主要目的：评估卟硒啉联合放疗在治疗原发术后高级别脊髓胶质瘤患者中的安全性；次要目的：评价卟硒啉联合放疗在治疗原发术后高级别脊髓胶质瘤患者中的多次给药PK特征；探索性目的：评价卟硒啉联合放疗在治疗原发术后高级别脊髓胶质瘤患者中的初步有效性；探索卟硒啉联合放疗在治疗原发术后高级别脊髓胶质瘤患者中的生物标志物。

开始日期2024-04-17

申办/合作机构

上海元熙医药科技有限公司初创企业

CTR20222921 / Active, not recruiting临床2期

一项在纤维化性间质性肺病患者中评价标准治疗联合卟硒啉片的安全性和药代动力学特征的单中心、随机、双盲、安慰剂对照IIa期临床试验

主要目的：评估标准治疗（由研究者决定）联合卟硒啉片在纤维化性间质性肺病患者中的安全性；次要目的：评价标准治疗（由研究者决定）联合卟硒啉片在纤维化性间质性肺病患者中的单次和多次给药PK特征；探索性目的：评价标准治疗（由研究者决定）联合卟硒啉片治疗纤维化性间质性肺病的初步有效性；探索标准治疗（由研究者决定）联合卟硒啉片治疗纤维化性间质性肺病的生物标志物

开始日期2023-04-17

申办/合作机构

上海元熙医药科技有限公司初创企业

CTR20210706 / Completed临床1期

评价BS1801在健康成年受试者单次及多次口服给药后的安全性、耐受性、药代动力学的I期临床试验

本试验分为2项子研究开展，每项研究试验目的如下：单次给药研究目的：主要目的：评价BS1801单次口服给药后的安全性和耐受性。次要目的：评价BS1801单次口服给药后的药代动力学特征。多次给药研究目的：主要目的：评价BS1801多次口服给药后的安全性和耐受性。次要目的：评价BS1801多次口服给药后的药代动力学特征。

开始日期2021-04-22

申办/合作机构

上海元熙医药科技有限公司初创企业

100 项与卟硒啉相关的临床结果

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100 项与卟硒啉相关的转化医学

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100 项与卟硒啉相关的专利（医药）

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项与卟硒啉相关的文献（医药）

2023-12-01·Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

TrxR/Trx inhibitor butaselen ameliorates pulmonary fibrosis by suppressing NF-κB/TGF-β1/Smads signaling

Article

作者: Sun, Jing ; Zhang, Guozhou ; Yin, Hanwei ; Chen, Yifan ; Zhang, Ying ; Zeng, Huihui

Pulmonary fibrosis is highly lethal with limited treatments. Butaselen (BS) is an inhibitor of thioredoxin reductase (TrxR)/thioredoxin (Trx) with anti-tumor activity. However, its impact on pulmonary fibrosis and the involved mechanisms remain unclear. Here, we demonstrate that BS is a potential drug for the treatment of pulmonary fibrosis. Specifically, BS can inhibit pulmonary fibrosis both in vitro and in vivo, with comparable efficacy and enhanced safety when compared with pirfenidone. BS and dexamethasone display a synergistic effect in inhibiting pulmonary fibrosis both in vitro and in vivo. Mechanistic studies reveal that BS can inhibit the TrxR activity during pulmonary fibrosis. RNA-sequencing analysis identifies that genes of ECM-related signaling pathways are notably affected by BS. BS can not only inhibit the activation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and reduce pulmonary fibrosis-related inflammation, but also reduce NF-κB-activated transcriptional expression of transforming growth factor-β1 (TGF-β1), which leads to the inactivation of Smad2/Smad3 and decrease of collagen formation and fibrosis. Moreover, the knockdown of Trx1 with siRNA can also inhibit NF-κB/TGF-β1/Smads signaling. In conclusion, the TrxR/Trx inhibitor butaselen can suppress pulmonary fibrosis by inhibiting NF-κB/TGF-β1/Smads signaling.

2023-03-01·Journal of immunology (Baltimore, Md. : 1950)

A Novel TrxR1 Inhibitor Regulates NK and CD8+ T Cell Infiltration and Cytotoxicity, Enhancing the Efficacy of Anti–PD-1 Immunotherapy against Hepatocarcinoma

Article

作者: Liu, Runyu ; Wen, Jinhua ; Bai, Man ; Yin, Hanwei ; Liu, Jiayi ; Su, Xiaoxia ; Zeng, Huihui

Abstract:

Hepatocellular carcinoma (HCC) has the third highest cancer-related mortality rate globally. The immunosuppressive microenvironment of HCC limits effective treatment options. HCC cells and associated microenvironmental factors suppress NK and T cell infiltration and cytotoxic activities. The abnormal number or function of NK and T cells leads to a lack of immune surveillance. Recently, immunotherapy targeting PD-1 and PD-L1 has been shown to activate functionally exhausted cytotoxic immune cells in some solid tumors. However, the response rate and therapeutic efficacy against solid tumors with little lymphocyte infiltration are limited, especially for HCC. Therefore, new targets and therapeutics that induce tumor cell apoptosis and overcome the problem of depletion of immune cells, thereby inhibiting the immune escape of HCC cells, are urgently required. Butaselen (2-bis[2-(1,2-benzisothiazol-2(2H)-ketone)]butane), an organic molecule containing selenium, is a new type of thioredoxin reductase inhibitor. In this study, we found that butaselen promoted NK and T cell activity and infiltration in the tumor microenvironment in HCC-bearing mice by enhancing the expression of CXCR3, NKG2D, and their respective ligands. When used alone, it can significantly inhibit tumor growth and exert a synergistic effect in combination with PD-1 blockade. We suggested the role of the thioredoxin reductase system in the regulation of the tumor immunosuppressive microenvironment and developed a new effective therapeutic molecule for HCC, revealing the mechanism of butaselen in inhibiting tumor cell immune escape.

2022-09-01·Current drug metabolism

Investigating the Metabolic Mechanisms of Butaselen, An Ebselen Analog

Article

作者: Peng, Chao ; Wu, Ping ; Wang, Zhijie ; Li, Yilin ; Zhong, Dafang ; Yin, Hanwei ; Tian, Qianqian ; Jiang, Jinfang ; Zhou, Jialan ; Zeng, Huihui ; Zhang, Yifan

Background::

Butaselen is an ebselen analog that is under clinical trials for treating hepatic and pulmonary fibrosis. Our previous studies showed that butaselen is mainly present in human plasma in the form of M2, a free Se-methylated metabolite.

Objective::

This study aimed to investigate the metabolic mechanisms of butaselen.

Methods and Results::

Butaselen was incubated with human plasma. Butaselen immediately disappeared, and the butaselen-HSA (human serum albumin) adduct was detected by HPLC-HRMS, showing that butaselen covalently binds to HSA. The butaselen-HSA adduct was precipitated using acetonitrile and then incubated with PBS, Cys, and GSH for 1 hour. The product was M1, a reduced form of butaselen. The results indicated that HSA, Cys, and GSH can reduce the butaselen-HSA covalent bond. The binding site for butaselen could be the cysteine-34 residue of HSA through pronase and trypsin hydrolysis. Incubating butaselen with cysteine, butaselen-Cys, butaselen-2Cys, and M1 were generated, indicating the covalent binding and reduction of butaselen by cysteine. We incubated liver microsomes and cytosol with butaselen, 6.22 and 246 nM M2 were generated, respectively. The results demonstrated that cytosolic enzymes are mainly involved in M2 production. The amount of M2 in the liver cytosol decreased from 246 nM to 2.21 nM when 10 mM m-anisic acid (a specific TPMT enzyme inhibitor) was added, showing that TPMT is responsible for M2 formation.

Conclusion::

Butaselen was covalently bound to HSA, and the binding site was the cysteine-34 residue of HSA. The butaselen-HSA adduct was reduced by free thiol compounds to generate M1. M1 was further metabolized to M2 by cytosolic TPMT. This study provides a basis for studying the pharmacokinetics of selenium-containing drugs.

项与卟硒啉相关的新闻（医药）

2022-09-12

·信狐药迅

厦门恩成兰索拉唑碳酸氢钠上市申请，礼来替尔泊肽进口申报 | 新受理（9.5-9.11）

每周药品注册受理数据，分门别类呈现，一目了然。新药上市申请药品名称企业名称分类受理号兰索拉唑碳酸氢钠胶囊厦门恩成制药有限公司2.2CXHS2200046舒格利单抗注射液基石药业(苏州)有限公司2.2CXSS2200077水痘减毒活疫苗北京民海生物科技有限公司3.3CXSS2200078新药临床申请药品名称企业名称分类受理号AB-218 胶囊葆元生物医药科技(杭州)有限公司1CXHL2200649BEBT-607片广州必贝特医药股份有限公司1CXHL22006501CXHL2200651BH009注射液珠海贝海生物技术有限公司2.2CXHL2200668DC561043片中国科学院上海药物研究所1CXHL22006541CXHL22006551CXHL2200656FB-1071福贝生物医药科技(北京)有限公司1CXHL2200663FZJ-003凝胶上海复旦张江生物医药股份有限公司1CXHL22006521CXHL2200653HMI-115和其瑞医药(南京)有限公司1CXSL2200442HR20031片(I)山东盛迪医药有限公司1CXHL2200661HR20031片(II)1CXHL2200662KP104注射液科越医药(苏州)有限公司1CXSL2200437KQ-L6自体嵌合抗原受体T细胞注射液上海科棋药业科技有限公司1CXSL2200440LM-101注射液礼新医药科技(上海)有限公司1CXSL2200438QL1706注射液齐鲁制药有限公司1CXSL2200439QX004N注射液江苏荃信生物医药股份有限公司1CXSL2200443TML-023软膏武汉科福新药有限责任公司2.2;2.4CXHL2200648TY-1091胶囊浙江同源康医药股份有限公司1CXHL22006591CXHL2200660Y101D武汉友芝友生物制药股份有限公司1CXSL2200456ZHB107-108舌下片江苏众红生物工程创药研究院有限公司2.4CXSL22004542.4CXSL22004492.4CXSL22004502.4CXSL22004512.4CXSL22004522.4CXSL2200453ZVS101e 注射液北京中因科技有限公司1CXSL22004471CXSL2200448卟硒啉片上海元熙医药科技有限公司1CXHL22006641CXHL22006651CXHL2200666聚乙二醇重组人促红素注射液深圳赛保尔生物药业有限公司1CXSL2200444注射用 GMDTC健尔圣(珠海)医药科技有限公司1CXHL2200667注射用TQB2934正大天晴药业集团南京顺欣制药有限公司1CXSL2200441注射用YL202苏州宜联生物医药有限公司1CXSL2200455自体RAK细胞注射液普华赛尔生物医疗科技有限公司1CXSL22004451CXSL2200446仿制药申请药品名称企业名称分类受理号阿加曲班注射液四川新斯顿制药股份有限公司4CYHS2201455阿立哌唑口服溶液锦州奥鸿药业有限责任公司3CYHS22015063CYHS2201507阿普米司特片桂林南药股份有限公司4CYHS2200763氨甲环酸注射液华夏生生药业(北京)有限公司3CYHS22014773CYHS2201478氨溴特罗口服溶液江苏广承药业有限公司3CYHS2201487奥拉帕利片湖南科伦制药有限公司4CYHS22014754CYHS2201476奥美沙坦酯氨氯地平片浙江诺得药业有限公司4CYHS2201502蛋白琥珀酸铁口服溶液北京民康百草医药科技有限公司4CYHS2201491锝[99mTc]替曲膦注射液南京江原安迪科正电子研究发展有限公司3CYHS2201457地夸磷索钠滴眼液健民药业集团股份有限公司4CYHS2201480江苏万高药业股份有限公司4CYHS2201453氟比洛芬凝胶贴膏湖南九典制药股份有限公司4CYHL2200076富马酸丙酚替诺福韦片杭州民生药业股份有限公司4CYHS2201466己酮可可碱注射液山东泰合医药科技有限公司3CYHS2201467利伐沙班细粒剂浙江恒研医药科技有限公司3CYHS22014843CYHS2201485磷酸奥司他韦干混悬剂浙江高跖医药科技股份有限公司3CYHS2201479硫酸特布他林雾化吸入用溶液健民药业集团股份有限公司4CYHS2201464吗啉硝唑氯化钠注射液四川汇宇制药股份有限公司4CYHS2201499帕拉米韦注射液河北天成药业股份有限公司3CYHS22015003CYHS2201501葡萄糖酸钙氯化钠注射液回音必集团抚州制药有限公司3CYHS22014973CYHS2201498吸入用硫酸沙丁胺醇溶液天津梅花生物医药科技有限公司4CYHS2201454吸入用异丙托溴铵溶液郑州深蓝海生物医药科技有限公司4CYHS22014684CYHS2201469西格列汀二甲双胍片(I)吉林惠升生物制药有限公司4CYHS2201495西格列汀二甲双胍片(II)4CYHS2201496腺苷钴胺胶囊海南赛立克药业有限公司3CYHS2201465盐酸胺碘酮注射液桂林南药股份有限公司4CYHS2201486盐酸伐地那非片海南红祥旗荣医药科技有限公司4CYHS22014934CYHS2201494盐酸利多卡因注射液石家庄四药有限公司3CYHS22014583CYHS22014593CYHS2201460盐酸罗哌卡因注射液山东华鲁制药有限公司4CYHS22014824CYHS2201483盐酸溴己新注射液海南葫芦娃药业集团股份有限公司3CYHS2201492依折麦布辛伐他汀片北京福元医药股份有限公司4CYHS2201489注射用卡非佐米齐鲁制药(海南)有限公司4CYHS22014724CYHS22014734CYHS2201474注射用帕瑞昔布钠陕西博森生物制药股份集团有限公司4CYHS22014704CYHS2201471注射用头孢他啶阿维巴坦钠南京恩泰医药科技有限公司4CYHS2201463注射用盐酸罗沙替丁醋酸酯武汉海特生物制药股份有限公司3CYHS2201488注射用盐酸头孢替安齐鲁安替制药有限公司3CYHS22015033CYHS22015043CYHS2201505左氧氟沙星片南京正科医药股份有限公司4CYHS2201490左氧氟沙星注射液安徽省先锋制药有限公司3CYHS2201462左乙拉西坦注射用浓溶液黑龙江珍宝岛药业股份有限公司4CYHS2201456ω-3脂肪酸乙酯90软胶囊人福普克药业(武汉)有限公司4CYHS2201481进口申请药品名称企业名称分类受理号AZD7789AstraZeneca AB1JXSL2200155DS-1062aDaiichi Sankyo, Inc.1JXSL2200156Inclisiran注射液Novartis Pharma AG2.4JXHL22002772.4JXHL2200278KIN-3248片Kinnjiu Biopharma Limited1JXHL22002821JXHL22002831JXHL2200284MK-0616胶囊Merck Sharp & Dohme LLC1JXHL22002751JXHL2200276NBQ72SNANTONG BENCAO QUADRIGA MEDICAL TECHNOLOGY HK LIMITED1JXHL2200279Tigulixostat片LG CHEM, LTD.1JXHL22002801JXHL2200281安纳白介素注射液(预充式)Swedish Orphan Biovitrum AB (publ)3.1JXSS2200034达格列净片AstraZeneca AB2.4JXHS22000792.4JXHS2200080古塞奇尤单抗注射液Janssen-Cilag International NV3.1JXSL2200163吉非替尼片Natco Pharma Limited5.2JYHS2200084利特昔替尼胶囊Pfizer Inc.1JXHS2200081硫酸瑞美吉泮口崩片Biohaven Pharmaceutical Ireland DAC5.1JXHS2200074替尔泊肽注射液Eli Lilly and Company5.1JXHS22000755.1JXHS22000765.1JXHS22000775.1JXHS2200078注射用福沙匹坦双葡甲胺MSN Laboratories Private Limited5.2JYHS2200083注射用培重组人凝血因子ⅧBaxalta US Inc.3.1JXSL22001573.1JXSL22001583.1JXSL22001593.1JXSL22001603.1JXSL22001613.1JXSL2200162中药相关申请无。

疫苗抗体

100 项与卟硒啉相关的药物交易

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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
肺纤维化	临床2期	中国	上海元熙医药科技有限公司初创企业	2023-04-17
高级别胶质瘤	临床1期	中国	上海元熙医药科技有限公司初创企业	2024-04-17
肝纤维化	临床申请批准	中国	上海元熙医药科技有限公司初创企业	2021-07-06