Delving into the Latest Updates on Sacubitril/Allisartan Isoproxil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Sacubatril/allisartan medoxomil, 沙库巴曲阿利沙坦钙

+ [2]

Target

AT1R x CD10

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists), enkephalinase inhibitors(Neprilysin inhibitors)

Therapeutic Areas

Cardiovascular DiseasesUrogenital Diseases

Active Indication

Essential HypertensionHeart failure with reduced ejection fractionRenal Insufficiency

Inactive Indication

Chronic heart failure

Originator Organization

Shenzhen Salubris Pharmaceuticals Co., Ltd.

Active Organization

Shenzhen Salubris Pharmaceuticals Co., Ltd.

Inactive Organization-

Drug Highest PhaseNDA/BLA

First Approval Date-

Regulation-

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Structure

Molecular FormulaC27H29ClN6O5

InChIKeyXMHJQQAKXRUCHI-UHFFFAOYSA-N

CAS Registry947331-05-7

View All Structures (2)

To compare the pharmacokinetic characteristics of S086 tablets after repeated oral administration in patients with different degrees of renal insufficiency and subjects with normal renal function matched by gender, age, and body mass index, and to evaluate the safety of S086 tablets after repeated oral administration in patients with different degrees of renal insufficiency and subjects with normal renal function.

Start Date07 Sep 2022

Sponsor / Collaborator

Shenzhen Salubris Pharmaceuticals Co., Ltd.

CTR20221444 / CompletedPhase 1

评价S086片与苯磺酸氨氯地平片在健康受试者中的单中心、开放、单用及联合用药药代动力学研究

[Translation] A single-center, open-label, monotherapy and combination pharmacokinetic study to evaluate the efficacy of S086 tablets and amlodipine besylate tablets in healthy subjects

评价S086片与苯磺酸氨氯地平片单用和联合用药的药代动力学特征、安全性。

[Translation]

To evaluate the pharmacokinetic characteristics and safety of S086 tablets and amlodipine besylate tablets used alone or in combination.

Start Date05 Jul 2022

Sponsor / Collaborator

Shenzhen Salubris Pharmaceuticals Co., Ltd.

100 Clinical Results associated with Sacubitril/Allisartan Isoproxil

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100 Translational Medicine associated with Sacubitril/Allisartan Isoproxil

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100 Patents (Medical) associated with Sacubitril/Allisartan Isoproxil

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10

Literatures (Medical) associated with Sacubitril/Allisartan Isoproxil

01 Aug 2024·European Journal of Pharmacology

Natriuretic peptide system in hypertension: Current understandings of its regulation, targeted therapies and future challenges

Review

Author: Shelke, Vishwadeep ; Dagar, Neha ; Gaikwad, Anil Bhanudas ; Puri, Bhupendra

The natriuretic peptide system (NPS) is the key driving force of the heart's endocrine function. Recent developments in NPS-targeted therapies have been found promising and effective against cardiovascular diseases, including hypertension. Notably, after discovering crosstalk between NPS and the renin-angiotensin-aldosterone system (RAAS), various combinations such as neprilysin/angiotensin II receptor type 1 AT₁ receptor inhibitors and neprilysin/renin inhibitors have been preclinically and clinically tested against various cardiac complications. However, the therapeutic effects of such combinations on the pathophysiology of hypertension are poorly understood. Furthermore, the complicated phenomena underlying NPS regulation and function, particularly in hypertension, are still unexplored. Mounting evidence suggests that numerous regulatory mechanisms modulate the expression of NPS, which can be used as potential targets against hypertension and other cardiovascular diseases. Therefore, this review will specifically focus on epigenetic and other regulators of NPS, identifying prospective regulators that might serve as new therapeutic targets for hypertension. More importantly, it will shed light on recent developments in NPS-targeted therapies, such as M-atrial peptides, and their latest combinations with RAAS modulators, such as S086 and sacubitril-aliskiren. These insights will aid in the development of effective therapies to break the vicious cycle of high blood pressure during hypertension, ultimately addressing the expanding global heart failure pandemic.

01 Jan 2024·Biomedicine & Pharmacotherapy

Protective effect of novel angiotensin receptor neprilysin inhibitor S086 on target organ injury in spontaneously hypertensive rats

Article

Author: Xing, Wei ; Liu, Tao ; Zhou, Zheng-Yang ; Xu, Wen-Jie ; Yan, Jie ; Sun, Jing-Chao ; Jin, Yi ; Xiao, Ying ; Lu, Yin-Suo

BACKGROUNDHypertension is a clinical syndrome characterized by elevated systemic arterial blood pressure associated with injury to the heart, kidney, brain, and other organs. Angiotensin receptor neprilysin inhibitors (ARNi), including angiotensin receptor blockers (ARBs) and neprilysin inhibitors (NEPi), have been shown to be safe and effective at reducing blood pressure and alleviating development of target organ injury. This study was used to develop S086 as a novel ARNi and conducted preclinical studies in animal models to evaluate the protective effects of S086 on target organs.METHODSThis study used a 14-month-old spontaneously hypertensive rat (SHR) model to evaluate the protective effects of S086 on the cardiovascular system and organs such as heart and kidney by blood pressure monitoring, urine and blood examination, pathological examination, and immunological index detection.RESULTSAfter administering S086 orally to the SHR, their blood pressure and levels of renal injury indicators such as serum creatinine and urinary microalbumin were reduced, and myocardial cell necrosis and cardiac fibrosis of the heart were significantly improved. In addition, there were also significantly improvements in the histological lesions of blood vessels and the kidneys.CONCLUSIONSThe findings showed that S086 effectively reduced the blood pressure of SHR and had effects on alleviating development of heart, blood vessels and kidney.

02 Sep 2022·Expert Opinion on Investigational DrugsQ2 · MEDICINE

A randomized, double-blind, placebo-controlled, single, and multiple dose-escalation Phase I clinical trial to investigate the safety, pharmacokinetic, and pharmacodynamic profiles of oral S086, a novel angiotensin receptor-neprilysin inhibitor, in healthy Chinese volunteers

Q2 · MEDICINE

Article

Author: Li, Xiaojiao ; Yan, Jie ; Zhang, Hong ; Mai, Jiajia ; Li, Ying ; He, Shiying ; Xu, Wenjie ; Wu, Min ; Yang, Lizhi ; Sun, Jingchao ; Hu, Yue ; Li, Jinfeng

BACKGROUNDThis study evaluated the safety, pharmacokinetic (PK), and pharmacodynamic (PD) profiles of single ascending doses (SAD) and multiple ascending doses (MAD) of S086 in healthy Chinese volunteers.RESEARCH DESIGN AND METHODSThis randomized, double-blind, placebo-controlled, Phase I clinical trial enrolled 113 subjects, including 65 subjects in the SAD (60-1080 mg) study and 48 subjects in the MAD study (180-720 mg). The safety, PK (sacubitril, LBQ657, and EXP3174) and PD (MAD study: blood pressure, pulse) of S086 were assessed.RESULTSThere were no deaths, serious adverse events, or discontinuations due to TEAEs, and there were no significant safety concerns associated with S086. PK parameters for sacubitril, LBQ657, and EXP3174 increased in a dose-dependent manner after single oral doses of S086. Plasma concentrations of sacubitril, LBQ657, and EXP3174 were maintained at steady state within 5 days of once-daily oral administration of S086. In the MAD study, S086 administration was associated with a dose-dependent decrease in mean diastolic and systolic blood pressure compared to baseline.CONCLUSIONSThe safety and PK profile profiles of S086 support the use of S086 240 mg once daily in a future Phase II study in patients with heart failure.TRIAL REGISTRATIONThe trial is registered at chinadrugtrials.org.cn (CT.gov identifier: CTR20182350 and CTR20182351).

100 Deals associated with Sacubitril/Allisartan Isoproxil

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Essential Hypertension	NDA/BLA	CN	Shenzhen Salubris Pharmaceuticals Co., Ltd.	07 Jul 2023
Heart failure with reduced ejection fraction	Phase 3	CN	Shenzhen Salubris Pharmaceuticals Co., Ltd.	12 Apr 2022
Renal Insufficiency	Phase 1	CN	Shenzhen Salubris Pharmaceuticals Co., Ltd.	07 Sep 2022
Chronic heart failure	Preclinical	CN	Shenzhen Salubris Pharmaceuticals Co., Ltd.	26 Dec 2018