Drug Database
AM

amlodipine besilate + irbesartan (DSP8153)

✓ Approved

Sumitomo Pharma Co., Ltd. · AGTR1 · Small Molecule

What is amlodipine besilate + irbesartan?

amlodipine besilate + irbesartan is a small molecule developed by Sumitomo Pharma Co., Ltd.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesDSP8153
CompanySumitomo Pharma Co., Ltd.
Drug ClassSmall Molecule
Molecular TargetAGTR1, CACNA1C
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Sumitomo Pharma Co., Ltd.

Mechanism of Action

Molecular Targets

amlodipine besilate + irbesartan 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

amlodipine besilate + irbesartan is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Vascular disordersHypertension✓ Approved

Related Research Articles

PubMedIranian journal of pharmaceutical research : IJPR2026-10-14

Yishen Xiaoke Formula Delays Renal Fibrosis in Rats with Diabetic Nephropathy by Suppressing the Transforming Growth Factor-Beta 1/Notch Signalling Pathway.

Chang Shanshan S, Zheng Xuan X, Chen Qiang Q, Liu Xuan X et al.

Yishen Xiaoke Formula (YSXKF), derived from the classical prescription Yuquan San, has been used clinically to treat diabetic nephropathy (DN) in patients with qi-yin deficiency syndrome. This study investigated whether YSXKF delays renal fibrosis progression in DN rats by regulating the transforming growth factor-beta 1 (TGF-β1)/Notch signalling pathway. Seventy-five male Sprague Dawley rats were included and randomly assigned to a control cohort (15 rats) or a model cohort (60 rats). DN was induced by unilateral nephrectomy, a high-fat/high-sucrose diet, and streptozotocin injection. DN rats were treated with YSXKF, irbesartan, or YSXKF combined with TGF-β1 activation for 8 weeks. After 8 weeks of intervention, 24-h urinary total protein (24-h UTP), circulating TGF-β1 levels, fasting blood glucose (FBG), and serum creatinine (Scr) were evaluated. Masson staining was performed to assess renal pathological changes, and quantitative reverse transcription polymerase chain reaction and immunohistochemistry were conducted to assess the levels of TGF-β1, Jagged1, and Hes1 in renal tissue. Compared with DN rats, YSXKF treatment significantly reduced 24-h UTP excretion, circulating TGF-β1 levels, FBG, and Scr. Histological analysis revealed attenuated glomerulosclerosis and interstitial fibrosis. YSXKF decreased renal mRNA and protein expression of TGF-β1, Jagged1, and Hes1. Activation of TGF-β1 markedly reversed these protective effects and restored Notch pathway activation. YSXKF delays renal fibrosis progression in DN rats by downregulating TGF-β1 expression and inhibiting Jagged1/Hes1 activation in the Notch signaling pathway, thereby reducing extracellular matrix deposition.

PMID 42871587
Read full article →
PubMedTrials2026-10-14

Evaluating sedation efficacy and perioperative safety of fospropofol disodium versus propofol in elderly patients undergoing elective TURP: study protocol for a randomized controlled trial.

Sui Hongyuan H, Wu Tong T, Gao Lijuan L, He Qingying Q et al.

Fospropofol disodium is the first novel water-soluble propofol prodrug in China. After administration, it is mainly converted to propofol by alkaline phosphatase on the surface of endothelial cells to exert its pharmacological effects. Compared with propofol, fospropofol disodium has the characteristics of longer duration of action, lower incidence of injection pain and adverse events related to the respiratory and circulatory systems, and no adverse reactions related to lipid metabolism. At present, there are few reports on the safety and efficacy of fospropofol disodium in the induction and maintenance of general anesthesia. Therefore, this study aims to evaluate the safety and efficacy of fospropofol disodium in routine anesthesia for elective surgery in the elderly, so as to provide new medication guidance for its application in the induction and maintenance stages of general anesthesia in the elderly population. Seventy elderly patients aged 65-85 years with American Society of Anesthesiologists (ASA) physical status II or III, scheduled for elective transurethral resection of the prostate under general anesthesia, will be enrolled. Patients will be randomly divided into the propofol group (group E) and the fospropofol disodium group (group F) using a random number table, with 35 cases in each group. Anesthesia induction: sufentanil 0.2-0.4 µg/kg and cisatracurium besilate 0.15 mg/kg will be administered intravenously. Group E will receive an intravenous bolus of propofol 1-1.5 mg/kg, while group F will receive an intravenous bolus of fospropofol disodium 10-15 mg/kg, both infused within 60 s. Tracheal intubation will be performed when the patient's Modified Observer's Assessment of Alertness/Sedation (MOAA/S) score decreases to 1 with BIS < 60 sustained for ≥3 min, followed by routine mechanical ventilation. For anesthesia maintenance, group E will receive continuous intravenous infusion of propofol 4-12 mg/(kg·h) and remifentanil 0.2-0.4 µg/(kg·min) via a syringe pump; group F will receive continuous intravenous infusion of fospropofol disodium 10-20 mg/(kg·h) and remifentanil 0.2-0.4 µg/(kg·min) via a syringe pump. During the operation, the infusion rates of maintenance anesthetics will be adjusted according to hemodynamic status to maintain blood pressure and heart rate fluctuations within 20% of the baseline values, and the Bispectral Index (BIS) value will be maintained between 40 and 60. After the operation, patients will be transferred to the post-anesthesia care unit (PACU). Primary outcomes of this study: success rate of sedation and time to onset of sedation. (1) perioperative indicators, (2) hemodynamic indices at each time point, (3) adverse reactions. Elderly patients undergoing transurethral resection of the prostate (TURP) are often complicated with multiple comorbidities, leading to a relatively high anesthetic risk. This trial takes the success rate of sedation and time to onset of sedation as the primary endpoints, to compare the application differences between fospropofol disodium and propofol. The aim of this study is to evaluate the safety and efficacy of fospropofol disodium in routine anesthesia for elective surgeries in the elderly population. The study was registered at the Chinese Clinical Trials Registry (ChiCTR2500115343) on December 24, 2025 ( http://www.chictr.org.cn/showproj.html?proj=294899 ).

PMID 42870298
Read full article →
PubMedThe AAPS journal2026-10-13

Physiologically based Biopharmaceutics Modeling (PBBM) Reveals a Low Dissolution-related Bioequivalence Risk for Immediate-Release Amlodipine Tablets.

de la Cruz Cruz Porfirio P, Gomide Larissa Lopes Rodrigues LLR, do Nascimento Gabriela Moraes GM, Urizar José Trinidad Pérez JTP et al.

A conservative BCS class III classification was recently proposed for amlodipine based on inconclusive permeability evidence. However, the scarce in vivo data suggest that amlodipine is slowly, though completely, absorbed. This means that the very rapid dissolution criterion associated with a BCS class III classification may be overly restrictive for immediate-release amlodipine products. The aim of this manuscript was to develop and validate a physiologically based biopharmaceutics model (PBBM) to assess the risk of bioequivalence failure associated with dissolution. Given that amlodipine is a lipophilic weak base, the absorption model incorporated a surrogate representation of intracellular lysosomal trapping through the FuEnt parameter, resulting in an adequate description of oral pharmacokinetics. Dissolution input included in vitro profiles obtained in phosphate buffer pH 6.8 at 50 rpm for different multisource products, fitted to either the Johnson model or the Z-factor approach. Although several products did not meet biowaiver dissolution criteria, virtual bioequivalence simulations conducted with the validated PBBM consistently predicted bioequivalence across tested formulations. Overall, these findings suggest that dissolution differences would have limited impact on the in vivo performance of amlodipine and support a low dissolution-related bioequivalence risk for immediate-release amlodipine tablets.

PMID 42864569
Read full article →
PubMedJournal of hypertension2026-10-12

Blood pressure and homocysteine-lowering effects of the amlodipine/folic acid combination in patients with hypertension and serum homocysteine concentration ≥10 μmol/l (H-type hypertension): a multicenter, randomized, double-blind, parallel-controlled clinical trial.

Li Jianping J, Zhang Yan Y, Fan Fangfang F, Yi Tieci T et al.

Elevated plasma homocysteine (Hcy ≥10 μmol/l) and hypertension, defined as H-type hypertension, can synergistically increase the risk of cardiovascular diseases, especially for stroke. We aimed to assess the efficacy and safety of amlodipine-folic acid in lowering both blood pressure (BP) and plasma Hcy, compared with amlodipine alone. Eligible participants (299 males and 241 females) were randomly assigned in a 1:1:1 ratio to 5 mg amlodipine (control, group A), 5 mg amlodipine plus 0.4 mg folic acid (group B), or 5 mg amlodipine plus 0.8 mg folic acid (group C). All participants were followed at 2, 4, 6, and 8 weeks. The primary outcome was the efficacy of lowering both BP and Hcy. Among the 540 participants who were randomized, the efficacy of lowering both BP and Hcy was significantly better in groups B and C compared with group A at the end of 4 weeks, and sustained at the end of 8 weeks (group B vs. group A: 31.7% vs. 6.1%, P < 0.001; group C vs. group A: 32.8% vs. 6.1%, P < 0.001). Both groups B and C were more efficacious in lowering Hcy and raising folate levels than amlodipine alone at 8 weeks. There was no significant difference in BP lowering and adverse events among the three treatment groups. In H-type hypertension patients, amlodipine-folic acid (5 mg/0.4 mg or 5 mg/0.8 mg) had a significantly higher efficacy of lowering both BP and plasma Hcy compared with amlodipine alone. The efficacy of BP lowering and safety profile were comparable among the three treatment groups. This trial was registered in clinicaltrials.gov, identifier: NCT01848873.

PMID 42861767
Read full article →
PubMedPLoS medicine2026-10-12

Comparative effectiveness of amlodipine versus nifedipine prescribed at discharge in patients with ischemic stroke or transient ischemic attack: A nationwide 5-year follow-up registry study.

Li Xinya X, Xia Xue X, Gao Meng M, Xu Qin Q et al.

Amlodipine and nifedipine are the most commonly prescribed calcium channel blockers (CCB) for patients suffering from ischemic stroke or transient ischemic attack (TIA). Nevertheless, there is a scarcity of direct comparative evidence on their effectiveness. This study aimed to compare the effectiveness of amlodipine and nifedipine in patients with ischemic stroke or TIA. This observational study was based on the Third China National Stroke Registry, which recruited consecutive adult patients with ischemic stroke or TIA from 2015 to 2018. In this study, ischemic stroke or TIA patients were prescribed either amlodipine or nifedipine at discharge. The primary outcome was the distribution of modified Rankin Scale (mRS) score, which assesses functional outcomes in patients with stroke, at 5 years. The intergroup differences were examined using ordinal logistic regression, yielding odds ratios (OR) and 95% confidence intervals (CI). Patient age, gender, body mass index, systolic blood pressure at admission, and onset date were adjusted. To improve baseline characteristic balance, inverse probability of treatment weighting (IPTW) was implemented. A total of 2,859 eligible patients were included, and there were 1847 patients in the amlodipine group and 1,058 patients in the nifedipine group after IPTW. The amlodipine group demonstrated significantly lower 5-year mRS scores in comparison to the nifedipine group, with an OR of 0.76 (95% CI [0.65, 0.89]; p < 0.001). A total of 956 (51.76%) amlodipine users and 632 (59.74%) nifedipine users achieved a mRS score > 0 at 5 years, with an OR of 0.71 (95% CI [0.61, 0.83]; p < 0.001). The sensitivity analyses yielded consistent results. The main limitations include the inherent observational design, the exclusive reliance on registry data, and relatively high loss-to-follow-up rate at 5 years. This study revealed that amlodipine, compared to nifedipine, may be associated with improved functional recovery in ischemic stroke or TIA patients. Randomized controlled trials are warranted to confirm these findings and refine CCB therapy.

PMID 42862855
Read full article →
PubMedHigh blood pressure & cardiovascular prevention : the official journal of the Italian Society of Hypertension2026-10-12

Real-World Adherence to Dihydropyridine Calcium-Channel Blockers: A Pharmacoepidemiologic Study.

Capacci Marco M, Rivasi Giulia G, Degli Esposti Luca L, Fumagalli Carlo C et al.

Low medication adherence contributes to uncontrolled cardiovascular (CV) risk. This study investigated 12- and 24-month adherence, all-cause mortality and CV events in subjects receiving originator or generic dihydropyridine calcium-channel blockers (CCBs) as recorded in administrative databases from Local Health Units across several Italian regions. We retrospectively analysed databases containing demographics and vital status, drug prescriptions, and hospital discharge diagnoses for more than 6 million individuals. Subjects receiving lercanidipine originator, generic lercanidipine, amlodipine originator, or generic amlodipine were included. Subjects with prior or occasional CCB use, inadequate follow-up time, chronic ischaemic heart disease or acute pulmonary heart disease, or switching between CCBs were excluded. Adherence was defined as a Proportion of Days Covered ≥ 80% at 12 and 24 months. Cox regression models estimated the association between treatments and a composite of all-cause mortality and CV events. Adherence was assessed in 3,860 propensity-score-matched subjects (965/group), selected from 14,849 eligible subjects. Lercanidipine originator was associated with higher (p < 0.001) 12-month (43%) and 24-month (38%) adherence than generic lercanidipine (31 and 26%) and amlodipine originator (22 and 19%). The events analysis included 15,808 subjects. Compared with originator lercanidipine, originator amlodipine, generic lercanidipine and generic amlodipine were associated with 43%, 30% and 33% higher hazards of the composite outcome, respectively (corresponding 95% Confidence Intervals: 1.28-1.60, 1.10-1.55, 1.17-1.50). Medium-term adherence was low across all treatments. Originator lercanidipine was associated with the highest adherence, with lower adjusted hazards of the composite outcome and all-cause mortality compared to the other treatments.

PMID 42862466
Read full article →

+8580 more articles available with a free account

Sign up free to view all articles →

Ask about amlodipine besilate + irbesartan