第一阶段主要目的： 1）评价EN002外用凝胶治疗非黑色素瘤皮肤癌的安全性和耐受性；次要目的： 1）评价EN002外用凝胶在非黑色素瘤皮肤癌受试者中的药代动力学特征； 2）探索EN002外用凝胶治疗非黑色素瘤皮肤癌的疗效，为后续阶段试验给药剂量和给药方案提供依据；第二阶段主要目的： 1）评价EN002外用凝胶治疗非黑色素瘤皮肤癌的抗肿瘤疗效，并确定适应症；次要目的： 1）评价EN002外用凝胶治疗非黑色素瘤皮肤癌的有效性和安全性； 2）评价受试者的生活质量改善情况。

开始日期2022-08-22

申办/合作机构

药源生物科技（启东）有限公司

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100 项与 EN-002 相关的临床结果

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100 项与 EN-002 相关的转化医学

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100 项与 EN-002 相关的专利（医药）

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项与 EN-002 相关的文献（医药）

2023-01-01·Journal of Natural Medicines

17β-neriifolin from unripe fruits of Cerbera manghas suppressed cell proliferation via the inhibition of HOXA9-dependent transcription and the induction of apoptosis in the human AML cell line THP-1

Article

作者: Ito, Akihiro ; Sekine, Saaya ; Yun, Young Sook ; Yahagi, Tadahiro ; Inoue, Hideshi ; Takase, Shohei ; Moriya, Fuki ; Yotsumoto, Satoshi ; Miyake, Katsunori

Homeobox A9 (HOXA9) is a transcription factor that is overexpressed in acute myeloid leukemia (AML). It is associated with the pathogenesis and progression of AML, and is a factor responsible for a poor prognosis. Therefore, the development of HOXA9-targeting molecules may contribute to not only better understanding of the mechanism of HOXA9 regulation, but also the development of therapeutic applications. We constructed a reporter assay system using the promoter region of the KBTBD10 gene, to which HOXA9 directly binds and regulates transcription, in the human acute monocytic leukemia cell line THP-1. Using this luciferase gene assay, we screened 1120 plant extracts and a methanol extract of the unripe fruits of Cerbera manghas was found to suppress the reporter gene expression mediated by the KBTBD10 promoter. From the extract, five steroid-type compounds were identified as the active constituents: 7α-neriifolin (1), 17β-neriifolin (2), 17α-digitoxigenin β-D-glucosyl-(1 → 4)-α-L-thevetoside (3), 17β-digitoxigenin β-D-glucosyl-(1 → 4)-α-L-thevetoside (4), and acetylthevetin B (5). Among the five compounds, 17β-neriifolin most potently inhibited HOXA9-dependent gene expression without affecting the HOXA9 mRNA levels, and suppressed cell proliferation by inducing apoptosis. The findings on the structure-activity relationships of the compounds from C. manghas may contribute to the development of small molecule inhibitors of HOXA9.

2021-12-02·Food Additives & Contaminants: Part A3区 · 农林科学

Authentication of tejocote (Crataegus mexicana)dietary supplements based on DNA barcoding and chemical profiling

3区 · 农林科学

Article

作者: Moon, Guiim ; Park, Eun Mi ; Shin, Dasom ; Kim, Jungju ; Suh, Junghyuck ; Kwon, Jeongeun ; Kang, Hui-Seung

Tejocote (Crataegus mexicana, Mexican hawthorn), known as a weight-loss supplement, has been marketed online and is easily available for overseas direct purchase. Alipotec (brand name) is known as one of the most popular products containing tejocote in Mexico and other countries. However, adverse effects have been reported by users of these supplements. Therefore it is necessary to find the reason for the side effect. Dietary supplement samples labelled as containing tejocote were analysed using mass spectrometry and DNA barcoding analysis. Our results demonstrate that Alipotec samples contained ingredients from different species, yellow oleander instead of tejocote. The rpoB barcode region was able to differentiate between tejocote and yellow oleander species. Moreover, it was also observed that three compounds, including thevetin B, neriifolin, and digitoxigenin, clearly distinguish between tejocote and yellow oleander samples. This is the first and preliminary investigation to use an integrated approach of both chemical and genomic profiling for the authentication of dietary supplement containing tejocote.

2021-10-01·Toxicology Letters2区 · 医学

Investigation of cardiac glycosides from oleander in a human induced pluripotent stem cells derived cardiomyocyte model

2区 · 医学

Article

作者: Wille, T ; Thiermann, H ; Amend, N ; Worek, F

The ingestion of Nerium oleander and Thevetia peruviana are common causes for poisoning in Southeast Asia. All parts of the oleander shrub contain cardiac glycosides of the cardenolide type. These glycosides act via inhibition of a Na⁺/K⁺-ATPase which might cause severe arrhythmia and subsequent death in oleander-poisoned patients. The current study uses human induced pluripotent stem cells derived cardiomyocytes (hiPSC-CM) in a microelectrode array (MEA) system to assess the cardiac effects of neriifolin, oleandrin, digitoxigenin, peruvoside and thevetin A from the oleander plant. Digoxin was used as established reference compound. All tested compounds showed a corrected field potential duration (FPDc) shortening and was the lowest for 600 nM digitoxigenin with -36.9 ± 1.2 %. Next to the dose-dependent pro-arrhythmic potential, a complete beat arrest of the spontaneously beating hiPSC-CM was observed at a concentration of 300 nM for neriifolin, 600 nM for oleandrin and 1000 nM for digitoxigenin and peruvoside. Thevetin A did not cause arrhythmia up to a final concentration of 1000 nM. Thus, it was possible to establish a cardiac effect rank order of the tested substances: neriifolin > oleandrin > digitoxigenin = peruvoside > digoxin > thevetin A.

项与 EN-002 相关的新闻（医药）

2023-01-31

·医药观澜

恩康药业完成B轮融资，开发DRIPs靶向疗法等

▎药明康德内容团队报道1月30日消息，恩康药业科技有限公司（以下简称“恩康药业”）宣布完成数千万B轮融资。本轮投资由谢诺投资独家领投，资金将主要用于新药研发。公开资料显示，恩康药业是一家致力于创新抗癌新药及药物制剂研发的医药研发公司，由香港科技大学生命科学部梁纯教授研究团队、澳门科技大学药物及健康应用研究院姜志宏教授研究团队共同创立。据恩康药业新闻稿介绍，该公司以高选择性新靶标抗癌药物筛选技术为核心，致力于靶向DNA复制起始蛋白（DRIPs）原研小分子及核酸抗癌药物的研发。其首个靶向DRIPs的潜在“first-in-class”抗癌药物EN002凝胶已完成临床前研究，且已经获得治疗非黑色素瘤皮肤癌及癌前病变的中国1/2期临床批件，现已进入临床试验阶段。临床前体外和体内药效结果表明，EN002与其靶标DRIP蛋白结合，抑制DRIP蛋白活性以及DNA复制，在对正常细胞损伤较小的情况下使癌细胞凋亡，并对肝癌、胃癌、肺癌、宫颈癌、前列腺癌、皮肤癌等十余种肿瘤细胞具有明显的抑制作用，且活性高于许多目前抗肿瘤药物，提示EN002具有广泛的临床应用前景。另外，恩康药业还致力于吸入型脂质体顺铂（ILC）和其它治疗肺部疾病药物的脂质体新剂型的研发。恩康药业已经与Eleison公司签订合作协议，共同开发ILC用于肺部肿瘤的治疗。该顺铂脂质体吸入剂已经分别在美国和中国获得3期临床批件，正在启动该3期临床研究。据恩康药业官网资料介绍，顺铂是治疗肺癌的经典一线用药，通过制备肺吸入型顺铂脂质体复合物，采用创新的工艺实现以雾化吸入的创新给药方式，能够显著提高顺铂的给药便捷性和有效率，并极大降低其全身系统性毒副作用。参考资料：[1]恩康药业完成数千万B轮融资，谢诺投资独家领投. Retrieved Jan 30 , 2023. from https://mp.weixin.qq.com/s/utr9LFKuQorsKit1PKCK7w[2]恩康药业官网. From http://www.ek-pharma.com/本文由药明康德内容团队根据公开资料整理编辑，欢迎个人转发至朋友圈。转发授权请在「医药观澜」微信公众号留言联系我们。其他合作需求，请联系wuxi_media@wuxiapptec.com。免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。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。

临床3期抗体药物偶联物

100 项与 EN-002 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
皮肤黑色素瘤	临床2期	中国	恩康药业科技(广州)有限公司	2022-08-22
皮肤黑色素瘤	临床2期	中国	药源生物科技（启东）有限公司	2022-08-22