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olmesartan + azelnidipine (Rezaltas / Rezaltas)

✓ Approved

Daiichi Sankyo Company Limited · AGTR1 · Small Molecule

What is olmesartan + azelnidipine?

olmesartan + azelnidipine is a small molecule developed by Daiichi Sankyo Company Limited. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesRezaltas, Rezaltas
CompanyDaiichi Sankyo Company Limited
Drug ClassSmall Molecule
Molecular TargetAGTR1, CACNA1C
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Daiichi Sankyo Company Limited

Mechanism of Action

Molecular Targets

olmesartan + azelnidipine acts on 2 molecular targets:

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

olmesartan + azelnidipine is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Vascular disordersHypertension✓ Approved

Related Research Articles

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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PubMedPharmaceutics2026-09-26

A Thermoresponsive In Situ Salified Self-Nanoemulsifying Drug Delivery System of Olmesartan Medoxomil: Overcoming Leakage and Drug Trapping Limitations.

Sherif Abdelrahman Y AY, Altamimi Mohammad A MA, Elzayat Ehab M EM

Background/Objectives: Solid self-nanoemulsifying drug delivery systems (SNEDDS) prepared by adsorption onto porous carriers are widely used to improve the oral delivery of poorly water-soluble drugs. However, this approach is limited by increased dosing volume and incomplete drug release. This study aims to develop a thermoresponsive in situ salified SNEDDS (T-IS-SNEDDS) that simultaneously prevents formulation leakage and overcomes the release limitations of conventional adsorption-based solidification. Methods: Excipients were selected by solubility screening of oils and surfactants. Sodium and calcium carbonate were evaluated for in situ salt formation. Adsorption-based solid SNEDDS and thermoresponsive formulations containing poloxamer 188 with propylene glycol or polyethylene glycol 400 were prepared. Droplet size was measured after aqueous dilution. Solid-state characterization used scanning electron microscopy, Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry, and powder X-ray diffraction. In vitro dissolution performance was evaluated against the raw drug and adsorption-based formulations. Results: Imwitor 308 and Tween 80 exhibited the highest solubilization capacities. Sodium carbonate (10 mg/g) markedly increased the solubility of olmesartan medoxomil from 4.11 ± 0.11 to 46.01 ± 1.92 mg/g. Although liquid in situ salified SNEDDS achieved rapid dissolution (94.2 ± 1.8% at 10 min), adsorption-based solidification required four capsules and yielded incomplete drug release (67.76 ± 3.18%). Both thermoresponsive formulations accommodated the therapeutic dose in a single capsule and released ≈95% of the drug within 60 min. Conclusions: The combined in situ salified drug loading and thermoresponsive matrix strategy successfully enables single capsule administration while overcoming the incomplete release of adsorption-based solid SNEDDS.

PMID 42797370
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