更新于：2024-11-01

ACE

更新于：2024-11-01

基本信息

别名

肽基二肽酶A、血管紧张素转换酶、ACE

+ [11]

简介

Dipeptidyl carboxypeptidase that removes dipeptides from the C-terminus of a variety of circulating hormones, such as angiotensin I, bradykinin or enkephalins, thereby playing a key role in the regulation of blood pressure, electrolyte homeostasis or synaptic plasticity (PubMed:2558109, PubMed:4322742, PubMed:7683654, PubMed:7523412, PubMed:15615692, PubMed:20826823). Composed of two similar catalytic domains, each possessing a functional active site, with different selectivity for substrates (PubMed:1851160, PubMed:1320019, PubMed:7683654, PubMed:7876104, PubMed:10913258, PubMed:19773553). Plays a major role in the angiotensin-renin system that regulates blood pressure and sodium retention by the kidney by converting angiotensin I to angiotensin II, resulting in an increase of the vasoconstrictor activity of angiotensin (PubMed:4322742, PubMed:1851160, PubMed:11432860, PubMed:19773553, PubMed:23056909). Also able to inactivate bradykinin, a potent vasodilator, and therefore enhance the blood pressure response (PubMed:2558109, PubMed:6055465, PubMed:4322742, PubMed:6270633, PubMed:7683654, PubMed:15615692). Acts as a regulator of synaptic transmission by mediating cleavage of neuropeptide hormones, such as substance P, neurotensin or enkephalins (PubMed:656131, PubMed:6270633, PubMed:6208535, PubMed:15615692). Catalyzes degradation of different enkephalin neuropeptides (Met-enkephalin, Leu-enkephalin, Met-enkephalin-Arg-Phe and possibly Met-enkephalin-Arg-Gly-Leu) (PubMed:656131, PubMed:6270633, PubMed:2982830). Acts as a regulator of synaptic plasticity in the nucleus accumbens of the brain by mediating cleavage of Met-enkephalin-Arg-Phe, a strong ligand of Mu-type opioid receptor OPRM1, into Met-enkephalin (By similarity). Met-enkephalin-Arg-Phe cleavage by ACE decreases activation of OPRM1, leading to long-term synaptic potentiation of glutamate release (By similarity). Also acts as a regulator of hematopoietic stem cell differentiation by mediating degradation of hemoregulatory peptide N-acetyl-SDKP (AcSDKP) (PubMed:8257427, PubMed:7876104, PubMed:8609242, PubMed:26403559). Acts as a regulator of cannabinoid signaling pathway by mediating degradation of hemopressin, an antagonist peptide of the cannabinoid receptor CNR1 (PubMed:18077343). Involved in amyloid-beta metabolism by catalyzing degradation of Amyloid-beta protein 40 and Amyloid-beta protein 42 peptides, thereby preventing plaque formation (PubMed:11604391, PubMed:16154999, PubMed:19773553). Catalyzes cleavage of cholecystokinin (maturation of Cholecystokinin-8 and Cholecystokinin-5) and Gonadoliberin-1 (both maturation and degradation) hormones (PubMed:2983326, PubMed:7683654, PubMed:9371719, PubMed:10336644). Degradation of hemoregulatory peptide N-acetyl-SDKP (AcSDKP) and amyloid-beta proteins is mediated by the N-terminal catalytic domain, while angiotensin I and cholecystokinin cleavage is mediated by the C-terminal catalytic region (PubMed:7876104, PubMed:10336644, PubMed:19773553). Isoform produced by alternative promoter usage that is specifically expressed in spermatocytes and adult testis, and which is required for male fertility (PubMed:1651327, PubMed:1668266). In contrast to somatic isoforms, only contains one catalytic domain (PubMed:1651327, PubMed:1668266). Acts as a dipeptidyl carboxypeptidase that removes dipeptides from the C-terminus of substrates (PubMed:1668266, PubMed:24297181). The identity of substrates that are needed for male fertility is unknown (By similarity). May also have a glycosidase activity which releases GPI-anchored proteins from the membrane by cleaving the mannose linkage in the GPI moiety. The GPIase activity was reported to be essential for the egg-binding ability of the sperm (By similarity). This activity is however unclear and has been challenged by other groups, suggesting that it may be indirect (By similarity). Soluble form that is released in blood plasma and other body fluids following proteolytic cleavage in the juxtamembrane stalk region.

关联

181

阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利

靶点

ACE x COX x HMG-CoA reductase x NCC

作用机制

ACE抑制剂 [+3]

在研机构

Alborz Darou Pharmaceutical Co.

原研机构

Alborz Darou Pharmaceutical Co.

在研适应症

心血管疾病

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

伊朗

首次获批日期2018-02-01

Lisinopril/Torasemide

赖诺普利/托拉塞米

靶点

ACE x NKCC2

作用机制

ACE抑制剂 [+2]

在研机构

Accupharma Sp Zoo

原研机构

Accupharma Sp Zoo

在研适应症

原发性高血压 [+1]

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

波兰

首次获批日期2017-09-28

Perindopril Arginine/ Indapamide/Amlodipine

精氨酸培哚普利/吲达帕胺/氨氯地平

靶点

ACE x VDCCs

作用机制

ACE抑制剂 [+2]

在研机构

Les Laboratoires Servier SAS

原研机构

Les Laboratoires Servier SAS

在研适应症

原发性高血压

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

新加坡

首次获批日期2016-05-23

880

项与 ACE 相关的临床试验

NCT03201939 / Suspended临床2期IIT

Optimal Management of HIV Infected Adults at Risk for Kidney Complications in Nigeria

In this study, the Investigators plan to determine the optimal means to prevent or slow the progression of kidney disease among genetically at-risk northern Nigerian HIV-infected adults. Based on data from studies of diabetic kidney disease that used medications that block the renin angiotensin aldosterone system (RAAS), we plan to evaluate whether or not RAAS inhibition (using a widely available medication that blocks RAAS) in HIV-infected adults produces similarly promising results.

开始日期2024-11-01

申办/合作机构

Vanderbilt University Medical Center

[+3]

NCT05293158 / Not yet recruitingN/AIIT

Impact of Hepatitis B Immunoglobulins in Patients With Chronic Hepatitis B on Hepatocellular Carcinoma

In the current literature, infection with the hepatitis B virus (HBV) is described as one of the main risk factors for the development of hepatocellular carcinoma (HCC).
According to the current study situation, the Hepatitis B surface antigen (HBsAg) is considered as an important marker, since low levels and sero-clearance of HBsAg are both correlated with a lower risk of HCC development / recurrence.Currently there is no treatment option available that efficiently targets HBsAg. Besides neutralizing infectious HBV virions, Hepatitis B immunoglobulins (HBIG) can directly bind and neutralize extracellular HBsAg/SVPs, and even intracellular HBsAg targeting is reported. In addition, HBIGs can initiate effector-cell attack (via antibody-dependent cellular cytotoxicity, ADCC) towards infected hepatocytes.
The potential benefit of HBIGs in the HCC context is further underlined by recent evidence for the ability of HBIGs to reduce the viability, proliferation, and self-renewal of tumor-initiating cells (TICs) - isolated from HBV-HCC patients - accompanied by downregulation of stemness markers, e.g., OCT-4.According to the current study situation, the use of HBIGs significantly reduces the risk of HBV reinfection after transplantation and improves the results of liver transplantation in patients with chronic HBV infection. The potential benefit of treating HBV-HCC patients on the LTx (liver transplantation) waiting list with hepatitis B immunoglobulin is the possible stop or inhibition of tumor progression while waiting for an LTx. So far there is no clinical evidence of this.
Mechanistically, hepatitis B immunoglobulin could occur through neutralization of circulating HBsAg, which is an important driver of an immunosuppressive environment in HBV patients, and possibly through direct effects against HBV HCC tumor cells (through antibody-dependent cellular cytotoxicity, ADCC). Therefore, the idea behind preoperative HBIG administration before liver transplantation is to reduce the rate of patients in whom a transplantation would no longer have been possible due to tumor progression. Thus, due to tumor progression in HBV-positive HCC-patients there is a monthly drop-out from the waiting list of about 4%.
The basic idea behind the treatment of HBV-HCC patients before tumor resection with hepatitis B immunoglobulin is to potentially stop or positively influence tumor progression through the effects mentioned above, in the time between diagnosis and resection.
Zhou et al. (2015) have shown a connection between HBsAg levels and HCC relapses after resection, although the exact role of HBsAg is still unclear. In no case will the treatment postpone the time of tumor resection, as only patients are considered who, for clinical reasons, can expect a certain time until resection. The present proof of concept study aims to quantify HBsAg reduction due to preoperative administration of HBIGs in HBV-positive HCC-patients and serve as a template for future multicentre clinical trials.

开始日期2024-11-01

申办/合作机构

Medizinische Universität Graz

CTR20242758 / RecruitingN/A

江苏嘉逸医药有限公司生产的培哚普利氨氯地平片（III）（规格：10 mg/5 mg）与LES LABORATOIRES SERVIER的培哚普利氨氯地平片（III）（开素达®，10 mg/5 mg）在中国健康受试者中进行的随机、开放、单剂量、两周期、双交叉、餐后状态下的生物等效性研究

以江苏嘉逸医药有限公司生产的培哚普利氨氯地平片（III）（规格：10 mg/5 mg）为受试制剂，以LES LABORATOIRES SERVIER的培哚普利氨氯地平片（III）（开素达®，规格：10 mg/5 mg）为参比制剂，考察两制剂在餐后状态下单次给药的药代动力学参数及相对生物利用度，评价两制剂是否具有生物等效性；同时评价两种制剂在健康人体中的安全性和耐受性。

开始日期2024-09-07

申办/合作机构

江苏嘉逸医药有限公司

100 项与 ACE 相关的临床结果

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100 项与 ACE 相关的转化医学

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0 项与 ACE 相关的专利（医药）

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29,184

项与 ACE 相关的文献（医药）

2025-02-01·Food Chemistry

ACE inhibitory effect and saltiness-enhancing properties of chicken-derived umami peptides: Digestive stability, inhibition kinetics, multiple ligand docking and central composite design

Article

作者: Sun, Baoguo ; Yang, Rui ; Liu, Zunying ; Liang, Li ; Zhang, Haotong ; Zhang, Yuyu ; Mao, Xiangzhao

Angiotensin-I-converting enzyme (ACE) inhibitory activity and saltiness-enhancing properties of chicken-derived umami peptides were investigated. DGGRYY and NEFGYSNR were screened and the IC₅₀ values were 28.71 μM and 283.24 μM, indicating their potential as novel ACE inhibitors. DGGRYY and NEFGYSNR have good pH and thermal stability. After gastrointestinal digestion, the ACE-inhibitory activity of DGGRYY retained about 53 %, whereas NEFGYSNR retained about 57 %. The inhibition pattern of both peptides was determined to be uncompetitive, consisting with the result of multiple ligand docking that the binding sites were outside the ACE active pocket. Trp59, Tyr62, Asp121, Arg124, and Ser516 were the key binding sites that contributed to the total binding energy. In addition, saltiness and palatability models were established according to sensory analysis and central composite design. In 0.1 % ∼ 0.3 % NaCl solutions, the addition of DGGRYY and NEFGYSNR could enhance the salty intensity and compensate for the palatability loss caused by salt reduction.

2025-01-01·Brain Research

Molecular profiling of a rat model of vascular dementia: Evidences from proteomics, metabolomics and experimental validations

Article

作者: Ban, Wenming ; Zhen, Yilan ; Zhu, Guoqi ; Wang, Xueqing ; Wang, Jingji ; Yang, Jun

Decrease of cerebral blood flow is the primary cause of vascular dementia (VD), but its pathophysiological mechanisms are still not known. This study aims to profile the molecular changes of a rat model of VD induced by bilateral common carotid artery ligation. The Morris water maze and new object recognition tasks were used to test the cognitive function of rats. Hematoxylin and Eosin (HE) staining was used to detect pathological changes in the hippocampus. After confirming the model, proteomics was used to detect differentially expressed proteins in the hippocampus, and metabolomics was used to detect differential metabolites in rat serum. Thereafter, bioinformatics were used to integrate and analyze the potential molecular profile. The results showed that compared with the sham control group, the spatial and recognition memory of the rats were significantly reduced, and pathological changes were observed in the hippocampal CA1 region of the model group. Proteomic analysis suggested 206 differentially expressed proteins in the hippocampus of VD rats, with 117 proteins upregulated and 89 downregulated. Protein-protein interaction network analysis suggested that those differentially expressed proteins might play crucial roles in lipid metabolism, cell adhesion, intracellular transport, and signal transduction. Metabolomics analysis identified 103 differential metabolites, and comparison with the human metabolome database revealed 22 common metabolites, which predicted 265 potential targets. Afterwards, by intersecting the predicted results from metabolomics with the differentially expressed proteins from proteomics, we identified five potential targets, namely ACE, GABBR1, Rock1, Abcc1 and Mapk10. Furthermore, western blotting confirmed that compared with control group, hippocampal GABBR1 and Rock1 were enhanced in the model group. Together, this study showed the molecular profile of VD rats through a combination of proteomics, metabolomics, and experimental confirmation methods, offering crucial molecular targets for the diagnosis and treatment of VD.

2025-01-01·Food Chemistry

One-step cascade amplification system based on entropy-driven catalysis and DNAzyme triggered DNA walker for label-free detection of acetamiprid

Article

作者: Zhu, Li ; Lu, Hao ; Zhang, Xuemei ; Zhu, Liping ; Yang, Li ; Xiong, Xiaoli ; Xiao, Ting

Herein, an electrochemical aptasensor for highly sensitive detection of acetamiprid (ACE) was constructed based on a one-step cascade amplification strategy. This innovative strategy integrated DNA walker containing DNAzyme sequence into entropy-driven catalysis (EDC) system. The trigger strand was released by aptamer-specific binding to ACE, initiating the EDC amplification circuit and delivering DNA walker strands. The dangling DNA walker continuously bound and cleaved hairpin substrate to form G-quadruplex fragments with the assistance of Mg²⁺. The G-quadruplex fragments folded and captured hemin to form multitudinous G-quadruplex/hemin complexes in the presence of K⁺, generating significantly enhanced current, enabling enzyme-free, label-free and highly sensitive detection of ACE, with a linear detection range of 100 fM to 50 nM and a detection limit of 68.36 fM (S/N = 3). The constructed aptasensor achieved the reliable detection of ACE in vegetable soil and cucumber samples, demonstrating its potential application prospects in environmental protection and food supervision.

278

项与 ACE 相关的新闻（医药）

2024-10-23

·凯莱英药闻

针对IgA肾病源头！全球首款APRIL单抗公布III期临床积极结果

欢迎关注凯莱英药闻 2024年10月22日，大冢制药公布了sibeprenlimab用于治疗成人免疫球蛋白 A 肾病 (IgA 肾病) 的 3 期临床试验积极顶线中期数据。该研究是一项多中心、随机、双盲、安慰剂对照试验，在约 530 名（同类中规模最大的）患有免疫球蛋白 A (IgA)肾病的成年患者中开展，旨在评估每四周皮下注射 400 mg的 sibeprenlimab 与安慰剂相比的疗效和安全性，结果显示治疗 9 个月后，使用sibeprenlimab的患者24小时尿蛋白/肌酐比值（UPCR）降低具有统计学意义和临床意义；药物安全性与之前报告的数据一致。公司计划与 FDA 一起审查中期结果，以便提交潜在的监管申请以加速批准；该研究仍在继续，最终结果预计将于 2026 年初公布。关于Sibeprenlimab Sibeprenlimab（VIS649）是一款抗增殖诱导配体（APRIL）单抗，通过结合和中和 APRIL，减少IgA和致病性半乳糖缺乏型 IgA1 (Gd-IgA1)的数量；通过减少 Gd-IgA1 的产生，sibeprenlimab 可能有助于减缓肾脏损伤和向终末期肾病(ESKD) 进展。该药物最初由Visterra公司开发，2018年大冢制药以约4.3亿美元的价格收购Visterra，获得sibeprenlimab以及一系列针对IgA肾病和其它肾脏疾病等适应症在内的在研产品。该药物2期临床试验的完整结果已发表在《新英格兰医学杂志》（NEJM）并于2023年肾脏病学会（ASN）大会中公布，结果显示：与安慰剂治疗相比，IgA肾病患者接受为期12个月的sibeprenlimab治疗后，蛋白尿状况显著减少。在第12个月时，与基线相比，接受2、4和8 mg/kg剂量的sibeprenlimab及安慰剂各组患者24小时尿蛋白/肌酐比值（UPCR）的几何平均比值降幅分别为47.2%、58.8%、62.0%和20.0%。接受2、4和8 mg/kg sibeprenlimab与安慰剂组患者的肾小球滤过率（eGFR）年变化分别为-2.7、+0.2、-1.5和-7.4 ml/min/1.73m2；说明使用sibeprenlimab后eGFR趋于稳定。不良事件（TEAE）的发生率与安慰剂类似，随访至第16个月期间，未发现不良毒性或临床意义上的免疫抑制证据。关于APRIL药物 APRIL是肿瘤坏死因子 (TNF) 家族中的一种细胞因子，能够促进 B 细胞存活和类别转换，产生 IgA，特别是Gd-IgA1，这种 IgA1在肾脏中形成免疫复合物。 IgA肾病患者体内APRIL会刺激到淋巴细胞，生成更多的致病性IgA；如果能阻断这一过程，那么理论上就可以从源头阻断IgA肾病。据不完全统计，目前针对APRIL在研的药物约十余种，尚未有产品上市获批。关于IgA肾病免疫球蛋白A肾病（即IgA肾病/IgAN）是一种免疫复合物引起的肾小球肾炎，通常表现为血尿、蛋白尿及进展型肾衰竭。IgAN虽然被认为属罕见病，但却是全球原发性肾脏疾病的最常见原因。IgAN与肾脏炎症、血尿及蛋白尿有关。患者最终会进展为肾衰竭或终末期肾脏疾病（ESRD）；在整个疾病过程中，多达50%的患者需要进行透析或肾脏移植。全球及中国IgAN患者人数未来预计保持相对稳定。根据弗若斯特沙利文报告，全球IgAN患者人数由2016年的887.64万人增加至2020年的926.69万人（包括中国的220万人）。预计全球IgAN患者总数将于2025年达到973.06万人（包括中国230万人），并于2030年达到1,016.52万人（包括中国237万人）。根据艾昆玮测算，2020 年到2025 年，全球IgA 肾病治疗药物市场预计将从5.67 亿美元增至 11.96 亿美元，CAGR 达16.1%。预计到 2030 年全球 IgA肾病治疗药物市场总规模将达到数十亿美元甚至更高水平。目前IgAN的治疗方案仍以支持治疗以及缓解症状为主，支持治疗主要以血管紧张素转化酶抑制剂（ACEI）和血管紧张素受体拮抗剂（ARB）控制血压以降低尿蛋白，糖皮质激素、免疫抑制剂等也被用于长期的治疗。当前治疗方案可能伴随较多的副作用，并且临床效果有限。 Iptacopan（伊普可泮，商品名：Fabhalta）于2024年8月获FDA加速批准用于降低成人IgA肾病（IgAN）患者的蛋白尿水平；Iptacopan是一款口服、强效、选择性、小分子FB抑制剂，通过作用于补体系统C5末端通路的上游；它可能在治疗多种替代通路功能异常导致的疾病同时，不影响其它补体通路介导的对微生物入侵的免疫反应，降低患者受到感染的风险。 Nefecon是一种布地奈德的缓释制剂，也是第一款获FDA及EMA批准上市，用于治疗IgAN的药品，通过在回肠派尔集合淋巴结处释放布地奈德进行治疗。该药物于2023年11月在国内获批，云顶新耀拥有在大中华区的开发权。 Sparsentan是一种双重内皮素血管紧张素受体拮抗剂(DEARA)，靶向阻断内皮素A受体和血管紧张素II亚型1受体通路，能够保护肾小球足细胞，防止肾小球硬化和系膜细胞增生，并减少蛋白尿产生；它是首个获批的IgA肾病非免疫抑制疗法。参考资料 1、公司官网 2、国信证券、华创证券感谢关注、转发，转载授权、加行业交流群，请加管理员微信号“hxsjjf1618”。 “在看”点一下

临床结果临床2期临床3期临床1期

2024-10-14

·GlobeNewswire-Health Care

Helio Genomics’ Methylation Model Score for Assessing Prognosis and Treatment Response in Patients with Hepatocellular Carcinoma Presented as Top Abstract at the 2024 San Antonio Liver Cancer Symposium

IRVINE, Calif., Oct. 14, 2024 (GLOBE NEWSWIRE) -- Helio Genomics (“Helio” or “the Company”), an AI-driven healthcare company specializing in diagnostics technology and test development for cancer detection, showcased the results from their latest collaboration with Ochsner Health, demonstrating the utility of cell-free DNA (cfDNA) methylation-based biomarkers for assessing biological aggressiveness and prognosis in patients with hepatocellular carcinoma (HCC) on Friday, October 11, 2024 at the 2024 San Antonio Liver Cancer Symposium in San Antonio, Texas. Dr. Shivani Mahajan, Head of Computational Science at Helio Genomics, presented a poster from the longitudinal study, entitled “Cell-free DNA methylation biomarkers for evaluating prognosis and treatment response in patients with hepatocellular carcinoma”. Additionally, Helio’s abstract was awarded as one of the top three abstracts by the Symposium Committee. “We are thrilled to be one of three top abstracts selected at the San Antonio Liver Cancer Symposium,” said Dr. Shivani Mahajan, Helio’s Head of Computational Science. “This award underscores the importance of having reliable biomarkers that can evaluate the biological aggressiveness in HCC patients to help physicians make better treatment decisions for improved patient outcomes. In this study, Helio’s methylation score outperformed other established metrics in predicting patients at high risk of progression and in identifying treatment responders, demonstrating that cfDNA methylation-based biomarkers have both diagnostic and prognostic utility.” “We were thrilled to collaborate with Helio Genomics, a company that is at the forefront of diagnostic technologies for early cancer detection,” said Paul Thevenot, PhD, Associate Professor of Research at Ochsner Health. “Reliable prognostic biomarkers for HCC are lacking and this study demonstrates that cfDNA methylation-based biomarkers have tremendous potential for addressing this unmet need in the field,” said Ari J. Cohen, MD, FACS, FAASLD, Director of the Multi-Organ Transplant Institute and Director of Transplant Research at Ochsner Health. Data Highlights: In this longitudinal study cohort (n=108), all enrolled patients were previously diagnosed with liver cirrhosis with varying underlying etiologies.All patients received liver-directed therapies.Blood specimens were drawn from patients at multiple time points starting at diagnosis (pre-treatment).Helio’s automated wet lab platform, ECLIPSE™, was used to generate targeted cfDNA methylation sequencing data.A model utilizing cell-free DNA (cfDNA) methylation-based features was trained (using a separate cohort) to distinguish between HCC and cirrhotic patients and applied to an independent longitudinal cohort of HCC patients to calculate a methylation score for each patient at multiple time points.Helio’s methylation model score from pre-treatment blood specimens outperformed other metrics such as the ALBI score, GALAD score, MELD score, Child-Pugh score, cumulative lesion size and biomarkers like AFP, AFP-L3 and DCP in predicting patient outcomes and can accurately classify patients with low or high risk of progression.Patients who responded to liver-directed therapy showed a significantly larger decline in their methylation score compared to those who did not respond and progressed to advance-stage disease.With biopsy contraindicated in early-to-intermediate-stage disease (BCLC A-B), circulating mediators (biomarkers / ctDNA) provide the best potential targets for assessing prognosis, identifying treatment responders, and ultimately developing personalized approaches to treatment. Helio was founded in 2016 and is headquartered in Irvine, CA. For more information, please visit our website at www.heliogenomics.com or www.linkedin.com/company/heliogenomics; information that may be important to investors will be routinely posted in both locations. About ECLIPSE™The ECLIPSE platform is Helio’s proprietary laboratory process designed to improve the accuracy and efficiency of cfDNA methylation pattern detection and quantification by optimizing each step of the cfDNA methylation capture process, which includes automated cfDNA extraction, library generation and enzymatic conversion, targeted capture and NGS. In particular, our ECLIPSE platform uses an enzymatic conversion approach as opposed to a traditional bisulfite conversion, which yields a higher quantity and quality of converted DNA. About Helio Genomics Helio Genomics is a commercial stage, AI-driven healthcare company specializing in diagnostics technology and test development for cancer detection. HelioLiver is a multi-analyte blood test that evaluates cell free DNA (cfDNA) methylation patterns, serum protein markers, and demographic information for the detection of hepatocellular carcinoma (HCC). For more information, please visit us at www.heliogenomics.com. Investor Contact: Jeremy Feffer Managing Director LifeSci Advisors jfeffer@lifesciadvisors.com

临床研究临床结果

2024-10-08

·圣因生物SanegeneBio

聚焦全国高血压日，高血压防控不容忽视

2024年10月8日是第27个全国高血压日。也就在前不久，《中国高血压防治指南（2024年修订版）》正式发布。国家高度重视高血压防控工作，预防和控制高血压越来越成为全社会的一大重要任务，在此呼吁公众提高对高血压的认识和防控。高血压被称为“沉默的杀手”，是心血管疾病的主要危险因素，也是亚洲和世界范围内死亡和发病的主要原因。仅在中国，高血压患病人数高达2.45亿人[1]，每年有大约180万人因高血压死亡[2]。高血压患病率逐年升高，近年来在中青年人群的上升趋势更为明显。然而高血压却多由于无明显症状而被很多人忽视，以致于病情逐渐加重引发并发症，严重影响患者的生活质量，甚至危及生命。高血压管理任重道远高血压是一种需要终身管理的慢性疾病，目前包括三种治疗措施：生活方式干预、药物治疗和器械干预性疗法。生活方式干预高钠、低钾膳食，超重和肥胖，吸烟，过量饮酒，心理社会因素等成为我国人群重要的高血压危险因素[3]。故高血压患者均应进行生活方式干预，有效预防和控制高血压的发展，主要包括：低盐、健康膳食，控制体重，戒烟，限制饮酒，运动干预，减轻精神压力，保持健康睡眠等。生活方式干预对于中青年高血压患者尤为重要，在中青年阶段及早干预、改变不良生活方式有利于遏制高血压以及心血管病的发生、发展[4]。药物治疗生活方式干预可帮助降低血压，但大多数高血压患者仍然需要药物治疗。针对高血压患者，医生会根据特殊人群的类型、合并症选择针对性的药物，进行个体化治疗。高血压患者应该遵循医嘱，按照医生建议服用降压药物，不可擅自停药或换药。一旦使用药物出现不良作用，患者应及时告知医生。中国高血压防治指南推荐的常用降压药包括钙通道阻滞剂（CCB）、血管紧张素转换酶抑制药（ACEI）、血管紧张素受体阻滞药（ARB）、噻嗪类利尿剂、β 受体阻滞剂等[2]。器械干预性疗法目前也有创新的非药物降压治疗方法正处于研究中，例如，对于药物难以控制血压或药物依从性差的高血压患者可考虑肾动脉交感神经消融术（RDN）作为辅助治疗手段。国家政策的指引，创新技术和药物的研究，都将加速推动高血压治疗方案的创新突破，为高血压患者带来更多获益。聚焦高血压创新RNAi疗法前景可期药物治疗作为目前高血压疾病的主要治疗策略，患者依从性差是当前最大的挑战，寻找有效、安全、便捷的药物疗法具有重要的临床意义。 RNAi疗法作为一种新型治疗方式，具有药物作用效果持久、安全性好、患者用药频率低、依从性高等差异化优势，在慢病领域展现出应用潜力，有望满足高血压疾病领域高度未满足的医疗需求，为高血压患者带来新的治疗选择和长期获益。圣因生物和信达生物合作开发的一款靶向血管紧张素原（AGT）的siRNA药物SGB-3908，用于治疗高血压。临床前试验数据显示，SGB-3908可抑制AGT在肝脏中的合成，从而可能导致AGT蛋白的持久减少，进一步导致血管收缩素 (Ang) II 的减少，最终起到舒张血管、降低血压的效果。SGB-3908采用了圣因生物独特创新的新一代siRNA药物平台技术，使得药物具有更加优异的活性和药效持久性，且安全耐受性良好。目前SGB-3908已在中国进入临床1期且并完成首例受试者给药。拓展阅读：圣因生物和信达生物共同宣布靶向AGT的siRNA药物临床I期研究完成首例受试者给药参考资料： [1] 中国心血管健康与疾病报告2022概要[J]. 中国循环杂志. 2023, 38(6): 583-612. [2] Frieden TR. China Can Substantially Reduce Its High Burden of Stroke and Heart Attack [J]. China CDC Weekly, 2020. DOI:10.46234/ccdcw2020.211. [3] 中国高血压防治指南修订委员会, 高血压联盟(中国), 中国医疗保健国际交流促进会高血压病学分会, 等. 中国高血压防治指南(2024年修订版)[J]. 中华高血压杂志, 2024, 32(7): 603-700. [4] 刘靖, 卢新政, 陈鲁原, 等. 中国中青年高血压管理专家共识[J]. 中华高血压杂志, 2020, 28(4): 316-324. | 圣因差异化优势 | 频获认可 | | SGB-3403 高胆固醇血症 | | SGB-3908 高血压 | | SGB-9768 补体介导的肾脏疾病 | | 圣因故事 |

临床2期核酸药物