a proxy. Results: Patients with IgAN who were modelled to receive treatment with sparsentan had an estimated total undiscounted life years of 25.5 years, a gain of 0.9 years in comparison with irbesartan. Patients were also more likely to spend more time in earlier CKD stages while in pre-ESRD. This translated to significant quality-adjusted life year gains for patients treated with sparsentan in comparison with irbesartan. Conclusions: This study presents a new structure for health economic models in IgAN that more comprehensively captures the effect of proteinuria in combination with CKD progression. This new approach ultimately allows for the more robust implementation of clinical trial data in IgAN and estimates of the cost-effectiveness of new treatments.

PMID 42279062
阅读全文 →
PubMedJournal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics2026-06-10

Comparative Efficacy and Safety of Topical Bepotastine Besilate 1.5% Versus Sodium Cromoglycate 4% in Chronic Allergic Conjunctivitis: A Prospective Study.

Jhanwar Mayank M, Goyal Sumit S, Nathan Ajay A

To compare the efficacy, safety, and patient satisfaction of bepotastine besilate 1.5% versus sodium cromoglycate 4% eye drops in the management of chronic allergic conjunctivitis. In this prospective, double-masked comparative study, 100 adult patients with chronic allergic conjunctivitis were assigned to receive either bepotastine twice daily (n = 50) or cromolyn 4 times daily (n = 50) for 6 months. The primary outcome was the change in ocular itching severity on a standardized 0-3 scale. Secondary outcomes included changes in redness, tearing, swelling, discomfort, treatment compliance, adverse events, and patient satisfaction. Assessments were conducted at baseline, 2 weeks, 6 weeks, 3 months, and 6 months. Both treatments significantly improved symptoms from baseline after 6 months. Bepotastine showed superior reduction in ocular itching severity (74.4% improvement) compared to cromolyn (63.8%, P < 0.01). Cromolyn was more effective in reducing conjunctival redness (70.0% vs. 59.3%). Bepotastine also showed numerical advantages in tearing, swelling, and discomfort relief. Adverse events were mild and comparable, with slightly more burning sensation reported in the cromolyn group. Compliance and patient satisfaction were higher in the bepotastine group, attributed to its convenient twice-daily dosing. Both bepotastine besilate and sodium cromoglycate are effective and safe for chronic allergic conjunctivitis. Bepotastine offers faster relief of itching and greater convenience, whereas cromolyn provides better control of conjunctival redness. Treatment choice should be individualized based on symptom profile and patient preferences.

PMID 42267878
阅读全文 →
PubMedClinical therapeutics2026-06-09

Efficacy and Safety Profile of a Triple Single-Pill Combination of Valsartan/Amlodipine/Chlorthalidone in Patients with Uncontrolled Hypertension.

Lee Hae-Young HY, Suh Soon-Yong SY, Youn Ho-Joong HJ, Chung Woo-Baek WB et al.

This randomized, double-blind, multicenter Phase III study evaluated the efficacy and safety profile of a single-pill triple combination of valsartan/amlodipine/chlorthalidone (KDF1901, Valdipine Plus) compared with a dual combination of valsartan/amlodipine (KDF1901-R) in patients with essential hypertension. Patients (n = 294) with inadequately controlled hypertension after a 4-week run-in phase with valsartan/amlodipine (80/5 mg) were randomized to receive KDF1901 (valsartan/amlodipine/chlorthalidone 160/10/25 mg, n = 147) or KDF1901-R (valsartan/amlodipine 160/10 mg, n = 147) for 8 weeks. The primary efficacy endpoint was the change in mean sitting systolic blood pressure (MSSBP) from baseline to week 8. Secondary endpoints included changes in mean sitting diastolic blood pressure (MSDBP), BP normalization rates, and response rates. Safety profile outcomes assessed treatment-emergent adverse events (TEAEs), laboratory parameters, and serious adverse events. At week 8, the KDF1901 group exhibited a significantly greater reduction in MSSBP (-22.8 ± 1.0 mmHg) compared with the dual therapy group (-16.7 ± 1.0 mmHg, P < 0.0001). Similarly, the mean MSDBP reduction was significantly greater with KDF1901 (P = 0.0006). BP normalization rates (75.9% vs 54.5%, P < .0001) and response rates (73.8% vs 51.7%, P < 0.0001) were significantly higher in the triple combination group. Overall, the incidence of TEAEs was similar between groups (24.7% vs 21.5%, P = 0.5783), with mild cases of dizziness were most commonly reported. Exploratory ad hoc analyses showed statistically greater changes in sodium, potassium, and uric acid levels with triple therapy, but clinically meaningful extreme electrolyte abnormalities were rare in both groups, and the overall laboratory profile remained acceptable. This trial reported that the single-pill triple combination KDF1901 significantly improved BP control compared with dual therapy without compromising tolerability. NCT07116863.

PMID 42259717
阅读全文 →
PubMedBMJ case reports2026-06-09

Hypokalaemic paralysis as a presenting feature of primary aldosteronism.

Khurana Shubham S, Kumar Vijay V, Adil Mohd M, Raj Neha N et al.

A woman in her 30s presented with acute flaccid paraparesis secondary to severe hypokalaemia. She had a known history of hypertension controlled on amlodipine and bisoprolol. Biochemical workup revealed metabolic alkalosis, renal potassium loss, suppressed plasma renin activity and markedly elevated aldosterone levels. CT imaging identified a left adrenal adenoma consistent with an aldosterone-producing adenoma. The patient underwent laparoscopic adrenalectomy, after which she no longer required antihypertensive medication and maintained normal serum potassium. This case highlights a reversible but often under-recognised cause of secondary hypertension presenting with hypokalaemic paraparesis.

PMID 42259571
阅读全文 →
PubMedACS omega2026-06-08

The State of Imidazolone as an Evolving Pharmacophore: Current Progress and Clinical Significance in Oncology and AMR.

Panda Preetesh Kumar PK, Mal Suvadeep S, Mahapatra Monalisa M, Ghose Aruna A et al.

Nitrogen-bearing heterocycles have been fundamental scaffolds in drug discovery, contributing significantly to the design and development of therapeutic agents since the inception of modern medicinal chemistry. Among them, imidazolones have shown notable therapeutic relevance, particularly in oncology, antimicrobial resistance (AMR), and inflammation, yet they remain relatively underexplored. Nevertheless, the significant therapeutic and clinical efficacy of imidazolone-bearing drugs, such as Nilutamide, Irbesartan, and Leucettinib-21, in anticancer, antihypertensive, and neurotherapeutic applications has stimulated increasing interest in imidazolone chemistry and its medicinal potential. This review systematically discusses the major synthetic strategies, structure-activity relationships, and mechanistic principles governing the biological activity of imidazolones. Particular emphasis is placed on their rapidly expanding role as anticancer agents targeting enzymes and signaling proteins such as carbonic anhydrases, epidermal growth factor receptors (EGFR), Bcl-2 protein family, and checkpoint kinases, along with their potential applications in antimicrobial and anti-inflammatory therapies. Furthermore, the review highlights the complementary roles of computational modeling and biological evaluation in understanding the interactions of imidazolone-bearing compounds with various microbial and cancer-related receptors. These integrated studies reveal their ability to engage multiple biological targets and validate their observed pharmacological activities. The convergence of in silico predictions with experimental findings offers valuable guidance for the rational development of imidazolone-based therapeutics. Overall, this review emphasizes imidazolones as promising scaffolds with significant potential for future drug discovery and development.

PMID 42255605
阅读全文 →
PubMedClinical case reports2026-06-08

Transcranial Direct Current Stimulation (tDCS) for the Treatment of Hemolacria Comorbid With Psychiatric and Somatic Symptoms: A Case Report.

Mohammadi Roghayeh R, Alipour Ahmad A

Hemolacria is a rare condition characterized by bloody tears. Its etiology is often multifactorial, but functional/psychosomatic mechanisms have been proposed when organic causes are excluded. A 48-year-old woman with a history of multiple traumatic brain injuries (coma in 2008, car accident in 2017) presented with refractory generalized anxiety disorder, major depressive disorder, insomnia disorder, and treatment-resistant hypertension. Since 2022, she developed bilateral hemolacria with a baseline frequency of 4-5 episodes daily despite extensive negative ophthalmological, neurological, hematological, and imaging workups. She had been on stable doses of sertraline 100 mg/day, amlodipine 10 mg/day, losartan 100 mg/day, and intermittent zolpidem for at least 6 months. Anodal transcranial direct current stimulation (tDCS) targeting the left dorsolateral prefrontal cortex (L-DLPFC; anode F3, cathode Fp2) was administered for 27 sessions over 61 days (1-2 mA, 20 min/session, 5 days/week). No concurrent medication changes were made during or after the intervention. Marked clinical improvement began around session 12. By session 27, standardized scores showed remission of symptoms (HAM-D-17 from 26 to 4, HAM-A from 34 to 6, PSQI from 16 to 5), office blood pressure normalized to 125-135/80-85 mmHg, and hemolacria frequency decreased to one minor episode every 43 days. All improvements were sustained at the 3-month follow-up without further tDCS. This single-case, open-label report describes concurrent reductions in psychiatric, cardiovascular, and hemolacria symptoms that occurred in temporal association with anodal tDCS over the L-DLPFC in a treatment-refractory patient after organic causes had been excluded. Given the uncontrolled design, causality cannot be established; alternative explanations including placebo response, non-specific effects of clinical attention, regression to the mean, or spontaneous remission cannot be excluded. Randomized controlled trials are warranted to investigate the potential efficacy and mechanisms of tDCS in functional hemolacria.

PMID 42256963
阅读全文 →

注册免费账户还可查看另外 8466 篇文献

免费注册查看全部文献 →

了解更多amlodipine besilate + irbesartan