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olmesartan + azelnidipine (Rezaltas / Rezaltas)

✓ Approved

Daiichi Sankyo Company Limited · AGTR1 · 小分子

什么是 olmesartan + azelnidipine？

olmesartan + azelnidipine 是一种小分子，由Daiichi Sankyo Company Limited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Rezaltas, Rezaltas
公司Daiichi Sankyo Company Limited
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, Daiichi Sankyo Company Limited

作用机制

分子靶点

olmesartan + azelnidipine 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

olmesartan + azelnidipine 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

PubMedHigh blood pressure & cardiovascular prevention : the official journal of the Italian Society of Hypertension2026-10-26

A Practical Treatment Platform Version 3.0 for Using Angiotensin Receptor Blocker-Based Single-Pill Combinations in Patients With Hypertension.

Tocci Giuliano G, Burnier Michel M, de la Sierra Alejandro A, Grassi Guido G et al.

Elevated blood pressure (BP) is the leading cause of cardiovascular disease and a major contributor to mortality, affecting almost one third of the adult population worldwide. Despite strong scientific evidence, guidelines and multiple therapeutic options, many patients remain undertreated or uncontrolled, largely due to poor medication adherence and medical inertia. Complexity of multi-pill regimens contributes significantly to non-adherence, whereas single-pill combinations (SPCs) improve adherence and persistence, accelerate BP control, and promote better long-term outcomes than multiple combinations. Appropriate selection of SPC in individual hypertensive patients may be a difficult though very important task for physicians. Thus, development of tools that may facilitate use of SPC in clinical practice is desirable. Among renin-angiotensin system blockers, olmesartan (OM) has demonstrated sustained efficacy, favourable tolerability, both as monotherapy and in SPCs with amlodipine and/or hydrochlorothiazide, which are available in multiple dosages. The present OM-based platform builds on earlier frameworks and incorporates guidelines' updates complemented by a systematic review of available literature. This "3.0" proposal expands patient categorization to include comorbidities or complications often overlooked in clinical practice guidelines, providing a practical, evidence-based approach to support individualized hypertension management complementing guideline recommendations.

PMID 42928416
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PubMedBMC musculoskeletal disorders2026-10-21

Effects of azelnidipine, a calcium channel blocker, in a rat femur fracture model.

Kaya Hilal H, Albayrak Abdulmecit A, Aydin Ali A, Bayir Yasin Y et al.

Fractures are an important public health problem as they reduce quality of life due to the occurrence of pain and complications. Osteoblasts originate from mesenchymal stem cells and play a vital role in bone formation. They also contain voltage-gated calcium channels. Azelnidipine is a dihydropyridine-derivative blocker of L- and T-type calcium channels. The signalling process involving the L-type calcium channel is important for the function of osteoblasts. Nevertheless, the impact of dihydropyridine chemicals on bone metabolism remains largely unexplored. To the best of our knowledge, no study has yet evaluated the specific effects of azelnidipine on bone healing. The aim of our study was to examine, for the first time, the impact of azelnidipine on the pathophysiology of bone fractures by radiographic and biochemical techniques. The study included 40 female rats in 5 groups (n = 8 in each group): a healthy sham group, femoral fracture control group, femoral fracture + 4 mg/kg azelnidipine group, femoral fracture + 8 mg/kg azelnidipine group, and femoral fracture + 16 mg/kg azelnidipine group. Serum tumour necrosis factor-α, interleukin-1β, interleukin-17, osteocalcin, osteopontin, total oxidant capacity, and bone-specific alkaline phosphatase levels significantly increased in the fracture control group compared to the sham group (p < 0.05). Azelnidipine treatment significantly reversed these elevations, particularly at the 16 mg/kg dose, restoring TNF-α, IL-1β, IL-17 levels back toward baseline (p < 0.05). Total antioxidant capacity measured in serum decreased in the fracture group 6.47 ± 1.46 U/mL, whereas azelnidipine significantly increased this parameter to 10.01 ± 1.85 U/mL in a dose-dependent manner (p < 0.05). In radiological findings, azelnidipine contributed positively to fracture healing. These results showed that azelnidipine, a calcium channel blocker, exhibits a potential healing effect in this rat femur fracture model, providing the first preclinical evidence of its potential therapeutic utility in bone recovery.

PMID 42902245
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PubMedFundamental & clinical pharmacology2026-10-18

Drug-Specific Associations of Angiotensin Receptor Blockers With Parkinson's Disease Risk in a Multicenter Electronic Health Record Cohort.

Tran Kyle K, Yang Jichen J, Pham Sally S, Luong Dylan D et al.

Angiotensin receptor blockers (ARBs) have demonstrated neuroprotective effects in preclinical models of Parkinson's disease (PD), but individual ARBs differ in pharmacological properties that may influence their neuroprotective potential. Using large-scale hospital electronic health records of the University of California health system, we tested whether specific ARBs are associated with lower PD risk. We conducted a new-user, active-comparator cohort study in the University of California Health Data Warehouse, encompassing 890 712 hypertensive patients across six academic medical centers from 2012 to 2025. Cox proportional hazards models estimated hazard ratios for individual ARB associations with incident PD, adjusting for demographics, nine preindex comorbidities, and index date. Robustness was assessed through propensity score matching and negative-control analysis. Drug-specific Cox analysis identified irbesartan (HR = 0.588, 95% CI 0.434 to 0.796, p = 0.0006) and olmesartan (HR = 0.797, 95% CI 0.665 to 0.956, p = 0.015) as associated with lower PD risk. Irbesartan survived Bonferroni correction for multiple comparisons, and propensity score matching supported both associations. In this large multicenter EHR cohort, irbesartan and olmesartan were associated with lower incident Parkinson's disease risk. These findings support further investigation of the renin-angiotensin system as a therapeutic target in Parkinson's disease and may inform the development or repurposing of agents with favorable central nervous system penetration and neuroprotective potential.

PMID 42893848
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PubMedClinical case reports2026-10-17

Improvement of Erectile Function After Switching From Valsartan to Olmesartan Within a Fixed-Dose Antihypertensive Combination: A Case Report.

Ćurković Mario M, Ćurković Nika N

Intra-class differences may exist between ARBs regarding tissue-specific outcomes. In this case, valsartan was probably associated with erectile dysfunction (Naranjo score 7). Switching to olmesartan was followed by resolutions of symptoms. An intra-class switch may be considered in selected patients with suspected drug-associated erectile dysfunction after evaluating other vascular, metabolic, or lifestyle contributions. Clinicians should remain cautious, as concurrent treatment modifications can confound definitive causal attributions.

PMID 42891090
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PubMedJournal of the American Heart Association2026-10-07

Restricting Placental Transfer of Angiotensin Receptor Blockers to Mitigate Fetal Toxicity: A Potential Therapeutic Strategy for Preeclampsia.

Inaoka Naoko N, Iriyama Takayuki T, Ariyoshi Yu Y, Yoshida Yuri Y et al.

Enhanced AT1R (angiotensin II type 1 receptor) signaling contributes to preeclampsia development; however, angiotensin receptor blockers are contraindicated during pregnancy because of associated fetal toxicity. We aimed to determine whether chemical modification of an angiotensin receptor blocker restricts placental transfer while preserving maternal pharmacological activity. Polyethylene glycol-modified olmesartan derivatives were synthesized to increase molecular size and hydrophilicity and evaluated in vitro for AT1R inhibitory activity. Placental transfer was assessed using an angiotensin II-induced pregnant mouse model and an ex vivo human placental perfusion model to identify a derivative with reduced placental permeability. The selected compound was evaluated in vivo for pharmacological activity and fetal toxicity in pregnant mice. A series of polyethylene glycol-modified olmesartan derivatives maintained pharmacologically relevant AT1R inhibitory activity in vitro. Evaluation in angiotensin II-treated pregnant mice revealed compound #6, a polyethylene glycol-modified dimer containing an ionizable tertiary amine, which exhibited reduced placental transfer (∼7% relative to olmesartan). Consistently, compound #6 exhibited minimal transplacental transfer in the human placental perfusion model, comparable to insulin, a negative control. Regarding fetal toxicity, olmesartan induced neonatal renal developmental toxicity at doses as low as one tenth of its minimum effective dose, whereas compound #6 exhibited clear renal toxicity only above its effective dose, indicating a discernible safety margin. Restricting placental transfer through rational chemical modification enables decoupling of maternal efficacy from fetal toxicity of angiotensin receptor blockers. Although further optimization is required, these findings provide proof of concept that AT1R inhibition may represent a therapeutic strategy for preeclampsia during pregnancy.

PMID 42841504
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PubMedAmerican journal of preventive cardiology2026-10-05

Study design, rationale, and baseline characteristics of ATTAIN-HYPERTENSION, a phase 3 trial of the oral GLP-1 receptor agonist orforglipron for hypertension.

Laffin Luke L, Schlaich Markus P MP, Hall Michael E ME, Xie Cathy C CC et al.

Up to three-quarters of primary hypertension is epidemiologically attributed to excess adiposity. Incretin-based therapies are consistently associated with reduced blood pressure (BP) in clinical trials; however, no prior trial has investigated incretin-based therapies for hypertension treatment with BP as its primary efficacy outcome. ATTAIN-HYPERTENSION is a phase 3 master protocol directing two identical, randomized, placebo-controlled studies. Participants with BMI≥25kg/m2 and systolic BP (SBP)≥140 mmHg or diastolic BP (DBP)≥90 mmHg, independent of antihypertensive treatment, are randomized 2:1 to orforglipron or placebo. The study includes 5 periods: screening, a 4-week run-in during which treated participants change to standard background medications (olmesartan, amlodipine, hydrochlorothiazide), a 48-week treatment period including dose escalation and return to baseline antihypertensive medication, a 12-week randomized withdrawal period, and a 2-week safety follow-up. Primary end point is the change in office SBP at Week 36. Key secondary end points include change in ambulatory SBP, percent change in hsCRP, percent change in body weight, percent change in triglycerides and non-HDL cholesterol, and change in SBP across the randomized withdrawal period. ATTAIN-HYPERTENSION randomized 538 participants in Trial 1 and 546 in Trial 2 between April 2025 and January 2026 at 100 locations across 10 countries. The randomized population has a mean (SD) age of 53.7 (11.8) years, BMI of 35.6kg/m² (6.9), and office SBP of 144.2 mmHg (10.3). At screening, 55.4% of participants were treated with antihypertensive medication. ATTAIN-HYPERTENSION investigates the efficacy and safety of orforglipron for the treatment of hypertension in adults with overweight or obesity. Described here are the novel trial design, its rationale, and the enrolled population's baseline characteristics. (ClinicalTrials.gov: NCT06948422).

PMID 42830762
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