排名前五的靶点	数量

PCSK9(前蛋白转化酶枯草杆菌蛋白酶Kexin-9)	3
MAPKAPK2 x TNF-α	3
GLP-1R(胰高血糖素样肽-1受体)	2
AT1R(血管紧张素II-1型受体)	2
PSD95(DLG4蛋白)	1

关联

项与深圳信立泰药业股份有限公司相关的药物

Fotagliptin Benzoate

苯甲酸福格列汀

靶点

DPP-4

作用机制

DPP-4抑制剂

在研机构

深圳信立泰药业股份有限公司

原研机构

重庆复创医药研究有限公司

在研适应症

2型糖尿病

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

中国

首次获批日期2024-06-28

Allisartan Isoproxil/Amlodipine Besylate

阿利沙坦酯/苯磺酸氨氯地平

靶点

AT1R x L-type calcium channel

作用机制

AT1R拮抗剂 [+1]

在研机构

深圳信立泰药业股份有限公司

原研机构

深圳信立泰药业股份有限公司

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

中国

首次获批日期2024-05-15

Enarodustat

恩那司他

靶点

HIF-PHs

作用机制

HIF-PHs抑制剂

在研机构

深圳信立泰药业股份有限公司 [+2]

原研机构

Japan Tobacco, Inc.

在研适应症

慢性肾衰竭贫血 [+3]

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

日本

首次获批日期2020-09-25

150

项与深圳信立泰药业股份有限公司相关的临床试验

NCT06830954

/ Not yet recruiting临床1期

Bioequivalence Study of Fluvastatin Sodium Extended Release Tablets in Healthy Participants

The purpose of this study is to evaluate the bioequivalence of the test preparation (Fluvastatin sodium extended release tablet, 80 mg) manufactured by Shenzhen Salubris Pharmaceuticals Co., Ltd. and the reference preparation (80 mg) manufactured by Beijing Novartis Pharma Co., Ltd. in healthy participants under fasting and fed conditions.

开始日期2025-02-01

申办/合作机构

深圳信立泰药业股份有限公司

CTR20243967

/ Recruiting临床2期

评价SAL0120片治疗慢性肾脏病（CKD）患者有效性和安全性的多中心、随机、双盲、安慰剂平行对照的II期临床研究

主要目的 1.评估SAL0120片治疗慢性肾脏病患者的有效性。次要目的 1.评估SAL0120片治疗慢性肾脏病患者的其他有效性结果。 2.评估SAL0120片治疗慢性肾脏病患者的安全性。 3.评价SAL0120片在中国慢性肾脏病患者中的药代动力学特征探索性目的（如必要）评估不同剂量的SAL0120片在慢性肾脏病患者中剂量-暴露-效应关系。

开始日期2024-12-26

申办/合作机构

深圳信立泰药业股份有限公司

CTR20244587

/ Recruiting临床3期

在S086单药治疗不能有效控制血压的原发性高血压患者中，评价S086联合氨氯地平治疗的有效性和安全性的多中心、随机、双盲、平行对照的Ⅲ期临床研究

主要目的：S086联合氨氯地平治疗原发性高血压的有效性；次要目的：S086联合氨氯地平治疗原发性高血压的安全性；

开始日期2024-12-26

申办/合作机构

深圳信立泰药业股份有限公司

100 项与深圳信立泰药业股份有限公司相关的临床结果

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0 项与深圳信立泰药业股份有限公司相关的专利（医药）

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项与深圳信立泰药业股份有限公司相关的文献（医药）

2025-04-01·Clinical Drug Investigation

Pharmacokinetics, Pharmacodynamics, and Safety Evaluation of the Novel HIF-PH Inhibitor Enarodustat: An Open-Label Phase I Study in Healthy Chinese Participants

Article

作者: Wang, Xiaohong ; Liu, Dongyang ; Cui, Cheng ; Li, Haiyan ; Zhang, Ruijie ; Niu, Xiaoye ; Lin, Wei ; Liu, Zichen ; Geng, Lei

BACKGROUND AND OBJECTIVES:

Enarodustat is a hypoxia-inducible factor-prolyl hydroxylase inhibitor. We evaluated the pharmacokinetics, pharmacodynamics, and safety profile of domestic enarodustat (SAL-0951) and analyzed the influence of ethnic factors.

METHODS:

In this phase I study, healthy Chinese participants received single and multiple oral doses (1, 5, and 15 mg) of SAL-0951 while in a fasted state. We monitored the pharmacokinetics, pharmacodynamics, and safety characteristics and analyzed the impact of ethnicity on pharmacokinetic characteristics.

RESULTS:

In total, 33 healthy Chinese participants were enrolled; the mean age was 31.2 ± a standard deviation of 5.5 years. After single doses of 1, 5, and 15 mg were administered under fasted conditions, SAL-0951 was rapidly absorbed. Mean maximum plasma concentration and area under the plasma concentration-time curve from time 0 to the last quantifiable concentration increased dose proportionately from 0.14 to 2.54 μg/mL and from 0.63 to 9.50 h × μg/mL, respectively. The elimination half-life was 6.13, 6.32, and 6.74 h, respectively, in these three groups, and the mean value of apparent clearance ranged from 1.64 to 1.89 L/h. SAL-0951 was excreted mostly as the parent compound. It reached a stable concentration after 5 days of multiple-dose administration. We observed no drug accumulation or time-dependent pharmacokinetic characteristics and no significant difference in pharmacokinetic characteristics between Chinese and Japanese participants.

CONCLUSION:

SAL-0951 was safe and well tolerated in healthy Chinese participants and had a linear pharmacokinetic profile. We found no ethnic differences in the pharmacokinetic characteristics of the drug between Chinese and Japanese populations.

CLINICAL TRIAL REGISTRATION:

Registered at Chinadrugtrials.org.cn, registration number CTR2020245.

2024-12-17·ACS Omega

Revealing Local Structure of Angiotensin Receptor-Neprilysin Inhibitor (S086) Drug Cocrystal by Linear and Nonlinear Infrared Spectroscopies

Article

作者: Li, Song ; Yan, Jie ; Yu, Pengyun ; Xu, Wenjie ; Xu, Haiyan ; Zhao, Juan ; Yang, Fan ; Wang, Jianping

Structurally knowing the active sites of a drug is important for understanding its therapeutic functions. S086 is a novel angiotensin receptor-neprilysin inhibitor that consists of the molecular moieties of EXP3174 (the active metabolite of the angiotensin receptor blocker losartan) and sacubitril (a neprilysin inhibitor prodrug) in a 1:1 molar ratio. There are two forms of cocrystals of S086, namely, ξ-crystal and α-crystal, which were formed both via intermolecular coordination bonding to calcium ions, with the aid of internal water. The binding state of multiple carboxyl anions (COO^-) to Ca²⁺ of EXP3174 and sacubitril was examined in this study using infrared (IR) absorption spectroscopy, in which the asymmetric stretching (as) and symmetric stretching (ss) modes of the COO^- groups were used as IR probes. Ultrafast two-dimensional (2D) IR spectroscopy was utilized for spectrally assigning the origin of multiple COO^- groups by the presence or absence of interchromophore vibrational coupling. Key structural variation between the two crystal forms was found: in the unit cell of ξ-crystal, the ratio of "bridging" and "bidentate" types of COO^- binding to Ca²⁺ for four EXP3174 molecules is 2:2, while the ratio is predicted to be 3:1 in the case of α-crystal. However, in both crystals, four sacubitril molecules are believed to similarly form a "trident" type of COO^- binding to Ca²⁺. Our study demonstrates that linear and nonlinear IR spectroscopies can be used to characterize local crystal structures of drugs and reveal subtle difference between similar crystal structures.

2024-09-01·JACC. Asia

Efficacy and Safety of Sacubitril/Allisartan for the Treatment of Primary Hypertension

Article

作者: Yan, Jie ; Lu, Xiao-Hong ; Zhang, Jin ; Wang, Qiang ; Zhou, Xiang-Nan ; Sun, Jing-Chao ; Chen, Shao-Xing ; Li, Jin-Feng ; Ge, Qian ; Zhang, Wei ; Li, Yan ; Liu, Zi-Chen ; Wang, Ji-Guang ; Xu, Wen-Jie

Background:

The prevalence of hypertension still increases with the very rapidly increasing longevity in some countries, such as China. The control rate remains low.

Objectives:

This randomized, double-blind, phase 3 study assessed the efficacy and safety of sacubitril/allisartan, compared with olmesartan in Chinese patients with mild-to-moderate hypertension.

Methods:

Eligible patients aged 18 to 75 years (n = 1,197) with mild-to-moderate hypertension were randomized to receive sacubitril/allisartan 240 mg (n = 399), sacubitril/allisartan 480 mg (n = 399), or olmesartan 20 mg (n = 399) once daily for 12 weeks. Patients who completed the 12-week treatment then received another 12-week extended treatment (n = 1,084) and 28-week prolonged treatment (n = 189). The primary end point was a reduction in clinic mean sitting systolic blood pressure (msSBP) from baseline at 12 weeks.

Results:

Sacubitril/allisartan 240 mg/d provided a greater reduction in msSBP than olmesartan at 12 weeks (between-group difference: -1.9 mm Hg [95% CI: -4.2 to 0.4 mm Hg]; P = 0.0007, for noninferiority). Sacubitril/allisartan 480 mg/d provided a significantly greater reduction in msSBP than olmesartan at 12 weeks (between-treatment difference: -5.0 mm Hg [95% CI: -7.3 to -2.8 mm Hg]; P < 0.001, for superiority). Greater reductions in 24-hour, and daytime and nighttime systolic and diastolic blood pressure were also observed with both doses of sacubitril/allisartan compared with olmesartan (P ≤ 0.001 for 480 mg/d). The blood pressure reductions tended to be dose-dependent for sacubitril/allisartan. Sacubitril/allisartan was well tolerated, and no cases of angioedema or death were reported.

Conclusions:

Sacubitril/allisartan is effective for the treatment of hypertension and well tolerated in Chinese patients.

1,031

项与深圳信立泰药业股份有限公司相关的新闻（医药）

2025-05-09

·九洲药业

【行研】共晶在药物研发中的应用与发展

在药物研发中，超过40%的候选化合物因溶解度低、稳定性差等理化性质问题而夭折。如何在不改变药物分子化学结构的前提下优化其性能？药物共晶技术凭借其独特的优势，成为近年来药物固态化学领域的研究热点。Jiuzhou News 药物共晶：超分子化学的巧妙设计1. 定义与核心特征药物共晶（Pharmaceutical Cocrystal）是活性药物成分（API）与共晶形成物（CCF）通过氢键、π-π堆积、范德华力等非共价键结合形成的多组分晶体，两者在室温下均为固体[1]。其核心特征包括：化学结构保留：API的分子结构未被破坏，仅通过物理结合优化其性能。广谱适用性：适用于有机酸、有机碱及中性分子，无需API具备可解离位点（与成盐技术相比）。▲图1 药物活性成分的不同固体形式[2]2. 传统固体形态的局限性传统药物固态形式（如多晶型、盐型和无定形）存在如下显著缺陷：多晶型：种类有限，溶解性改善幅度小（通常仅提升约2倍）。盐型：依赖API的可解离位点，适用范围受限。无定形：热力学稳定性差，易发生相变。相较而言，共晶通过灵活选择CCF，可显著提升药物溶解度、稳定性及工艺可控性。共晶技术的核心优势1. 改善溶解性与生物利用度共晶通过重构分子间相互作用，可改善药物的溶解度和溶出速率。例如：芹菜素-茶碱共晶的固有溶出速率提升8.4倍；中性药物（如布洛芬）通过共晶技术实现显著增溶。2. 增强稳定性共晶可抑制API的吸湿性、高温下相变及降解。例如：丙泊酚-异烟酰胺共晶将液态丙泊酚转化为热稳定性更高的固态形式[3]；达格列净-柠檬酸共晶，有效避免了生产过程中脱溶剂的风险，吸湿性也得到显著改善[4]。3. 优化机械性能共晶可改善API的流动性、可压性及机械强度。例如：替莫唑胺-橙皮素共晶因分子排列优化，更易于直接压片[5]。4. 保持原有药效，实现协同治疗共晶仅通过物理结合改善药物性质，不改变药理活性，不影响API的靶点作用。可将多种API结合为单一共晶，简化联合用药。如抗SARS-CoV-19药物Paxlovid的多组分设计。5. 生产工艺灵活可控共晶可通过溶液法、研磨法、超临界流体和热熔挤出等多种方法制备，且化学计量比固定（如1:1摩尔比），可便于制剂工艺控制。6. 拓展专利保护范围药物共晶通过申请专利，获得知识产权，可延长药物生命周期。例如：诺华的抗心衰药物Entresto®（诺欣妥）通过共晶设计突破专利壁垒，成为全球首个获批的共晶药物[6]。共晶制备方法：从传统到创新1. 传统方法固体法：干法/湿法研磨，绿色环保但效率低，放大生产受限（如槲皮素-烟酰胺共晶需精确控制乙醇用量）。溶液法：蒸发结晶、冷却结晶等，可获高纯度共晶，但对溶剂依赖性高（如槲皮素-脯氨酸共晶需延长蒸发时间）。▲表1 药物共晶制备方法比较2. 创新技术热熔挤出技术：无溶剂连续生产，降低热降解风险（如羟基酪醇-烟酰胺共晶熔点降至135°C，稳定性提升）。超临界流体技术：利用超临界CO₂制备高质量共晶（如槲皮素-脯氨酸共晶溶解度提升2倍），环保但设备成本高。▲图2热熔挤出装置示意图[6]典型案例与产业化应用1.Entresto®（诺欣妥）设计亮点：沙库巴曲（脑啡肽酶抑制剂）与缬沙坦（血管紧张素受体拮抗剂）以1:1摩尔比形成共晶，协同抗心衰。成药性提升：解决沙库巴曲游离酸的吸湿性问题，提高制剂稳定性。2.Steglatro®（艾托格列净-L-焦谷氨酸共晶）通过共晶设计提升糖尿病药物的溶解度，降低给药剂量。3.抗病毒药物阿德福韦酯共晶调整晶型后显著提高生物利用度，降低临床用药频率。4.信立泰S086（沙库巴曲/阿利沙坦）国内首个1类新药共晶，通过代谢物EXP3174的创新设计突破专利壁垒，展现“老药新用”的开发策略。未来发展与前景1. 法规支持：2018年FDA将共晶归为API的多晶型（“溶剂化物的特殊情况”），简化审批流程，加速共晶药物上市[7]。2. 技术革新：MicroED结构解析与自动化筛选技术推动共晶高效开发。3. 战略潜力：精准药物设计：优化复方制剂与联合疗法（如抗病毒/抗肿瘤多靶点共晶）。专利布局：通过共晶设计规避原研晶型专利，延长药物生命周期。小结药物共晶技术通过超分子设计，在不改变API化学结构的前提下，突破传统固态形式的局限性，成为提升药物成药性的重要工具。随着法规支持和技术进步，共晶将在精准药物设计、复方制剂开发中发挥更大潜力，成为下一代药物研发的“隐形引擎”。其核心优势不仅在于提升现有药物的临床效果，还为联合疗法和新型制剂设计提供了创新路径。参考资料[1] 杜冠华，吕扬.《晶型药物》[M] .第二版.人民卫生出版社，2019,25~26.[2]Zhu B Q, Xia M Y, Ding Z F, et al. Enhancing physical and chemical stability of hygroscopic hydroxytyrosol by cocrystal formation1. IntJPharm,2023.646:123470.[3]Ma X Q, Zhuang C, Wang B C, et al. Cocrystal of apigenin withhigher solubility, enhanced oral bioavailability, and anti-inflammatoryeffect.Cryst Growth Des, 2019,19(10):5531-5537.[4]Liu F, Wang L Y, Li Y T, et al. Protective effects of quercetin againstpyrazinamide induced hepatotoxicity via a cocrystallization strategyof complementary advantages.Cryst Growth Des, 2018,18(7)3729-3733.[5] 孙晶晶,贾丽娜,林波等.药物共晶的研究进展[J].化工学报,2021(2)[6] SPRINGUEL G, LEYSSENS T. Innovative chiral resolution using enantiospecific co-crystallization in solution[J]. Crystal Growth &Design, 2012, 12(7): 3374-3378.[7]Pharmaceutical Quality/CMC , et al. Regulatory Classification of Pharmaceutical Co-Crystals Guidance for Industry,2018免责声明本公众号注明原创的内容权利均属九洲药业所有，未经授权，不得擅自使用或许可他人使用。如需获得授权，请和九洲药业提前联系。已获得授权的，应在授权范围内使用，并注明来源且不得再全部或部分转授权他人。本公众号对转载、分享的内容、陈述、观点判断保持中立，不对所包含内容的合法性、准确性、可靠性或完善性提供任何明示或暗示的保证，该等内容版权归原作者所有，仅供学习参考之用，若对转载、分享的内容有任何权利疑问，烦请联系九洲药业。

申请上市

2025-05-09

·同写意

驯鹿生物伊基奥仑赛注射液获沙特阿拉伯药监局孤儿药资格认定

细胞疗法免疫疗法孤儿药ASH会议

2025-05-07

·健识局

信立泰高血压新药获批临床

近日，据CDE官网显示，信立泰SAL0140片获批临床，用于未控制高血压（包括难治性高血压）。SAL0140是醛固酮合酶（CYP11B2）抑制剂，临床前研究显示，其可选择性抑制醛固酮合成酶的活性，实现抑制醛固酮的合成而不影响皮质醇的水平。在高血压猴模型中，SAL0140可抑制醛固酮的生成，每天用药一次可达到平稳控制血压的疗效。根据相关规定，自受理之日起60日内，若未收到药审中心否定或质疑意见，申请人可按提交的方案开展临床试验。据相关研究报道，目前，中国高血压患病人数约为2.45亿。高血压是最常见的慢性病之一，也是心脑血管病最主要的危险因素。高血压会增加脑卒中、心肌梗死、心力衰竭、肾衰竭等的发病风险。运营｜廿十三药企发“国难财”？重罚3.26亿元！董事长被留置，药企开盘一字跌停新规 | 港交所新政：创新药企可用“保密形式”IPO

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当前项目

药物(靶点)	适应症	全球最高研发状态

硫酸氢氯吡格雷 ( P2Y12 receptor )	心肌缺血更多	批准上市
阿利沙坦酯 ( AT1R )	高血压更多	批准上市
苯甲酸福格列汀 ( DPP-4 )	2型糖尿病更多	批准上市
阿利沙坦酯/苯磺酸氨氯地平 ( AT1R x L-type calcium channel )	原发性高血压更多	批准上市
阿利沙坦酯/吲达帕胺 ( AT1R )	原发性高血压更多	申请上市