P2 Efficacy Evaluation of Sabizabulin Monotherapy Versus Active Control for Treatment of ER+HER2- MBC in Patients Who Have Shown Previous Disease Progression on a Nonsteroidal Aromatase Inhibitor, Fulvestrant and CDK 4/6 Inhibitor

To demonstrate the efficacy of sabizabulin in the treatment of ER+HER2- metastatic breast cancer (MBC) as measured by progression free survival (PFS) by RECIST v1.1.

开始日期2023-03-15

申办/合作机构

Veru, Inc.

NCT05008510

/ Withdrawn临床2期

Phase 2 Clinical Efficacy and Safety Study of Sabizabulin (VERU-111) Monotherapy and Sacituzumab Govitecan-hziy/Sabizabulin Combination Therapy for the Treatment of Metastatic Triple Negative Breast Cancer

To compare the following:
1. The efficacy of sabizabulin monotherapy to sacituzumab govitecan-hziy monotherapy
2. The efficacy of sacituzumab govitecan-hziy/sabizabulin combination therapy to sacituzumab govitecan-hziy monotherapy
These comparisons will be made in the efficacy in the treatment of metastatic triple negative breast cancer (mTNBC) in patients previously treated with at least two systemic chemotherapies for metastatic disease as measured by radiographic progression free survival (rPFS) as the primary endpoint.

开始日期2021-12-30

申办/合作机构

Veru, Inc.

NCT04844749

/ Terminated临床3期

VERACITY - Randomized, Active-Controlled, Phase 3 Study of VERU-111 for the Treatment of Metastatic Castration-Resistant Prostate Cancer in Patients Who Have Failed Prior Treatment With at Least One Androgen Receptor Targeting Agent

To demonstrate the efficacy of VERU-111 (Sabizabulin) in the treatment of metastatic castration-resistant prostate cancer in patients who have failed prior treatment with at least one androgen receptor targeting agent as measured by radiographic progression-free survival.

开始日期2021-06-24

申办/合作机构

Veru, Inc.

100 项与沙比沙布林相关的临床结果

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100 项与沙比沙布林相关的转化医学

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100 项与沙比沙布林相关的专利（医药）

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项与沙比沙布林相关的文献（医药）

2025-11-01·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of novel 4-aryl-2-benzoyl-imidazoles as colchicine binding site inhibitors

Article

作者: Miller, Darcie J ; Xie, Yang ; Miller, Duane D ; Albadari, Najah ; Wang, Qinghui ; Chen, Hao ; Li, Wei ; Wu, Zhongzhi ; Ma, Dejian ; Oldham, Michael L ; Gruntz, Judith Quadrozzi

Highly potent tubulin inhibitors serve as critical payloads in several FDA-approved antibody-drug conjugates (ADCs). However, all these compounds are natural products with complex structures, which limit the ability to adjust their physicochemical properties for the optimal balance between payload release and ADC stability during systemic circulation, as well as efficient tumor penetration. Although taxanes are widely used in cancer therapy, they are unsuitable for ADCs due to insufficient potency and a high tendency to develop acquired drug resistance. Colchicine binding site inhibitors (CBSIs) are attractive alternatives, offering tunable properties and the potential to overcome multidrug resistance associated with the use of many existing tubulin inhibitors. However, most CBSIs lack sufficient potency for viable ADC applications. In our pursuit of a highly potent CBSI suitable for ADC use, we identified a novel series of sabizabulin derivatives. These compounds were evaluated in vitro across four cancer cell lines, including one with high resistance to taxanes. Among them, compound 11b emerged as the most promising one with IC₅₀ values ranging from 0.6 nM to 1.3 nM in cancer cells, entering the potency range as a potential ADC payload. Importantly, 11b also effectively overcame taxane-associated drug resistance. Mechanistic studies confirmed that 11b directly binds to the colchicine site on tubulin, as demonstrated by its high-resolution crystal structure in a complex with tubulin protein. In vivo efficacy studies using a taxane-resistant prostate cancer xenograft model (PC-3/TxR) revealed that 11b significantly suppressed tumor growth, disrupted angiogenesis, and induced apoptosis. Together, these findings highlight 11b as a highly potent CBSI with the capability of overcoming acquired drug resistance to taxanes, suggesting its strong potential as a next-generation ADC payload.

2024-12-01·RUSSIAN CHEMICAL BULLETIN

The effect of microtubule destabilizing compounds on the infection of Vero cells with the SARS-CoV-2 coronavirus

作者: Esaulkova, Ya. L. ; Adaeva, O. I. ; Demchuk, D. V. ; Semenov, V. V. ; Semenova, M. N. ; Belyaevskaya, S. V. ; Kuptsova, T. S. ; Zarubaev, V. V.

Microtubules, cytoskeleton components, are essential for viruses for their transportation to the replication site as well as for the subsequent release from the cell, so affecting the structure and function of microtubules could be considered as a promising approach to suppress viral infection.In this regard, 50 chem. compounds of various structures with microtubule destabilizing mechanism of action were tested on Vero cells infected with the SARS-CoV-2 coronavirus (Wuhan line).Combretastatin analogs, polyalkoxy-substituted 4,5- and 3,4-diarylpyridazines (24 compounds), were synthesized in 73-99% yields by the Diels-Alder reaction of tetrazines with aryl- and diarylacetylenes.The previously described antitubulin agents were also studied, including various derivatives of combretastatin, podophyllotoxin, and indibulin, as well as isoflavonoid glaziovianin, etc.Nine compounds with a selectivity index >10 were found within the analogs of combretastatins A-2 and A-4, namely, 5 diarylpyridazines, diarylpyrazole, two diarylisoxazoles, and chalcone.In general, the ability of the compounds to suppress viral infection did not depend on the value of their antimitotic antitubulin activity.However, the most effective inhibitor of viral infection, bromo-substituted diarylpyrazole 9 with a selectivity index of 241, exhibited a pronounced antimitotic effect as well, causing sea urchin embryo cleavage alteration at a concentration of 5 nmol L-1.

2024-11-01·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel thiophene[3,2-d]pyrimidine-based tubulin inhibitors with enhanced antitumor efficacy for combined use with anti-pd-l1 immunotherapy in melanoma

Article

作者: Peng, Xiaopeng ; Zhao, Huiting ; Liu, Jin ; Wang, Yuxi ; Li, Ling ; Wu, Chengyong ; Chen, Jianjun ; Xu, Chenglong

Herein, we designed and synthesized a series of novel 2-methylthieno [3,2-d]pyrimidine analogues as tubulin inhibitors with antiproliferative activities at low nanomolar levels. Among them, compound DPP-21 displayed the most potent anti-proliferative activity against six cancer cell lines with an average IC₅₀ of ∼6.23 nM, better than that of colchicine (IC₅₀ = 9.26 nM). DPP-21 exerted its anti-cancer activity by suppressing the polymerization of tubulin with an IC₅₀ of 2.4 μM. Furthermore, the crystal structure of DPP-21 in complex with tubulin was solved by X-ray crystallography to 2.94 Å resolution, confirming the direct binding of DPP-21 to the colchicine site. Moreover, DPP-21 arrested the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis. Additionally, DPP-21 was able to effectively inhibit the migration of cancer cells. Besides, DPP-21 exhibited significant in vivo anti-tumor efficacy in a B16-F10 melanoma tumor model with a TGI of 63.3 % (7 mg/kg) by intraperitoneal (i.p.) injection. Notably, the combination of DPP-21 with NP-19 (a PD-L1-targeting small molecule inhibitor reported by our group before) demonstrated enhanced anti-cancer efficacy in vivo. These results suggest that DPP-21 is a promising lead compound deserving further investigation as a potential anti-cancer agent.

147

项与沙比沙布林相关的新闻（医药）

2025-11-04

·百度百家

新冠药物研发：从基础到临床的成功跨越

《中国科学基金》2022年第36卷第4期封面专题，探讨了疫苗、抗体及小分子药物的研发进展，特别是针对新冠肺炎的口服小分子药物。这一领域的研究动态，对于疫情防控和药物创新具有重要意义。 △ 药物研发的重要性 2019年底至今，新型冠状病毒肺炎（简称“新冠肺炎”）在我国及全球范围内大流行，严重威胁着人类健康。有效的治疗药物成为战胜新冠疫情的关键，而口服小分子药物更是当前抗新冠病毒药物研发的热点。 △ 常俊标教授的贡献常俊标，博士，现任郑州大学/河南师范大学教授及博士生导师，同时荣获全国杰出专业技术人才与国家杰出青年科学基金。他不仅主持了多项国家级科研课题，包括国家重点研发计划、重大新药创制专项以及国家自然科学基金重点项目，还在创新药物研发领域取得了显著成就。其研究成果多次发表在Science、Nature等顶尖杂志上，并成功获得国内外授权发明专利50余件，其中5件已实施。此外，他还荣获了国家科技进步奖二等奖和国家自然科学奖二等奖等多项殊荣。更为值得一提的是，他成功研发出1个1.1类创新药（适用于艾滋病和新冠肺炎的治疗），并已有2个创新药正在进行临床试验。 △ 2.1. 药物研发现状自疫情发生以来，本研究团队便积极投入到抗新冠肺炎药物的筛选与研发工作中。经过近三十年的创新药物研究积累，我们成功研发出抗新型冠状病毒口服小分子药物阿兹夫定，为疫情防控贡献了一份力量。本文将详细介绍阿兹夫定的研发历程，并梳理国内外口服小分子抗新冠药物的研发现状。 △ 2.2. 阿兹夫定的研发与作用小分子药物在抗病毒方面主要通过阻断病毒在细胞内的复制来实现其作用。这类药物的作用靶点通常具有保守性、高稳定性，同时生产成本低廉，易于生产、存储和运输。更重要的是，它们可以通过口服给药，极大地提高了给药的便捷性，为医患双方带来了极大的便利。目前，国内外针对新冠肺炎的口服小分子药物研发工作主要集中在新冠病毒的主蛋白酶3CLpro和RNA依赖的RNA聚合酶RdRp上。 2022年7月25日，国家药品监督管理局依据相关法规，启动应急审批通道，附条件批准了阿兹夫定片增加治疗新冠病毒肺炎的适应症。这意味着阿兹夫定，作为我国首个自主研发并拥有全球专利的口服小分子新冠肺炎治疗药物，正式获得认可。此前，美国食品药品监督管理局也已批准帕罗维德和莫那匹韦用于新冠肺炎轻中症的治疗。 △ 2.3. 其他治疗药物综述与展望 2.3.1 △ 帕罗维德辉瑞制药研发的帕罗维德，是一种包含奈玛特韦与利托那韦的组合药物。其中，奈玛特韦主要针对病毒主蛋白酶3CLpro发挥作用，而利托那韦则负责减缓奈玛特韦在体内的代谢速度。临床数据显示，帕罗维德能有效降低新冠肺炎非住院患者的住院或死亡率。 2.3.2 △ 莫那匹韦默克制药研发的莫那匹韦，最初是针对委内瑞拉马脑炎病毒的药物。后来，科学家们发现它对诱发重症急性呼吸综合征（SARS）、中东呼吸综合征（MERS）等的冠状病毒同样有效。在新冠肺炎爆发后，该药物更是被转化为抗新冠病毒药。 2.3.3 △ 巴瑞替尼巴瑞替尼，一种酪氨酸蛋白激酶JAK 1/2抑制剂，由美国Incyte公司发现并授权给美国礼来公司。最初，该药物主要用于中重度活动性类风湿关节炎成年患者的治疗。 △ 3.1. 3CLpro抑制剂研究在针对新冠病毒3CLpro的抑制剂药物研发领域，日本盐野义的S-217622已取得了显著的进展。 △ 3.2. RdRp抑制剂研究在新冠病毒RdRp抑制剂药物的研发竞赛中，君实生物的VV116脱颖而出。 △ 3.3. 其他靶点药物研发除了RdRp抑制剂外，其他靶点的药物也在不断涌现。其中，美国Veru公司开发的Sabizabulin备受瞩目，它是一款口服微管蛋白抑制剂。 △ 3.4. 总体展望与建议自新冠肺炎疫情爆发以来，我国科学家在新冠病毒研究方面取得了显著进展，不仅解析了病毒结构，还发现了新的药物靶点，为抗病毒药物的设计和研发提供了有力支持。展望未来，为了更好地应对新发突发病毒性疾病的挑战，我们需要加快药物研发速度。尽管我国在原创抗病毒药物研发方面起步较晚，但可以充分利用自由探索和“举国体制”并重的优势，加强前瞻性布局，重视病毒性疾病治疗药物的研发。通过学科交叉，多维度、全方位探寻病毒和宿主互作的调控网络，解析病毒共性发病机制，寻找新的药物治疗靶点。同时，我们还需要阐明关键药物靶点的工作机制，积累抗病毒药物研发经验，并提前对潜在的广谱抗病毒药物进行筛选和临床前研究，为未来新发突发病毒传染性疾病提供储备药物，从而更好地保障人民的生命安全和身体健康。

疫苗核酸药物

2025-11-03

·凯美科

感染性疾病领域天然产物衍生药物的临床研发进展

前文内容，请点击以下链接: 天然产物衍生药物的临床开发与审批现状综述(2014-2025) 3. 感染性疾病领域天然产物衍生药物临床评估进展天然产物（NPs）在新一代抗感染药物的研发中始终发挥着关键作用。然而，尽管临床需求紧迫且耐药性威胁日益加剧，大型制药公司却已缩减甚至放弃了抗感染药物的开发投入。抗菌药物研发进展明显放缓，尤其针对革兰氏阴性菌（G-ve）的药物研发陷入停滞90–92，其中商业回报不足是导致这一领域萎缩的重要原因93–95。目前，抗菌药物的创新重任主要落在：中小型生物技术公司（部分公司如Achaogen、Tetraphase虽成功获批新抗生素却因收入不足而倒闭）公私合作项目及非营利性倡议与此同时，间接作用型抗菌药和生物制剂等非传统手段逐渐成为新的研发方向90,96–99，例如：直接或间接作用的噬菌体、蛋白质、微生物及单克隆抗体（mAbs）；通过毒力抑制、耐药性缓解、肠道菌群重建或增强宿主免疫力以清除感染的间接作用制剂。相比之下：抗真菌药物创新仍十分有限，近几十年来仅有少数新类别进入临床或获批49,100；抗病毒药物研发因应对SARS-CoV-2等新发病毒威胁而较为活跃，但多数成果仍局限于特定病毒，广谱抗病毒药物的需求持续存在101；抗寄生虫药物研发管线也相对薄弱，突破性疗法寥寥无几102,103。本文在第3.1节（表4）中详述处于临床试验阶段的NP与NP-D类抗菌药物，并在第3.2节（表5）中讨论抗寄生虫、抗病毒及抗真菌候选药物。表4 截至2024年12月31日处于临床试验阶段的NP和NP-D抗菌化合物（按年份排序）注释说明： a 如果抗生素类别与先导化合物不同时标注 b 同时作为抗真菌药物进行临床试验（详见第3.3节） c 结构未公开缩写词解释： ABSSSI：急性细菌性皮肤及皮肤结构感染 CABP：社区获得性细菌性肺炎 cUTI：复杂性尿路感染 PJI：假体周围关节感染 TB：结核病表5 截至2024年12月31日处于临床试验阶段的NP和NP-D抗寄生虫、抗病毒和抗真菌化合物（按年份排序）注释说明： a Q-格里菲辛为天然产物（NP），通过直接分离（I）工艺生产 b 反式藏红花素同时开展肿瘤学相关临床试验 c HRS9432由福建圣迪制药开发，江苏恒瑞医药参与 d PL-18同时具有抗菌活性研究缩写说明： NP：天然产物；NP-D：天然产物衍生物；SS：半合成；TS：全合成；I：直接分离 ARDS：急性呼吸窘迫综合征；COVID-19：2019冠状病毒病 3.1 抗菌药物那氟霉素（Nafithromycin, 3.01，WCK 4873）酮内酯类抗生素 III期临床试验完成药物类别：酮内酯类抗生素，具有广谱抗菌活性104–106。研发单位：印度Wockhardt Limited。研发进展：在印度完成一项针对社区获得性细菌性肺炎（CABP）的III期临床试验（CTRI/2019/11/021964）107。2025年1月2日（略超出本综述截止日期），Wockhardt宣布那氟霉素在印度获批用于CABP治疗108。抗菌肽药物开发（江苏普莱医药生物技术有限公司）培西加南（Peceleganan, 3.02，PL-5, V681）抗菌肽 III期临床试验完成结构特征：26聚体α螺旋抗菌肽，为天蚕素A与蜂毒肽B的杂交肽109,110。研发进展：完成一项针对皮肤伤口感染的III期临床试验（ChiCTR2100047202）111。正在开展另一项III期试验（ChiCTR2300071255）评估其伤口感染疗效。已向中国国家药品监督管理局（NMPA）提交伤口感染的上市申请。同时开展II期临床试验（NCT06189638）评估其对糖尿病足感染的治疗效果112。 PL-18（3.03）抗菌肽 Ib/II期临床试验结构特征：15聚体α螺旋抗菌肽，源自幽门螺杆菌核糖体蛋白L1（RpL1）的N端序列109,110,113。研发进展：完成一项针对细菌性阴道病（栓剂给药）的I期临床试验（NCT05340790）。目前正在进行一项Ib/II期临床试验（CTR20232467），评估其对单纯性外阴阴道念珠菌病的疗效。扎洛加南（Zaloganan, 3.04，PLG0206，WLBU2）抗菌肽 I期临床试验完成药物类别：24聚体抗菌肽（AMP），灵感来源于具有广谱抗菌活性的人源抗菌肽LL37114–117。抗菌谱：对革兰阳性菌（G+ve）、革兰阴性菌（G-ve）及生物膜均有抑制作用。研发进展：完成一项针对假体周围关节感染（PJI）的I期临床试验（NCT05137314），采用术中局部冲洗给药118。完成一项静脉给药的I期试验（ACTRN12618001920280）。CARB-X近期宣布支持开发3.04的缓释制剂，用于治疗骨折相关感染119。 HRS-8427（结构未公开）头孢菌素衍生物 III期临床试验药物类别：头孢地尔（cefiderocol, 2.23）衍生物120–122。研发单位：江苏恒瑞医药。研发进展：正在进行一项针对复杂性尿路感染（cUTI）的III期临床试验（NCT06569056）。头孢地尔（2.23，第2.1节）为一种通过整合铁载体增强细胞摄取的头孢菌素类抗生素，2019年首次获批用于cUTI治疗123,124。贝那培南（Benapenem, 3.05）碳青霉烯类 II/III期临床试验完成药物类别：静脉用碳青霉烯类抗生素，结构与厄他培南相关。研发进展：2020年5月在中国完成一项针对cUTI的II/III期临床试验（NCT04505683）125,126。上海医药集团于2021年获得授权，其2023年年报中将3.05列为在研项目127。桑费曲南酯（Sanfetrinem cilexetil, 3.06，GV-104326）三环碳青霉烯类 II期临床试验药物类别：合成三环碳青霉烯类（三环类）抗生素的前体药物128,129。研发历史：1990年代已完成针对呼吸道感染的II期临床试验，后因商业考量暂停开发130。2022年5月启动一项早期杀菌活性（EBA）II期试验（NCT05388448）131。拓展方向：目前已有其他研究关注β-内酰胺类药物在结核病治疗中的重新定位132,133。利福斯替尼唑（Rifasutenizol, 3.07，TNP-2198）杂合分子 III期临床试验完成药物类别：利福霉素-甲硝唑杂合分子134。研发单位：天恩医药（TenNor）。给药特性：口服给药，无全身性吸收。研发进展：近期完成一项III期临床试验（NCT05857163），联合雷贝拉唑和阿莫西林用于治疗幽门螺杆菌感染患者135。利法喹嗪酮（Rifaquizinone, 3.08，TNP-2092，CBR 2092）杂合分子 II期临床试验完成药物类别：利福霉素-喹啉嗪杂合分子（先导化合物ABT-719，具氟喹诺酮类特性）136–138。研发单位：天恩医药（TenNor Therapeutics）。适应症与进展：静脉给药：已完成针对革兰阳性菌急性细菌性皮肤和皮肤结构感染（ABSSSI）的II期试验（NCT03964493）。已完成针对假体周围关节感染（PJI）的II期试验（NCT04294862）。计划开展上述两适应症的III期临床试验139。口服给药：正在评估用于肝硬化肝性脑病（I/II期，NCT06135675）及腹泻型肠易激综合征（I期）的治疗。作用机制：通过杂合结构双靶点作用——RNA聚合酶（利福霉素组分）及DNA旋转酶/拓扑异构酶IV（喹啉嗪酮组分）137。乌普加南（Upleganan, 3.09，EVER206，SPR206）多粘菌素类似物 I期临床试验完成药物类别：多粘菌素类似物。研发合作：美国Spero Therapeutics 大中华区、韩国及部分东南亚地区：Everest Medicines 其他地区：辉瑞欧洲（Pfizer Europe）适应症：多重耐药革兰阴性菌感染。研发进展：已完成四项I期临床试验（NCT03792308、NCT04868292、NCT04865393、ChiCTR2200056692）140–142。计划开展II期临床试验。 MRX-8（结构未公开）多粘菌素类似物 I期临床试验完成药物类别：多粘菌素类似物，为通过极性酯键连接脂肪酸尾链形成的"软性"前体药物，水解后生成活性代谢物MRX-8039（3.14）143–145。研发单位：MicuRx。研发进展：已完成两项I期临床试验（NCT04649541、CRT20221866）147。专利US9971394中化合物34（3.15）为代表性实例146。 BRII-693（3.10，QPX-9003，F365）合成多粘菌素衍生物 I期临床试验完成药物类别：合成多粘菌素衍生物，由莫纳什大学研究人员发现148。适应症：铜绿假单胞菌和鲍曼不动杆菌感染。研发进展：Qpex制药（现为盐野义子公司）于2022年7月完成I期试验（NCT04808414）。全球开发权已授权给Brii Biosciences公司149。 ASK0912（3.11，多粘菌素S2，IMB-0912）天然多粘菌素 I期临床试验进行中药物类别：天然多粘菌素类抗生素。安全性优势：与多粘菌素B和E相比，肾细胞毒性和急性毒性较低150。临床前研究：在鲍曼不动杆菌小鼠模型中显示出良好的体内活性151。研发单位：江苏奥赛康药业。研发进展：已完成一项I期试验（CTR20222379）122,152。另一项I期试验（CTR20243311）正在进行中。齐法环素（Zifanocycline, 3.12，KBP-7072）四环素衍生物 I期临床试验完成药物类别：氨甲基环素类四环素衍生物，为蛋白质合成抑制剂，具有广谱抗菌活性153–155。研发单位：KBP BioSciences。研发进展：已完成四项I期临床试验（最近一项为NCT05507463）。 EBC-1013（3.13）非传统抗菌药 I期临床试验药物来源：为替吉拉诺替酯（tigilanol tiglate, 3.14，第7.1节）的半合成衍生物156–158。研发单位：QBiotics。适应症与进展：正在开展I期临床试验（ACTRN12624000544572），评估其促进下肢静脉溃疡伤口愈合的潜力156。为目前唯一进入临床试验阶段的非传统NP-D类抗菌药物。同步开发用于犬、马等动物的急慢性伤口管理。作用机制：作用于细菌细胞壁，导致革兰阳性菌与革兰阴性菌细胞壁通透性增加通过靶向胞外聚合物基质破坏已形成的生物膜激活免疫细胞产生活性氧（ROS）156 临床前研究：在糖尿病慢性伤口小鼠模型中，3.13可提高宿主防御肽表达、调节细胞因子水平、激活免疫细胞并加速伤口愈合156。 RG6436（GGDC-0829，结构未公开）芳基霉素衍生物 I期临床试验药物类别：芳基霉素（arylomycin）衍生物159–161。研发单位：基因泰克（罗氏）。作用靶点：芳基霉素（如arylomycin A-C16, 3.15）为链霉菌来源的SPase抑制剂162,163。SPase（信号肽酶）通过水解分泌蛋白N端信号肽，对细菌生存和毒力至关重要164–166。RG6436特异性抑制大肠杆菌I型信号肽酶LepB167。研发进展：正在开展I期临床试验（ISRCTN18049481），开发为静脉制剂用于复杂性尿路感染（cUTI）治疗。相关候选药物：另一芳基霉素LepB抑制剂RG-6319（结构未公开）已完成两项I期试验（ISRCTN15259645、ISRCTN16073754），但后续开发已中止，资源集中于RG6436168。 3.2 抗寄生虫、抗病毒及抗真菌药物依莫赛普（Emodepside, 3.16，BAY 44-4400）抗寄生虫药 II期临床试验药物类别：PF1022A的双吗啉衍生物。研发单位：被忽视疾病药物研发计划组织（DNDi）。应用背景：自2005年起与吡喹酮联用治疗猫、狗寄生性线虫感染169。临床进展：正在进行针对类圆线虫（Strongyloides stercoralis）的II期试验（NCT06373835）盘尾丝虫病的II期试验（NCT05180461）170–172 已完成针对人鞭虫（Trichuris trichiura）、钩虫（NCT05017194）及单独钩虫感染（NCT05538767）的II期试验173 母体化合物PF1022A：1992年首次从Rosellinia属真菌中报道174，对鸡蛔虫有体内活性，但对细菌、酵母及其他真菌无体外活性175–177。作用机制：主要激活SLO-1钾通道178,179 与latrophilin受体相互作用180,181 导致虫体麻痹及GABA能传递调节182 格里菲辛（Griffithsin）抗病毒蛋白 I期临床试验完成药物来源：从新西兰红藻Griffithsia sp.中分离的121个氨基酸凝集素。抗病毒谱：对HIV、2型单纯疱疹病毒及丙型肝炎病毒具有皮摩尔级抑制活性。作用机制：通过结合病毒颗粒表面高甘露糖寡糖末端的甘露糖残基，引发聚糖交联，抑制病毒入侵185,186。研发进展：路易斯维尔大学开发了鼻喷剂型（Q-格里菲辛，含M78Q突变以提高氧化稳定性）已完成两项用于COVID-19预防的I期试验（NCT05437029、NCT05122260）187 早期I期试验（NCT02875119）评估其与卡拉胶联用预防性传播感染的潜力，安全性良好188 生产优势：可通过重组表达系统生产183,184。沙比沙布林（Sabizabulin, 3.17，VERU-111，ABI-231）抗病毒/抗肿瘤 III期临床试验完成药物类别：康普瑞汀A4（combretastatin A4, 3.18）结构启发类似物189。研发单位：Veru Inc。临床进展： 2022年中完成一项针对COVID-19高危急性呼吸窘迫综合征（ARDS）患者的III期试验（NCT04842747）；中期分析显示较安慰剂组绝对死亡率降低24.9%190 后续开发将取决于资金与合作临床需求曾评估用于转移性去势抵抗性前列腺癌治疗191，但一项III期试验（NCT04844749）于2023年因战略原因中止作用机制：通过结合微管蛋白秋水仙碱位点破坏微管聚合，导致快速分裂细胞周期停滞与凋亡189 可干扰冠状病毒S蛋白分布，阻碍病毒颗粒胞内运输、组装与复制192,193 藏红花素（Transcrocetin, 3.19）抗病毒/ARDS治疗 II期临床试验完成药物来源：黄色脱辅基类胡萝卜素，源自栀子（Gardenia jasminoides）与藏红花（Crocus sativus）等植物194。生物合成：通过玉米黄质酶切及醛基还原生成195–197。临床进展： Leaf4Life开发的脂质体制剂（LEAF-4L6715）已完成COVID-19相关ARDS的I/II期试验（NCT04378920）198 一项III期试验（NCT06640777）已注册但尚未启动其钠盐制剂由Diffusion Pharmaceuticals（现属CervoMed）开展COVID-19的II期试验（NCT04573322）200，但后续开发似已中止作用机制：通过降低血浆粘度并改变水分子结构，增强氢键形成，促进氧扩散梯度下的氧输送效率194,199。 SF001（3.20，AM-2-19）抗真菌药 I期临床试验药物类别：两性霉素B的N-1,3-二羟丙基-2-酰胺衍生物201,202。研发单位：Elion Therapeutics。临床进展：正在开展静脉制剂I期试验，评估治疗侵袭性曲霉病潜力口服剂型亦在评估中安全性优势：两性霉素B的人肾毒性与其胆固醇提取作用相关；3.20通过选择性增强麦角固醇提取能力，在小鼠及人原代肾细胞中显示肾脏保护特性203–205。 HRS9432（结构未公开）抗真菌药 II期临床试验药物类别：阿尼芬净（anidulafungin）衍生物121。研发单位：福建新cadia制药。临床进展：正在开展II期试验（NCT06194201），评估治疗念珠菌血症和/或侵袭性念珠菌病。相关药物：其他棘白菌素类药物如瑞扎芬净（rezafungin, 2.35）已于2023年获批（第2节）48。 SCY-247（3.21）抗真菌药 I期临床试验启动药物类别：第二代Fungerp类抗真菌药49,206–208，为真菌来源三萜烯芬净（enfumafungin, 3.22）衍生物209。研发单位：Scynexis。临床进展：2024年12月宣布启动针对侵袭性真菌感染的I期试验（ACTRN12624001393549、ACTRN12624001392550）210。同类首创新药：伊布雷沙芬净（ibrexafungerp, 2.30）作为首个Fungerp类药物于2021年获批（第2节）47,49。待续广州凯美科信息技术有限公司是一家以化学信息学软件为核心业务的企业。公司成立于2019年10月，竭诚为国内医药、化工、食品等领域用户提供高质量的化学信息学软件解决方案和技术服务。作为加拿大ACD/Labs公司在国内的合作伙伴，我们在化合物结构鉴定、化学信息管理、色谱方法开发、化合物成药性评价、药物分子设计、分子模拟等方面累积了丰富的服务经验，并且得到广泛好评。产品包括(点击查看详情)： ✅ 化合物波谱解析系列 ✅ 化合物成药性预测 ✅ 化合物性质预测系列 ✅ 色谱方法开发系列 ✅ 实验室化学信息管理 —————————————————— ✅ 智能解析｜👉 [申请核磁/质谱解析软件演示]✅ 疑难攻坚｜📩 [提交疑难数据，获取专家支援]✅ 购买升级｜💼 [单位采购/版本更新/技术培训] 📢 联系我们：▔▔▔▔▔▔▔▔▔▔▔🧑 产品经理｜胡炽文📲 电话/微信｜18680221948📮 服务邮箱｜hcw@chemico.com.cn🌍 官网直达｜www.chemico.com.cn 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临床3期微生物疗法

2025-08-12

·GlobeNewswire-Health Care

Veru Announces Selection of Novel Modified Release Oral Enobosarm Formulation for Chronic Weight Loss Management Following Pharmacokinetic Clinical Study

Aug. 11, 2025 -- Veru Inc. (NASDAQ: VERU), a late clinical stage biopharmaceutical company focused on developing innovative medicines for the treatment of cardiometabolic and inflammatory diseases, today announced selection of a novel modified release oral formulation for enobosarm, a selective androgen receptor modulator, for chronic weight loss management, following confirmation of pharmacokinetic endpoints in a clinical study. The single dose, open label pilot study evaluated the plasma concentration versus time profile of a proprietary, patentable modified release formulation of enobosarm 3mg. The new formulation demonstrated the intended distinct target product release profile, which includes a reduction in maximum plasma concentration (Cmax), a delayed time to maximum plasma concentration (Tmax), a distinct secondary peak plasma concentration, and similar extent of absorption (AUC) compared to historical values for enobosarm immediate release capsules. “The novel enobosarm oral formulation’s unique manufacturing process is protected by a robust patent estate of already issued global patents with protection through 2037 and beyond. Patent applications on enobosarm’s new oral formulation have been filed and if issued, expiry is expected to be 2046,” said Mitchell Steiner, M.D., Chairman, President, and Chief Executive Officer of Veru. “This novel modified release oral enobosarm formulation is planned to be available for the Phase 3 clinical studies and for commercialization.” The novel modified release oral formulation of enobosarm was developed in collaboration with Laxxon Medical using smart delivery systems, including the Company’s proprietary patented SPID®-Technology to create advanced, unique oral delivery release profiles, as well as an innovative additive manufacturing process. “We are proud to partner with Veru, which leveraged our proprietary SPID®-Technology to develop a novel oral formulation while ensuring strong IP protection for future commercialization,” said Helmut Kerschbaumer, Chief Executive Officer of Laxxon Medical. “This innovation has the potential to meaningfully advance Veru’s clinical program and differentiate its enobosarm formulation.” Veru is a late clinical stage biopharmaceutical company focused on developing innovative medicines for the treatment of cardiometabolic and inflammatory diseases. The Company’s drug development program includes two late-stage novel small molecules, enobosarm and sabizabulin. Enobosarm, a selective androgen receptor modulator (SARM), is being developed as a next generation drug that makes weight reduction by GLP-1 RA drugs more tissue selective for loss of fat and preservation of lean mass thereby improving body composition and physical function. Sabizabulin, a microtubule disruptor, is being developed for the treatment of inflammation in atherosclerotic cardiovascular disease. Obesity Program - Enobosarm is a next generation drug that makes weight reduction by GLP-1 RA more tissue selective for fat loss – Phase 2b QUALITY clinical studyEnobosarm Obesity Program The Company has previously announced positive topline and safety results from the Phase 2b QUALITY clinical study, which is a multicenter, double-blind, placebo-controlled, randomized, dose-finding clinical trial designed to evaluate the safety and efficacy of enobosarm 3mg, enobosarm 6mg, or placebo as a treatment to augment fat loss and to prevent muscle loss in 168 older patients (≥60 years of age) receiving semaglutide (Wegovy®) for chronic weight management. After completing the efficacy dose-finding portion of the Phase 2b QUALITY clinical trial, participants continued into a Phase 2b maintenance extension study where all patients discontinued semaglutide treatment, but continued receiving placebo, enobosarm 3mg, or enobosarm 6mg as monotherapy in a double-blind fashion for 12 weeks. On June 24, 2025, the Company announced positive results from the Phase 2b QUALITY and Maintenance Extension clinical study showing enobosarm significantly reduced body weight regain, prevented fat regain, and preserved lean mass after semaglutide discontinuation. In conclusion, the Phase 2b QUALITY and Maintenance Extension clinical trial confirms that preserving lean mass with enobosarm plus semaglutide led to greater fat loss during the active weight loss period, and after semaglutide was discontinued, enobosarm monotherapy significantly prevented the regain of both weight and fat mass during the maintenance period such that by end of study there was greater loss of fat mass while preserving lean mass for a higher quality weight reduction compared to the placebo group. Laxxon Medical is a leading pharma-technology company and global leader of smart drug delivery systems in the pharmaceutical industry, pioneering a new generation of advanced pharmaceuticals designed to optimize drug delivery and maximize patient success through SPID®-Technology, Laxxon’s proprietary 3D screen printing (3DSP) technology platform. SPID®-Technology unlocks innovative drug delivery advancements paired with fast-tracked market access and extensive IP protection to yield disruptive opportunities in drug development and commercialization. With SPID®-Technology, Laxxon can develop and manufacture advanced versions of new and existing pharmaceutical drugs while extending and adding new patent protection through the technology transfer process. Laxxon can fully utilize the FDA’s 505b(2) regulatory pathway in the US and Hybrid applications under article 10(3) of Directive 2001/83/EC in the EU, which fast tracks product routes to market. Laxxon's pipeline includes ongoing working-projects with notable pharma players, biotech companies and research universities, in addition to 13 in-house Advanced Patented Generics products. Laxxon's IP is continuously growing, and together with the licensed IP from Exentis Group, consists of more than 230 patents and patent applications with more than 5,000 patent claims. The content above comes from the network. if any infringement, please contact us to modify.

临床结果

100 项与沙比沙布林相关的药物交易

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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
新型冠状病毒感染	申请上市	加拿大	Veru, Inc.	2023-01-31
转移性去势抵抗性前列腺癌	临床3期	美国	Veru, Inc.	2021-06-24
急性呼吸窘迫综合征	临床3期	美国	Veru, Inc.	2021-05-18
急性呼吸窘迫综合征	临床3期	阿根廷	Veru, Inc.	2021-05-18
急性呼吸窘迫综合征	临床3期	巴西	Veru, Inc.	2021-05-18
急性呼吸窘迫综合征	临床3期	保加利亚	Veru, Inc.	2021-05-18
急性呼吸窘迫综合征	临床3期	哥伦比亚	Veru, Inc.	2021-05-18
急性呼吸窘迫综合征	临床3期	墨西哥	Veru, Inc.	2021-05-18
严重急性呼吸综合征	临床3期	美国	Veru, Inc.	2021-05-18
严重急性呼吸综合征	临床3期	阿根廷	Veru, Inc.	2021-05-18

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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


NCT04842747 (phase 3 \| VERU-111, CTgov)	临床3期	新型冠状病毒感染 \| 急性呼吸窘迫综合征 \| 严重急性呼吸综合征	204	VERU-111 (9mg of VERU-111 Oral Daily)	壓獵築餘繭觸顧鏇築願 = 鏇蓋齋繭襯範鹽鏇廠鑰積選製醖淵鏇獵鹹糧製 (築積餘夢遞鹽鏇願觸憲, 蓋淵願淵構齋餘簾繭衊 ~ 糧餘艱繭獵膚蓋艱鬱淵) 更多	-	2023-04-18
NCT04842747 (phase 3 \| VERU-111, CTgov)	临床3期	新型冠状病毒感染 \| 急性呼吸窘迫综合征 \| 严重急性呼吸综合征	204	placebo (Placebo Capsule Once Daily)	壓獵築餘繭觸顧鏇築願 = 鬱餘範蓋選遞壓鏇淵淵積選製醖淵鏇獵鹹糧製 (築積餘夢遞鹽鏇願觸憲, 衊構齋窪夢醖蓋範艱鑰 ~ 觸鑰壓窪鹹鹽簾鹽製範) 更多	-	2023-04-18
NCT04842747 (Literature) 人工标引	临床3期	新型冠状病毒感染	204	Sabizabulin	壓選糧觸鹹廠鏇糧積選(餘積網鬱簾廠艱醖夢遞) = 獵繭築觸齋築艱願糧鹹膚觸構醖蓋窪鹹醖憲襯 (範壓鑰窪願範製觸齋廠 )	积极	2022-07-06
NCT04842747 (Literature) 人工标引	临床3期	新型冠状病毒感染	204	Placebo	壓選糧觸鹹廠鏇糧積選(餘積網鬱簾廠艱醖夢遞) = 獵積淵鏇鏇齋遞艱簾襯膚觸構醖蓋窪鹹醖憲襯 (範壓鑰窪願範製觸齋廠 )	积极	2022-07-06
NCT03752099 (ASCO2022)	临床1/2期	转移性去势抵抗性前列腺癌	80	Sabizabulin	鹹範淵鏇憲構願築鏇鬱(鬱願積鏇遞膚膚鹹製網) = 5.6% and 3.7%, respectively 淵簾鏇糧構餘糧鑰襯膚 (築艱選鹽衊窪壓範襯衊 ) 更多	-	2022-06-02
NCT03752099 (ASCO_GU2022)	临床1/2期	转移性去势抵抗性前列腺癌	80	Sabizabulin	襯築遞遞蓋網繭淵艱膚(鏇鏇製憲願觸積獵獵蓋) = no clinically relevant neurotoxicity 廠觸網願廠製遞艱簾餘 (繭構獵觸衊夢遞餘範廠 ) 更多	积极	2022-02-16
NCT04844749 (VERACITY, ASCO_GU2022)	临床3期	转移性去势抵抗性前列腺癌	245	Sabizabulin 32mg/d oral	遞醖範繭糧淵壓選膚廠(積襯鹽壓繭憲糧網遞廠) = 範醖壓鬱鏇衊築範範窪願積構願顧遞齋簾築構 (衊網獵願觸鏇襯選窪膚 )	积极	2022-02-16
NCT04388826 (CTgov)	临床2期	新型冠状病毒感染 \| 成人呼吸窘迫综合征 \| 急性呼吸窘迫综合征 ... 更多	39	Veru-111 (Veru-111 18 mg)	襯繭鑰夢願窪蓋積遞鬱 = 憲糧築鹹壓餘淵衊膚衊構餘鏇選選顧齋觸構鹹 (廠憲顧構襯餘鏇鑰鏇願, 鏇積網憲願獵鬱窪鬱鏇 ~ 簾壓遞鑰願襯鹹夢蓋鏇) 更多	-	2021-11-24
NCT04388826 (CTgov)	临床2期	新型冠状病毒感染 \| 成人呼吸窘迫综合征 \| 急性呼吸窘迫综合征 ... 更多	39	Veru-111 (Placebo)	襯繭鑰夢願窪蓋積遞鬱 = 廠廠壓鏇醖繭醖鹹願齋構餘鏇選選顧齋觸構鹹 (廠憲顧構襯餘鏇鑰鏇願, 糧餘餘範齋觸餘築簾壓 ~ 襯繭壓壓襯衊觸艱齋簾) 更多	-	2021-11-24
NCT03752099 (ESMO 12021 \| ESMO 22021) 人工标引	临床1/2期	转移性去势抵抗性前列腺癌	-	sabizabulin	艱積構齋繭獵齋鑰獵製(鹹繭膚築簾襯網築構廠) = Sabizabulin was well tolerated with the most common adverse events (>10% frequency) in patients that received 63 mg dose (n=54) including diarrhea, fatigue, ALT and AST increases which were mostly Grade 1 and 2. 襯鹹膚鬱鏇積繭願顧齋 (糧艱窪窪鏇艱網膚鹹構 )	积极	2021-09-19
NCT03752099 (ASCO2021)	临床1/2期	转移性去势抵抗性前列腺癌	58	VERU-111	鹽積獵觸淵艱窪積鹽選(願範鑰艱襯鹹廠築網鹹) = 夢築醖顧襯艱願網獵鹽繭遞衊壓醖蓋鑰齋鹹憲 (壓夢製壓淵艱繭鬱鹹遞 ) 更多	-	2021-05-28
NCT03752099 (ASCO_GU2021)	临床1/2期	转移性去势抵抗性前列腺癌	40	VERU-111	顧鏇蓋淵構範築衊壓鹹(製膚願鏇鏇選簾襯遞膚) = 3 /11 men had Grade 3 diarrhea 鹹鹽艱衊窪衊衊範襯構 (廠糧製餘獵醖艱鏇鑰艱 )	积极	2021-03-02
NCT03752099 (ESMO2020)	临床2期	转移性去势抵抗性前列腺癌	30	VERU-111	構築餘蓋壓網觸鏇遞蓋(觸糧顧糧鑰鏇廠願齋築) = 3 /11 men had Grade 3 diarrhea at MTD of VERU-111 範膚網鏇構範壓憲餘觸 (衊膚糧鹹觸襯襯壓齋獵 ) 更多	积极	2020-09-18