A First in Human, Single Center, Single Dose, Randomized, Placebo-controlled, Dose, Escalating Study to Evaluate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Subcutaneously Administered ENT-03S for the Treatment of Obesity and Diabetes

Single center, single-dose, randomized, placebo-controlled, dose-escalating study to evaluate, safety, tolerability, pharmacokinetics, and pharmacodynamics of escalating doses of ENT-03S in obese but otherwise healthy subjects and in subjects with obesity and Type 2 diabetes.

开始日期2023-06-13

申办/合作机构

Metabolics Pharma, Inc.

100 项与 ENT-03 相关的临床结果

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100 项与 ENT-03 相关的转化医学

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100 项与 ENT-03 相关的专利（医药）

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项与 ENT-03 相关的文献（医药）

2024-12-01·DIABETES OBESITY & METABOLISM

A novel, centrally acting mammalian aminosterol, ENT ‐03, induces weight loss in obese and lean rodents

Article

作者: Kinney, William A. ; Zemel, Michael ; Fleming, Alexander ; Zasloff, Michael ; Stewart, Alexandre F. R. ; Zhang, Chen ; Chen, Hsiao‐Huei ; Barbut, Denise ; Hecksher‐Sørensen, Jacob

Abstract:

ENT‐03, a spermine bile acid we recently discovered in the brain of newborn mice acts centrally to regulate energy and metabolism. Obese, diabetic (ob/ob) mice treated with five doses of ENT‐03 over 2 weeks, demonstrated a rapid decrease in blood glucose levels into the range seen in non‐obese animals, prior to any significant weight loss. Weight fell substantially thereafter as food intake decreased, and serum biochemical parameters normalized compared with both vehicle and pair‐fed controls. To determine whether ENT‐03 could be acting centrally, we injected a single dose of ENT‐03 intracerebroventricularly to Sprague–Dawley rats. Weight fell significantly and remained below vehicle injected controls for an extended period. By autoradiography, ENT‐03 localized to the arcuate nucleus of the hypothalamus, the choroid plexus and cerebrospinal fluid. Significant cFos activation occurred in multiple anatomical regions within the hypothalamus and brainstem involved in appetite suppression, food‐entrained circadian rhythmicity, autonomic function, and growth. These data support a role for ENT‐03 in the treatment of type 2 diabetes and obesity. Phase 1 studies in subjects with obesity and diabetes are currently in progress.

2016-03-01·Bioorganic & medicinal chemistry3区 · 医学

Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease

3区 · 医学

Article

作者: Akaji, Kenichi ; Takanuma, Daiki ; Saito, Yota ; Konno, Hiroyuki ; Wakabayashi, Masaki

Synthesis of serine derivatives having the essential functional groups for the inhibitor of SARS 3CL protease and evaluation of their inhibitory activities using SARS 3CL R188I mutant protease are described. The lead compounds, functionalized serine derivatives, were designed based on the tetrapeptide aldehyde and Bai's cinnamoly inhibitor, and additionally performed with simulation on GOLD softwear. Structure activity relationship studies of the candidate compounds were given reasonable inhibitors ent-3 and ent-7k against SARS 3CL R188I mutant protease. These inhibitors showed protease selectivity and no cytotoxicity.

2008-03-01·Bioorganic & medicinal chemistry3区 · 医学

Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety

3区 · 医学

Article

作者: Froehlich, Roland ; Schepmann, Dirk ; Wuensch, Bernhard ; Englberger, Werner ; Jung, Bettina ; Lehmkuhl, Kirstin

Directed by molecular modeling studies the pharmacophoric benzhydryl moiety of the delta opioid receptor agonist SNC80 was separated and the two phenyl residues were attached to different positions of the conformationally constrained 6,8-diazabicyclo[3.2.2]nonane framework in order to find novel delta agonists. The crucial reaction step in the chiral pool synthesis was the establishment of the three carbon bridge by a Dieckmann analogous cyclization of the allyl and propyl derivatives 6 and 7 to yield the mixed methyl silyl acetals 8 and 9, respectively. Stereoselective Grignard reaction, dehydration, and introduction of the pharmacophoric (N,N-diethylcarbamoylbenzyl) residue led to the designed delta receptor agonists 3, ent-3, and 20 with a double bond in the bicyclic framework. Hydrogenation of the allyl derivative 14 was performed with ammonium formate and Pd/C to yield the saturated ligands 24a and 24b. Removal of the allyl substituent with RhCl(3), hydrogenation of the ring system, and re-attachment of the allyl moiety provided the allyl derivatives 4a and 4b. In receptor binding studies with the radioligand [(3)H]-deltorphine II only ent-3 showed considerable delta receptor affinity (K(i)=740 nM). Since ent-3 also interacts with mu receptors (K(i)=250 nM) it belongs to the very interesting compound class of mixed delta/mu ligands.

项与 ENT-03 相关的新闻（医药）

2025-07-01

·药明康德

穿越血脑屏障小分子上市申请递交在即；2-4周一针，罗氏创新双抗使凝血功能恢复正常…… | 一周盘点

▎药明康德本期看点1. ROS1选择性抑制剂zidesamtinib用于接受过酪氨酸激酶抑制剂（TKI）治疗的晚期ROS1阳性非小细胞肺癌（NSCLC）患者，在一项1/2期临床试验中取得积极结果，其上市申请递交在即。2. 早期数据表明，罗氏（Roche）的在研双特异性抗体NXT007有望使血友病A患者的凝血功能恢复正常。3. 用于治疗慢性乙型肝炎病毒（HBV）感染的下一代衣壳组装调节剂ABI-4334在1b期临床试验中展现强力的抗病毒活性，高剂量组患者接受治疗28天，血浆HBV DNA平均降低3.2 log IU/mL。NXT007：公布1/2期临床试验数据罗氏宣布，其新一代在研双特异性抗体NXT007在治疗血友病A的1/2期临床试验中取得积极数据，将推进至3期临床试验。NXT007由罗氏旗下的Chugai Pharmaceutical公司研发，基于已上市药物Hemlibra的框架优化设计，旨在模拟因子VIII功能，同时延长半衰期，提高疗效和用药便利性。该药通过将凝血因子IXa和X桥接在一起，激活体内自然凝血级联反应，有望使血友病A患者的凝血功能恢复正常，并减少治疗负担。在这项研究中，30名12至65岁、无因子VIII抑制剂，且既往未接受过Hemlibra治疗的血友病A患者在接受了4至6周的负荷剂量后，在维持期每2至4周皮下注射递增剂量的NXT007。结果显示，高剂量组（B-3和B-4）的患者在整个维持期内均保持止血正常化状态，未出现需治疗的出血事件。安全性方面，NXT007的耐受良好，目前未报告血栓栓塞事件。Zidesamtinib：公布1/2期临床试验数据Nuvalent公司公布了其新型ROS1选择性抑制剂zidesamtinib在1/2期临床试验ARROS-1中的关键积极数据。该试验针对接受过TKI治疗的晚期ROS1阳性NSCLC患者。Zidesamtinib是一种具脑渗透性的ROS1抑制剂，设计用以治疗那些对现有ROS1抑制剂具抗性的癌症，包含那些带有G2032R、S1986Y/F、L2026M或D2033N突变的肿瘤。结果显示，在117例曾接受过TKI治疗的ROS1阳性NSCLC患者中（其中50%曾接受过≥2种ROS1 TKI±化疗），由盲态独立中心审查（BICR）评估的客观缓解率（ORR）为44%，初步估计的缓解持续率在12个月时为78%，18个月时为62%。在其中55名曾接受过1种ROS1 TKI（克唑替尼或恩曲替尼）±化疗的患者中，ORR为51%，初步估计的缓解持续率在12和18个月时均为93%。Zidesamtinib还显示出颅内抗肿瘤活性，对携带ROS1 G2032R耐药突变的肿瘤也有作用，整体安全性良好，剂量减少和停药的比例较低，分别为10%和2%。该公司计划于2025年7月启动滚动提交zidesamtinib的新药申请（NDA），目标在2025年第三季度完成。ABI-4334：公布1b期临床试验数据Assembly Biosciences公司公布了其在研下一代衣壳组装调节剂ABI-4334用于治疗慢性HBV感染患者的1b期临床试验数据。此前公布的150 mg剂量组的结果显示，ABI-4334显示出很强的抗病毒活性，在28天的治疗中，血浆HBV DNA平均降低了2.9 log IU/mL。此次公布的400 mg剂量组的结果类似于先前的报道，在28天的治疗中，血浆HBV DNA平均降低了3.2 log IU/mL。此外，在400 mg剂量下继续观察到ABI-4334良好的安全性和耐受性，半衰期支持每日一次口服给药。TERN-601：公布1期临床试验数据Terns Pharmaceuticals公司公布了其每日一次在研减重疗法TERN-601在肥胖或超重健康成年人中进行的1期试验积极结果。TERN-601是一种口服小分子胰高血糖素样肽-1（GLP-1）受体激动剂，由Terns内部研发。TERN-601通过Terns内部基于结构的药物研发技术设计，采用该公司专有的三维定量构效关系（QSAR）模型所开发。此次公布的结果显示，TERN-601在治疗肥胖方面表现出显著的疗效和良好的安全性。在28天内，每日一次给药可实现统计学显著且呈剂量依赖性的体重减轻。在最高剂量组中，有67%的患者体重减轻≥5%。其独特的药代动力学特性使其在24小时内维持平稳的血药浓度曲线，有效半衰期为9-10小时，支持每日一次给药。此外，药物在肠道中的暴露量高于血浆，且游离药物比例低，从而在不牺牲耐受性的前提下实现了有意义的体重减轻。安全性方面，未出现因治疗导致的中断、减量或停药，＞95%的胃肠道不良事件为轻度，患者的肝酶、生命体征和心电图均无明显变化。ENT-03：公布1a期临床试验数据Metabolics Pharma公司公布了其候选药物ENT-03在肥胖和糖尿病患者中开展的1a期临床试验的的初步结果。该研究数据显示，在所有测试剂量下，ENT-03均表现出良好的安全性和耐受性。在较高剂量组中，ENT-03在减轻体重和提高胰岛素敏感性方面呈现出积极趋势。ENT-03是一种新型中枢神经系统作用的氨基类固醇化合物，具有蛋白酪氨酸磷酸酶1B（PTP1B）抑制活性。它通过作用于大脑中调控能量代谢和血糖平衡的神经回路，达到调节葡萄糖水平、改善胰岛素敏感性并促进体重减轻的效果。临床前研究表明，ENT-03作为单药疗法有效，并且在与GLP-1受体激动剂联合使用时表现出累加效应。此外，ENT-03在停药后仍可维持较长时间的体重降低以及血糖和胰岛素水平的正常化。APR-1051：公布联合治疗1期试验的初步数据Aprea Therapeutics公司公布了其下一代口服WEE1抑制剂APR-1051治疗HPV阳性头颈部鳞状细胞癌患者的新临床数据。APR-1051是一种口服、高选择性的WEE1抑制剂，旨在最大限度地减少脱靶活性并优化药理选择性。该疗法目前正在1期临床试验ACESOT-1051中对携带DDR相关通路基因突变（DDR）的晚期实体瘤患者进行评估。该试验中，一名62岁HPV阳性的晚期口咽鳞状细胞癌男性患者，既往接受过三线铂类治疗后进展，在接受每日口服一次70 mg亚治疗剂量的APR-1051后实现疾病稳定，首次影像学评估时肿瘤缩小了5%。该患者对治疗的耐受性良好，未报告剂量限制性毒性。参考资料（可上下滑动查看）[1] LOMOND THERAPEUTICS ANNOUNCES U.S. FDA CLEARANCE OF IND APPLICATION FOR LONITOCLAX, A SELECTIVE BCL2 INHIBITOR WITH LIMITED IMMUNE SUPPRESSION AND IMPROVED SAFETY COMPARED TO VENETOCLAX AND VENETOCLAX- LIKE MOLECULES. Retrieved June 27, 2025, from https://www.prnewswire.com/news-releases/lomond-therapeutics-announces-us-fda-clearance-of-ind-application-for-lonitoclax-a-selective-bcl2-inhibitor-with-limited-immune-suppression-and-improved-safety-compared-to-venetoclax-and-venetoclax--like-molecules-302487020.html[2] Archeus Technologies Receives FDA Clearance of Investigational New Drug Application for ART-101 in Development for the Treatment of Prostate Cancer. Retrieved June 27, 2025, from https://www.businesswire.com/news/home/20250620911569/en/Archeus-Technologies-Receives-FDA-Clearance-of-Investigational-New-Drug-Application-for-ART-101-in-Development-for-the-Treatment-of-Prostate-Cancer[3] Terns Pharmaceuticals Presents Positive Data from Phase 1 Study of TERN-601 Once-daily Oral GLP-1R Agonist for Treatment of Obesity at 85th Annual American Diabetes Association Scientific Sessions. Retrieved June 27, 2025, from https://www.globenewswire.com/news-release/2025/06/23/3103837/0/en/Terns-Pharmaceuticals-Presents-Positive-Data-from-Phase-1-Study-of-TERN-601-Once-daily-Oral-GLP-1R-Agonist-for-Treatment-of-Obesity-at-85th-Annual-American-Diabetes-Association-Sci.html[4] Forte Biosciences Announces Positive Data in FB102 Celiac Disease Phase 1B Study. Retrieved June 27, 2025, from https://www.fortebiorx.com/investor-relations/news/news-details/2025/Forte-Biosciences-Announces-Positive-Data-in-FB102-Celiac-Disease-Phase-1B-Study/default.aspx[5] Nuvalent Announces Positive Pivotal Data from ARROS-1 Clinical Trial of Zidesamtinib for TKI Pre-treated Patients with Advanced ROS1-positive NSCLC. Retrieved June 27, 2025, from https://investors.nuvalent.com/2025-06-24-Nuvalent-Announces-Positive-Pivotal-Data-from-ARROS-1-Clinical-Trial-of-Zidesamtinib-for-TKI-Pre-treated-Patients-with-Advanced-ROS1-positive-NSCLC[6] Cellarity Initiates Phase 1 Clinical Study of CLY-124, a First-in-Class Globin-Switching Oral Medicine for the Treatment of Sickle Cell Disease. Retrieved June 24, 2025 from https://www.prnewswire.com/news-releases/cellarity-initiates-phase-1-clinical-study-of-cly-124-a-first-in-class-globin-switching-oral-medicine-for-the-treatment-of-sickle-cell-disease-302492168.html[7] Contineum Therapeutics Provides Update on Phase 1b Positron Emission Tomography (PET) Trial of PIPE-791. Retrieved June 24, 2025 from https://www.businesswire.com/news/home/20250625697950/en/Contineum-Therapeutics-Provides-Update-on-Phase-1b-Positron-Emission-Tomography-PET-Trial-of-PIPE-791[8] Sangamo Therapeutics Announces Positive Topline Results From Registrational STAAR Study in Fabry Disease. Retrieved June 24, 2025 from https://www.businesswire.com/news/home/20250624043784/en/Sangamo-Therapeutics-Announces-Positive-Topline-Results-From-Registrational-STAAR-Study-in-Fabry-Disease[9] Immutep Announces Positive Update from Phase I Study of IMP761, a First-in-Class LAG-3 Agonist Antibody for Autoimmune Diseases. Retrieved June 24, 2025 from https://www.immutep.com/detail/immutep-announces-positive-update-from-phase-i-study-of-imp761-a-first-in-class-lag-3-agonist-antibody-for-autoimmune-diseases.html#:~:text=SYDNEY%2C%20AUSTRALIA%2C%20June%2023%2C%202025%20--%20Immutep%20Limited,a%20first-in-class%20LAG-3%20agonist%20antibody%20for%20autoimmune%20diseases.[10] Aclaris Therapeutics Initiates Phase 1a/1b Program for its Novel Bispecific Antibody ATI-052. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/23/3103239/37216/en/index.html[11] Early data suggest Roche’s NXT007 may have the potential to provide haemostatic normalisation in people with haemophilia A. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/23/3103084/0/en/Early-data-suggest-Roche-s-NXT007-may-have-the-potential-to-provide-haemostatic-normalisation-in-people-with-haemophilia-A.html[12] Verdiva Bio to Present New Data Highlighting Once-Weekly Potential of Its Investigational Oral Obesity Candidates at the ADA 85th Scientific Sessions. Retrieved June 24, 2025 from https://www.businesswire.com/news/home/20250620108098/en/Verdiva-Bio-to-Present-New-Data-Highlighting-Once-Weekly-Potential-of-Its-Investigational-Oral-Obesity-Candidates-at-the-ADA-85th-Scientific-Sessions[13] Plus Therapeutics Announces FDA Clearance of its Investigational New Drug Application using REYOBIQTM for the Treatment of Childhood Brain Cancer. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/25/3104980/0/en/Plus-Therapeutics-Announces-FDA-Clearance-of-its-Investigational-New-Drug-Application-using-REYOBIQTM-for-the-Treatment-of-Childhood-Brain-Cancer.html[14] Assembly Biosciences Reports Positive Topline Results from Phase 1b Clinical Trial of Next-Generation Investigational Capsid Assembly Modulator ABI-4334 in Chronic Hepatitis B. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/25/3105003/16259/en/Assembly-Biosciences-Reports-Positive-Topline-Results-from-Phase-1b-Clinical-Trial-of-Next-Generation-Investigational-Capsid-Assembly-Modulator-ABI-4334-in-Chronic-Hepatitis-B.html[15] Biogen to Advance Investigational Spinal Muscular Atrophy Asset to Registrational Studies Based on Positive Interim Phase 1 Results. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/25/3104985/0/en/Biogen-to-Advance-Investigational-Spinal-Muscular-Atrophy-Asset-to-Registrational-Studies-Based-on-Positive-Interim-Phase-1-Results.html[16] Blue Earth Therapeutics: SNMMI Presentation of Results from Lutetium (177Lu) rhPSMA-10.1 Injection Phase 1 Clinical Trial. Retrieved June 24, 2025 from https://www.prnewswire.com/news-releases/blue-earth-therapeutics-snmmi-presentation-of-results-from-lutetium-177lu-rhpsma-10-1-injection-phase-1-clinical-trial-302490153.html[17] Metabolics Pharma Announces Positive Top-Line Results from Phase 1a Clinical Trial of ENT-03 in Obese and Diabetic Subjects. Retrieved June 24, 2025 from https://www.businesswire.com/news/home/20250625436712/en/Metabolics-Pharma-Announces-Positive-Top-Line-Results-from-Phase-1a-Clinical-Trial-of-ENT-03-in-Obese-and-Diabetic-Subjects[18] Aprea Reports Anti-Proliferative Results and Promising Early-Stage Clinical Data for Next-Generation WEE1 Inhibitor, APR-1051, in HPV+ Head and Neck Squamous Cell Carcinoma (HNSCC) in Collaboration with MD Anderson Cancer Center. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/25/3105158/0/en/Aprea-Reports-Anti-Proliferative-Results-and-Promising-Early-Stage-Clinical-Data-for-Next-Generation-WEE1-Inhibitor-APR-1051-in-HPV-Head-and-Neck-Squamous-Cell-Carcinoma-HNSCC-in-C.html[19] CRISPR Therapeutics Reports Positive Additional Phase 1 Data for CTX310™ Targeting ANGPTL3 and Provides Update on In Vivo Cardiovascular Pipeline. Retrieved June 24, 2025 from https://www.globenewswire.com/news-release/2025/06/26/3105698/0/en/CRISPR-Therapeutics-Reports-Positive-Additional-Phase-1-Data-for-CTX310-Targeting-ANGPTL3-and-Provides-Update-on-In-Vivo-Cardiovascular-Pipeline.html免责声明：本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

临床结果临床3期临床2期临床成功申请上市

2023-07-03

·药研发

【药研发0704】众生昂拉地韦甲流III期临床成功 | 药物牧场ALPK1抑制剂获批临床...

「本文共：16条资讯，阅读时长约：3分钟」今‍日‍头条众生昂拉地韦甲流III期临床成功。众生药业1类创新药昂拉地韦片（ZSP1273）在治疗甲型流感的III期临床获积极结果。在ITT患者人群中，与安慰剂相比，昂拉地韦组中位缓解时间（7项流感症状缓解时间）显著缩短（-39%，38.83hvs63.35h，P<0.001）；发热缓解时间显著缩短（-39%，P<0.001）。昂拉地韦组的中位缓解时间和发热缓解时间均短于奥司他韦组，二者病程均缩短近10%。昂拉地韦组3级及以上治疗相关不良事件（TRAE）的发生率与奥司他韦组近似。‍‍‍国‍‍‍‍‍‍‍‍‍内‍‍‍‍药‍‍讯‍‍‍‍1.华东医药FRα-ADC拟纳入优先审评。华东医药从ImmunoGen公司引进的叶酸受体α（FRα）靶向ADC新药索米妥昔单抗注射液（Elahere）的上市申请获CDE纳入拟优先审评，用于治疗FRα阳性、铂类耐药的上皮性卵巢癌、输卵管癌或原发性腹膜癌患者。在Ⅲ期临床（SORAYA）中，研究者评估的Elahere客观缓解率达到31.7%（95% CI：22.9%，41.6%）。去年11月，FDA已加速批准Elahere上市，用于单药治疗FRα高表达、对含铂疗法耐药的晚期卵巢癌经治患者。2.正大天晴多靶点TKI早期临床见刊。正大天晴在《信号转导与靶向治疗》上发表ALK/ROS1/MET酪氨酸激酶抑制剂（TKI）安奈克替尼（unecritinib，TQ-B3101）治疗ROS1融合阳性晚期非小细胞肺癌的（NSCLC）患者的Ⅰ/Ⅱ期临床最新结果。研究显示，TQ-B3101达到80.2%的ORR，中位DOR为20.3个月，中位PFS为16.5个月，6个月PFS率达到83.2%，12个月PFS率达到53.8%。药物3级及以上不良事件发生率低，无3级或更高级别的眼毒性和神经毒性。3.银诺长效GLP-1R激动剂Ⅲ期临床积极。银诺医药在ADA年会上公布长效GLP-1R激动剂苏帕鲁肽治疗2型糖尿病的两项Ⅲ期临床积极结果。单药治疗24周数据显示，苏帕鲁肽1mg和3mgQW剂量组可使患者HbA1c水平较基线分别下降1.73%和2.15%，具统计学意义。在联合用药的临床中，当苏帕鲁肽（3mg）与二甲双胍联用治疗24周时，患者HbA1c水平较基线下降了1.81%，达到主要研究终点。4.药物牧场ALPK1抑制剂获批临床。药物牧场（DrugFarm）口服高选择性ALPK1抑制剂DF-003获FDA临床许可，即将在健康志愿者中开展单次和多次递增剂量的Ⅰ期临床试验。DF-003可抑制ALPK1和导致ROSAH患者患病的ALPK1 T237M驱动突变。该产品在心脏和肾脏动物疾病模型以及ROSAH转基因小鼠模型中展现出显著的临床前活性；并具有良好的类药特性，以及符合人体每日一次给药的半衰期。5.杭州浩博乙肝ASO疗法获批临床。浩博医药反义寡核苷酸（ASO）疗法1类化药AHB-137获国家药监局临床许可，拟开发用于慢性乙型肝炎的治疗。AHB-137可靶向所有HBV RNA将其降解，在临床前研究中已显示出对乙肝表面抗原的降低能力。今年3月，该新药在新西兰健康志愿者中开展的Ⅰ期临床完成第一队列受试者给药，该项试验旨在评估AHB-137的安全性、耐受性、药代动力学以及在慢性乙肝患者中的初始疗效。6.艺妙神州CAR-T疗法获批实体瘤临床。北京艺妙神州自研的新一代抗肿瘤药物IM83嵌合抗原受体T细胞注射液（IM83 CAR-T细胞注射液），获国家药监局临床试验默示许可，拟开发用于治疗GPC3阳性肿瘤。IM83采用了全新的CAR分子设计，提高了CAR-T细胞在体内抑瘤的持续性。在研究者发起的临床研究中，该产品展现出积极的疗效和良好的安全性，被证实能够有效杀伤靶点阳性的肝癌细胞。‍‍‍‍国‍‍‍‍‍‍‍‍‍‍际‍‍‍‍药‍讯‍‍1.Allecra公司新型抗生素组合报NDA。Allecra公司抗生素组合enmetazobactam/头孢吡肟向FDA提交新药申请，用于治疗复杂性尿路感染（cUTIs）。在III期临床ALLIUM中，与哌拉西林/他唑巴坦相比，头孢吡肟/enmetazobacta符合非劣效性和优效性标准，两组总成功率为79.1%和58.9%（调整后的分层差异为21.2%[95%分层Newcombe CI：14.3%，27.9%]）。此前，欧洲EMA已受理这一组合的上市许可申请，用于医院获得性/呼吸机相关细菌性肺炎。2.全球首款非激素更年期新药Ⅲ期临床积极。安斯泰来神经激肽3（NK3）受体拮抗剂Veozah（fezolinetant）治疗由更年期引起的中重度血管舒缩症状（VMS，即潮热）的Ⅲb期临床（DAYLIGHT）达到主要终点。与安慰剂相比，Veozah（45mg）治疗24周时患者的中重度VMS的发生频率在统计学上显著降低。最常见的治疗伴发不良反应（TEAE）是COVID-19感染和头痛。今年5月，FDA已批准Veozah上市，成为全球首款非激素更年期新药。3.双重ET拮抗剂降血压III期临床积极。Idorsia公司靶向双重内皮素（ET）受体的口服拮抗剂aprocitentan治疗顽固性高血压的Ⅲ期临床（PRECISION）最新结果积极。aprocitentan（12.5mg、25mg）和安慰剂组患者中non-dippers（夜间血压降幅未达10%）的比例分别为66%、62%和60%。在接受治疗4周后，三组中分别有44%、40%和31%的non-dippers的夜间血压下降模式达到正常化。此外，12.5 mg（-11.25vs-2.79 mmHg；p<0.01）和25 mg（-13.12vs-6.29 mmHg；p<0.01）剂量的aprocitentan均可诱导患者夜间收缩压的显著降低。4.创新HER2/3双抗获突破性疗法认定。Merus公司创新HER2/HER3双抗zenocutuzumab获FDA突破性疗法认定，用于治疗晚期不可切除或转移性NRG1融合阳性胰腺癌经治患者。在Ⅰ/Ⅱ期临床eNRGy中，zenocutuzumab在这类NRG1融合阳性癌症患者中达到34%的客观缓解率（ORR），中位缓解持续时间为9.1个月。在非小细胞肺癌、胰腺癌、乳腺癌、胆管癌患者中均观察到缓解病例。5.Enterin公司启动PTP1B抑制剂减肥临床。Enterin公司皮下注射PTP1B抑制剂ENT-03在ClinicalTrials官网登记启动一项I期临床，评估ENT-03在伴有或不伴有2型糖尿病的肥胖患者中的安全性、耐受性、药动学和药效学。ENT-03旨在通过作用于调节能量和代谢的大脑回路调节葡萄糖水平并使体重减轻。在肥胖的糖尿病小鼠中，ENT-03快速降低血糖，减少食物摄入和肥胖，消除肝脏脂肪，并改善肝功能。6.礼来收购ADC公司Emergence。礼来将收购ADC开发商Emergence Therapeutics，并获得该公司靶向Nectin-4的ADC药物先导候选产品ETx-22及其他ADC项目。2021年12月，Emergence宣布完成8700万欧元A轮融资以用于推进ETx-22的临床概念验证。ETx-22是新一代Nectin-4 ADC，经过优化提高疗效的同时，最大限度降低了毒性（尤其是皮肤毒性）。目前，全球范围内同类产品只有维恩妥尤单抗（Padcev）获批上市。‍‍‍‍‍‍‍‍‍医‍‍‍‍‍‍药‍‍‍‍‍‍‍‍‍‍‍‍‍热‍‍‍‍‍‍‍点‍‍‍‍‍‍‍‍‍1.北京安贞医院安徽医院开工。6月26日上午，国家心血管病区域医疗中心（北京安贞医院安徽医院）在合肥市开工建设。该项目是由安徽省人民政府和首都医科大学附属北京安贞医院合作共建，2022年10月获国家发改委、国家卫生健康委等三部委批复，依托安徽医科大学第一附属医院建设，总建筑面积19.6万平方米，总投资15亿元，拟新建床位1000张。 2.江苏太仓卫健委资助本地高考生学医。近期，江苏省太仓市卫健委在其官方微信公众号发文，出台最新「政府资助生」政策，鼓励考生报考医学专业。公告显示，太仓籍优秀高中毕业生，报考江苏省或全国重点高校医学类专业并在本科批次以上录取，专业为临床医学（包括精神卫生）、麻醉学、医学影像学、口腔医学或中医学，本科一次性资助5万元；硕士8万元或首套房10万元安家费；博士给予15万元安家费。3.北京养老服务网上线。6月28日，北京养老服务网及配套的小程序上线运行。该网站涵盖了居家养老、机构养老、养老助餐、养老政策、养老人才、养老志愿服务等多个服务板块，可以提供“一站式”服务。对于实在不熟悉网络操作的老年人，还可以直接拨打网站首页右上角的客服电话400-670-5115，通过电话语音向客服表达诉求。小程序不仅可以查询家附近的养老机构，还支持老人/家属在线一站式选餐。‍‍‍‍‍‍‍评‍‍‍‍‍审‍‍‍‍动‍‍态‍‍‍‍‍‍‍ 1. CDE新药受理情况（07月03日) 2. FDA新药获批情况（北美06月30日）股市资讯上个交易日 A 股医药板块 -0.76%涨幅前三跌幅前三仟源医药+14.77% 太极集团-10.00%百利天恒+10.79% 安必平 -8.00%艾力斯 +5.75% 贵州三力 -6.74%【恒瑞医药 (47.36,-0.54.-1.13%)】截至2023年6月30日，公司通过集中竞价交易累计回购股份364.82万股(总股本0.06%)，已支付总金额1.68亿元。【德源药业(24.22.0.64.2.71%)】与中国科学院上海药物研究所签订《技术开发合同》，拟针对两个不同靶点的代谢性疾病领域的创新药进行前期探索性技术合作开发。【白云山 (23.700,0.050,0.21%) (31.64,-0.24.-0.75%)】分公司白云山化学制药厂收到国家药品监督管理局核准签发的头孢地尼化学原料药《上市申请批准通知书》。- The End -戳“阅读原文”，了解更多医药研发及股市资讯。

临床3期优先审批临床结果抗体药物偶联物临床2期

2023-06-24

·GlobeNewswire-Health Care

Enterin Presents Data Demonstrating Strong Benefit of ENT-03 on Body Weight, Adiposity and Blood Glucose Vs. Semaglutide in a Diet Induced Obesity Mouse Model

Data presented at the American Diabetes Association 83rd Scientific SessionsPHILADELPHIA, June 24, 2023 (GLOBE NEWSWIRE) -- Enterin Inc., a privately held, Philadelphia-based, clinical-stage biopharmaceutical company pioneering novel treatments for neurodegenerative and metabolic diseases, presented in vivo data demonstrating benefit on body weight, adiposity and blood glucose of ENT-03 compared to semaglutide in an obese, diabetic animal model, with persistence of benefit on weight beyond treatment. The data were presented at the American Diabetes Association’s (ADA) 83rd Scientific Sessions in San Diego. “ENT-03 differs profoundly from the GLP-1 agonists both with respect to its pharmacology and mechanism of action,” said Michael Zasloff, M.D., Ph.D., Scientific Director of the Medstar Georgetown Transplant Institute, Co-Founder and Chief Scientific Officer of Enterin and senior author of the paper. “We believe ENT-03 can add a new dimension to the management of Type 2 diabetes and obesity.” ENT-03 is a novel, endogenous, centrally acting mammalian aminosterol with Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activity, which normalizes glucose and causes weight loss by acting on brain circuits that regulate energy and metabolism. In obese, diabetic mice, ENT-03 rapidly lowers blood glucose, reduces food intake and adiposity, eliminates liver fat, and improves liver function. The study presented today compared the effects of subcutaneously administered ENT-03 to semaglutide on blood glucose, adiposity, and body weight over a 10-week treatment period in a diet-induced obesity (DIO) mouse model. Within one-to-two weeks of treatment with ENT-03, DIO mice exhibit a rapid and substantial fall in blood glucose, out of proportion to the loss of weight. In contrast, in semaglutide treated DIO mice, glucose falls in proportion to weight loss. Weight loss continues smoothly in the ENT-03 treatment group over the 10-week period, plateauing at lean body weight, and blood glucose remains in the normoglycemic range. In contrast, the effects of semaglutide on both weight loss and blood glucose begin to diminish between four and six weeks after initiation of treatment, since both body weight and blood glucose increase despite continued dosing. Within several days following the end of the 10-week treatment period, the semaglutide group exhibited a sharp rebound in food intake and body weight and by five weeks approached the body weight of the untreated obese mice. In contrast, ENT-03 treated animals maintained the lower weight and the reduced food intake, with no evidence of rebound in either. Body fat, which decreased significantly in both groups during treatment, increased at a faster rate in the semaglutide group post-treatment compared with the ENT-03 group. Results can be found online at www.enterininc.com and at https://diabetesjournals.org/diabetes/article/72/Supplement_1/854-P/149928/854-P-ENT-03-a-Centrally-Acting-Endogenous. “Weight loss during treatment with ENT-03 is progressive, profound and outlasts the treatment period for prolonged periods, which suggests that a neuroregenerative process might be taking place,” said Denise Barbut, M.D., F.R.C.P., Co-Founder, President, and Chief Medical Officer of Enterin and first author of the paper. Phase 1 studies in obese and diabetic subjects are currently in progress (IND155001). Results of the first-in-human, randomized, double-blind, single ascending dose study involving approximately 49 subjects with obesity with or without Type 2 diabetes are expected to be available in the fourth quarter of 2023. ENT-03 is Enterin’s second compound in clinical trials. The first compound, ENT-01, has completed a successful randomized Phase 2b study in patients with Parkinson’s disease (https://www.acpjournals.org/doi/10.7326/M22-1438). About Enterin Inc. Enterin Inc. is the first company to develop novel compounds that repair the dysfunctional gut-brain axis in patients with neurodegenerative diseases. Enterin Inc. is pioneering the medical community’s understanding of the link between infections, dysfunction of the enteric nervous system (ENS) and the onset and progression of neurodegenerative disease. Enterin’s lead compound, ENT-01, displaces membrane-bound alpha-synuclein (αS) aggregates from nerve cells in the ENS and improves neural signalling between the gut and the brain. Enterin Inc. has completed a large, randomized Phase 2b clinical trial in patients with Parkinson’s disease. The study met all the endpoints. Preparations for Phase 3 studies are currently underway. The second compound, ENT-03, increases insulin sensitivity by acting at the level of the brain. It is being developed for the treatment of diabetes, obesity, and Alzheimer’s disease. For more information, please visit www.enterininc.com. Company contact:Katherine WolfChief Financial Officerk.wolf@enterininc.com

临床2期临床结果

100 项与 ENT-03 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
2型糖尿病	临床1期	美国	Enterin, Inc.	2023-06-05
肥胖	临床1期	美国	Enterin, Inc.	2023-06-05
阿尔茨海默症	临床前	美国	Enterin, Inc.	-

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05925920 (CTgov)	临床1期	2型糖尿病 \| 肥胖	49	ENT-03S (Cohort 1 (no T2D): ENT-03S 3 mg)	選獵淵遞鏇壓壓淵襯餘 = 廠憲壓願廠鹹簾壓淵淵糧繭蓋衊艱鏇鏇衊製憲 (繭獵選積淵鏇網鬱鹹鏇, 艱糧鏇網蓋窪憲淵糧鬱 ~ 選壓蓋繭願衊選製顧網) 更多	-	2026-06-01
NCT05925920 (CTgov)	临床1期	2型糖尿病 \| 肥胖	49	ENT-03S (Cohort 2 (no T2D): ENT-03S 6 mg)	選獵淵遞鏇壓壓淵襯餘 = 糧淵鬱鬱築餘製鹽鏇糧糧繭蓋衊艱鏇鏇衊製憲 (繭獵選積淵鏇網鬱鹹鏇, 繭衊鹽遞繭膚築衊遞襯 ~ 願夢鹽顧廠憲蓋遞膚衊) 更多	-	2026-06-01
ADA2025	临床1期	2型糖尿病 \| 代谢良性肥胖	49	ENT-03	鬱鹹鹽遞憲鏇膚醖醖觸(鹹願鑰鏇憲壓糧構蓋鏇) = All TEAEs were reported as mild (grade 1) or moderate (Grade 2), indicating a favorable AE profile. Mild nausea was observed in 4 patients, and 2 patients had moderate vomiting (3 mg dose and 50 mg dose). Four mild injection site reactions were observed and did not require intervention. 壓壓艱簾觸簾鬱積獵淵 (鏇選蓋願鑰夢壓顧製齋 )	积极	2025-06-20