更新于：2024-11-01

Boric acid

硼酸

更新于：2024-11-01

概要

概要

基本信息

简介硼酸，即正硼酸，是一种白色结晶化合物，可用于多种用途，包括作为防腐剂、杀虫剂和阻燃剂。此外，其作为药物使用已超过100年，在包括美国在内的许多国家上市销售。它通常用作轻微切割和烧伤的消毒剂，以及用于某些阴道感染的治疗。硼酸也用于某些处方药物，用于治疗眼部感染。它是由Wilhelm Homberg通过矿物酸作用于硼砂而制备的，并被命名为"sedative salt of Homberg"。其确切的作用机制尚未完全理解。但是人们认为硼酸通过破坏真菌和细菌的细胞膜导致细胞死亡。此外，需要注意的是，硼酸在大量摄入或经过皮肤吸收时可能具有毒性。因此，应仅按医疗保健专业人员的指示或产品标签所示使用。

药物类型

小分子化药

别名

hydrogen borate、orthoboric acid

靶点-

作用机制-

治疗领域

肿瘤感染神经系统疾病+ [2]

在研适应症-

非在研适应症

自然流产细菌性阴道炎念珠菌病+ [9]

原研机构

ChoA Pharmaceutical Co., Ltd.

在研机构

ChoA Pharmaceutical Co., Ltd.

非在研机构

University of British Columbia

Bangalore Medical College & Research Institute

最高研发阶段批准上市

首次获批日期

美国 (2012-06-30)

最高研发阶段(中国)-

特殊审评-

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结构

分子式BH3O3

InChIKeyKGBXLFKZBHKPEV-UHFFFAOYSA-N

CAS号10043-35-3

关联

项与硼酸相关的临床试验

RBR-7m7yjdj / Recruiting临床3期IIT

Evaluation of the effectiveness of Boric Acid in otological bandage for treatment of infectious process in mastoid cavities: randomized and blind clinical study

开始日期2023-06-24

申办/合作机构-

CTRI/2022/01/039685 / CompletedN/AIIT

comparative evaluation of boric acid with chlorhexidine mouthwash in plaque induced gingivitis treatment- a double blind randomised controlled clinical trial

开始日期2022-01-27

申办/合作机构-

NCT04930107 / Recruiting早期临床1期IIT

Prospective Studies of Vaginal Yeast and Microbiome Related to Vulvovaginal Candidiasis in Canadian Females

Vulvovaginal candidiasis (VVC; colloquially referred to as a 'yeast infection') is a prevalent mucosal infection caused by Candida spp. that affects
75% of women at least once in their life. VVC usually responds well to treatment, yet a small but significant fraction of women experience recurrent yeast infections even with weekly treatment. A further complication in understanding the causes of recurrent infections is that approximately one in five females have vaginal yeast present without any symptoms at any given point. The link between fungi, other microbes in the vagina ("microbiome"), and the human immune system remain poorly understood in the switch from having yeast present in the vagina without any symptoms and symptomatic yeast infections. Fungi also compose a normal component of the microbiome at other sites in the body (e.g., oral, skin, gastrointestinal tract, rectum) where they may serve as a source of re-infection following treatment.
In addition to the commonly prescribed 'first choice' antifungal drug fluconazole, a second-line treatment, boric acid, has shown promise in the literature and has been used locally with success at increasing the time between recurrent infections. A drawback of this therapy, however, is cost, as it is a compounded medication, and patients have to pay out of pocket. The purpose of this study is to understand how the yeast and bacterial microbial communities differ for females with recurrent infections from females with their first yeast infection and females with vaginal yeast present without any symptoms, and to track yeast diversity following treatment with either boric acid or fluconazole. The investigators hypothesize that they will identify multiple subpopulations of yeast at multiple anatomical body sites in females with VVC and recurrent VVC. They anticipate finding evidence for recurrent infection from secondary sites by linking genomic diversity of vaginal yeast strains during symptomatic infection to strains from other body sites. They hypothesize that yeast isolated from females with recurrent infections will exhibit different drug response phenotypes than yeast from females with asymptomatic vaginal yeast. They hypothesize that the vaginal microbiome of post-treatment patients treated with boric acid will differ from that of fluconazole. Combined, they hypothesize that post-treatment response will differ between the drugs, indicating that treatment specifics influence the vaginal environment.

开始日期2021-12-07

申办/合作机构

University of Manitoba

[+2]

100 项与硼酸相关的临床结果

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100 项与硼酸相关的转化医学

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100 项与硼酸相关的专利（医药）

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653

项与硼酸相关的文献（医药）

2024-12-01·Biological Trace Element Research

Effects of Boric acid as Maternal Feed Additives on the Development and Sex Ratio of Mouse pups

Article

作者: Aykal, M B ; Sogut, I ; Gecin, M N ; Kar, F ; Taskin, A C

AbstractBoron is primarily used in industrial applications, with recent interest revolving around its effects on metabolism. In this study, we administered boric acid (BA), which has positive effects on reproduction, in conjunction with feed supplementation to serve as a model for experimental animal development and breeding. The pregnancy performance, offspring development, and biochemical effects of mice given feed supplemented with BA at concentrations of 0 (control group), 250, and 500 ppm (BA groups) were investigated. A total of 18 female Balb-C mice were utilized for pregnancy. The mice were given the BA-supplemented feed during a period encompassing three weeks of pregnancy and three weeks of lactation. The numbers and weights of offspring born in cages on days 19–21 were determined. Blood and tissue samples were collected from the offspring during the third week postnatal, and the malondialdehyde (MDA) and total antioxidant and oxidant status (TAS, TOS, and OSI) levels were determined. A significant increase in female offspring was observed in the groups born to mice fed with BA compared to the control group. Positive development in organ weights was observed in the 250-ppm BA group. The 250-ppm group exhibited a significant increase in TAS compared to the control group, while TOS and MDA levels showed a decrease. Also, the levels of BA groups were found to decrease in both the OSI index serum and organ samples compared to the control group. Thus, the use of 250-ppm BA demonstrated positive effects on female offspring production, organ development, and antioxidant levels.

2024-12-01·Biological Trace Element Research

Genome-Wide Screens Identify Genes Responsible for Intrinsic Boric Acid Resistance in Escherichia coli

Article

作者: Kürkçü, Merve Sezer ; Çöl, Bekir ; Di Bek, Esra

AbstractBoric acid (BA) has antimicrobial properties and is used to combat bacterial infections, including Enterobacteria. However, the molecular mechanisms and cellular responses to BA are still unknown. This genomics study aims to provide new information on the genes and molecular mechanisms related to the antimicrobial effect of BA in Escherichia coli. The Keio collection of E. coli was used to screen 3985 single-gene knockout strains in order to identify mutant strains that were sensitive or hypersensitive to BA at certain concentrations. The mutant strains were exposed to different concentrations of BA ranging from 0 to 120 mM in LB media. Through genome-wide screens, 92 mutants were identified that were relatively sensitive to BA at least at one concentration tested. The related biological processes in the particular cellular system were listed. This study demonstrates that intrinsic BA resistance is the result of various mechanisms acting together. Additionally, we identified eighteen out of ninety-two mutant strains (Delta_aceF, aroK, cheZ, dinJ, galS, garP, glxK, nohA, talB, torR, trmU, trpR, yddE, yfeS, ygaV, ylaC, yoaC, yohN) that exhibited sensitivity using other methods. To increase sensitivity to BA, we constructed double and triple knockout mutants of the selected sensitive mutants. In certain instances, engineered double and triple mutants exhibited significantly amplified effects. Overall, our analysis of these findings offers further understanding of the mechanisms behind BA toxicity and intrinsic resistance in E. coli.

2024-11-01·Biotechnology and Genetic Engineering Reviews

The mechanism of sodium butyrate on the growth of mouse B16 melanoma cells by inhibiting the differentiation of M2-type macrophages and down-regulating the expressions of VEGF and TGF-β

Article

作者: Jin, Jun ; Wang, Xiaobo ; Jia, Zhenhua ; Wang, Wei

Melanoma is a highly malignant cancer with a high differentiation potential and metastatic capacity. Sodium butyrate, known for its anti-cancer activity, is used in various types of solid tumors. This study aimed to investigate the effects of sodium butyrate on B16 melanoma cells using in vitro and in vivo mouse models. The study utilized MTT assay, flow cytometry, and immunoblot analysis. Mice were treated with normal saline (control) or 1 mM, 2 mM, 3 mM, or 5 mM sodium butyrate. Results showed that cell viabilities were significantly reduced in 2 mM, 3 mM, and 5 mM sodium butyrate groups after 24 to 48 hours (p < 0.01 for all). Moreover, sodium butyrate exhibited a tumor suppression effect that was time-dependent and lasted for 30 days (p < 0.01 for all). A significant tumor suppression effect was observed in the case of 5 mM sodium butyrate after 30 days (p < 0.001 for all). As compared to control (no sodium butyrate), tumor-associated macrophages were decreased in 2 mM, 3 mM, and 5 mM sodium butyrate groups (<0.01 for all). The maximum reduction was observed in 5 mM sodium butyrate groups. Sodium borate decreased the release of interleukin-10, vascular endothelial growth factor, transforming growth factor beta, and β-actin (<0.01 for all). A significant reduction was observed in the case of 5 mM concentration. Overall, these findings suggest that sodium butyrate is effective in the treatment of melanoma and may offer a promising new avenue for melanoma therapy.

项与硼酸相关的新闻（医药）

2024-07-25

·药融圈

投资12亿！珠海联邦制药高栏港原料药项目

▲8月15-16日苏州2024生物医药创新者峰会扫码报名注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需得到授权。近日，关于珠海联邦制药高栏港原料药项目在相关网站公示。项目基本情况项目名称：珠海联邦制药高栏港原料药项目建设单位：珠海联邦制药股份有限公司建设性质：新建建设地点：珠海市金湾区南水镇石化七路总投资：120000万元行业类别：C2710化学药品原料药制造建设内容有：全厂占地约119709.33m2，建筑面积156728.23m2，预计年产头孢哌酮钠500吨/年，头孢他啶300吨/年，头孢呋辛酯300吨/年，头孢呋辛钠300吨/年，头孢噻肟钠300吨/年，头孢曲松钠800吨/年，舒巴坦钠600吨/年，头孢哌酮钠舒巴坦钠混粉400吨/年，头孢他啶无水碳酸钠混粉300吨/年，他达拉非7.8吨/年，阿维巴坦四丁基铵盐24吨/年，氟硼酸钾（副产品）704吨/年，M（2-巯基苯并噻唑）（副产品）513吨/年，六甲基二硅醚（副产品）166吨/年，并配套建设废液热能综合利用系统。产品方案备注：101车间头孢哌酮钠与头孢他啶不同时生产，申报产量按单种产品全年生产时申报。头孢哌酮钠舒巴坦钠、头孢他啶无水碳酸钠为混粉销售产品，只是一种销售方式，不会增加头孢哌酮钠、舒巴坦钠、头孢他啶的产量。该项目已于2023年11月22日奠基，整个项目建设工期约一年半，预计2025年上半年建成投用。珠海联邦制药股份有限公司在金湾区三灶镇经营已逾25年，年产值近70亿元，是一家集研发、生产、销售为一体的现代化先进制药公司。版权声明：本文转自原料药情报局，如不希望被转载的媒体或个人可与我们联系，我们将立即删除 8月15日苏州国际博览中心C馆C101FDA对新兴医疗产品的监管联合主办：FDA专家协会会议日程 09:00-09:05 致辞李宁｜君实生物，副董事长 09:05-09:20 新兴医疗产品的概述杜新｜埃格林医药，联合创始人&CEO 09:20-09:45 新兴医疗产品的发展趋势和监管挑战陆金华｜星尘生物，CSO 09:45-10:10 CGT 产品临床试验的注意要点李长青｜埃格林医药，联合创始人&CMO 10:10-10:35 CGT产品的临床药理学考量杨劲｜中国药科大学，教授 10:35-11:00 CGT产品的cGMP合规考量孙志刚｜绿叶制药集团，高级副总裁 11:00-12:00 小组讨论：新兴医疗产品的国际化杜涛、王亚平、胡育志，毕吕存，张明东，王幼民 12:00-13:30 午餐 13:30-14:00 小核酸药物的开发与监管考量杨永胜｜海昶生物，高级副总裁&核酸创新研究院院长 14:00-14:30 FDA对溶瘤病毒产品的的监管张静｜杰科生物，CMO 14:30-15:00 首个DMD基因疗法的FDA审评审批争议-案例研究王亚宁｜瑞宁康生物医药，创始人&CEO 15:00-15:30 美国食品药品监督管理局在药品研发中使用人工智能和机器学习的监管概况韩晓梅｜E7 CAPITAL创始人&CEO 15:30-16:00 人工智能/机器学习创新医疗器械监管策略胡云富｜泛生子，首席医疗官 16:00-16:45 小组讨论：新兴医疗产品监管的进一步深化陈少羽、门宇欣、何如意、赵孝斌、王玉萍、高光、窦金辉, 温弘扫码报名参会【关于药融圈】药融圈PRHub旨在帮助生物医药科技型企业进行品牌推广及商务拓展服务，针对客户的真实需求制定系统化解决方案，通过“翻译-降维-场景化”将客户的品牌信息以直白易懂的方式被公众知悉，同时在流量渠道覆盖100万+垂直用户基础上实现合作目的，帮助合作伙伴完成从品牌开始到商务为终的闭环营销服务。我们已经完成了数十场线下1000人规模的生物医药研发类会议，涵盖小分子新药，大分子新药，改良型新药，BD跨境交易等多个领域，服务了百余家上市/独角兽/生物技术/制药企业。

核酸药物高管变更

2024-04-30

·药渡

制药巨头Merck解决又一挑战性Suzuki偶联

Suzuki反应在日常科研和药物开发过程中发挥着重要的角色，是构建碳碳键的利器。然而，杂环邻位硼酸酯的Suzuki偶联反应一直以来都是个挑战，可能的原因主要是催化循环中转金属速度比较慢，还有就是这类硼酸酯不稳定，容易脱硼分解。前一段时间，我们报道了日本化学家攻克2-吡啶硼酯稳定性难题的推文（Chem. Commun., 2018, 54, 9290-9293 ），受到了广大读者的强烈反响，该篇文章报道一类新型双硼试剂(pin)B–B(aam)，在钯催化条件下可构建一系列芳基硼化物，关键是可用于构建稳定的吡啶-2-硼酸衍生物。然而，在现实工作中，我们发现这个方法仍然存在一些缺陷，比如有的硼试剂无法制备出来。小编最近在浏览文献时（DOI: 10.1021/ol802556f），偶然发现一篇以前的文章，Merck科学家报道的溴代芳烃与吡啶-2-硼酸衍生物的Suzuki偶联反应，非常具有实用意义，只需要在反应体系中添加廉价的氯化亚铜，就可高效实现挑战性杂环邻位硼酸酯的Suzuki偶联。而不加铜盐，转化率很低，甚至为0。图片来源：OL最近检索文献时，发现两年后，同样来自Merck的科学家解决了氯代芳烃与吡啶-2-硼酸衍生物的Suzuki偶联反应，工作发表在Tetrahedron Letters 上（DOI:10.1016/j.tetlet.2011.07.088）。为什么会有这个研究，是因为溴代芳烃的反应催化体系[Pd(OAc)2/dppf/CuCl]不适用于氯代芳烃。从下表可以看出，dppf作为配体，产率只有5%。作者随后筛选了一系列常见的配体，像S-Phos，X-Phos，Brett-phos等等，以及不同的碱，硼酸酯的当量等等参数，最终发现S-Phos是最佳配体。图片来源：TL作者拓展众多苯环系列，吡咯硼酸酯等硼酸酯，产率最高可达到99%。同时，我们截取了挑战性的吡啶-2-硼酸酯的偶联，如下图所示，铜盐对反应的影响非常明显。不加铜盐，产率是0，而加了铜盐，产率可以达到73%。除了吡啶硼酸酯，吡嗪硼酸酯也能较好地参与反应，产率达到了60%。图片来源：TL大家在实际工作中，遇到氯代芳烃参与的Suzuki反应，可以优先尝试S-Phos这个配体，效果还是不错的。如果硼酸酯是杂环硼酸酯，反应不理想，可以加一点氯化亚铜。有机合成路线做一个有用有料有情怀的公众号很赞的分享↓↓↓

2024-02-01

·BioSpace

FDA Issues Reminder of Non-Substitution of PEDMARK® (sodium thiosulfate injection) for Pediatric Patients Receiving Cisplatin

RESEARCH TRIANGLE PARK, N.C., Feb. 01, 2024 (GLOBE NEWSWIRE) -- Fennec Pharmaceuticals Inc. (NASDAQ: FENC; TSX: FRX), a commercial stage specialty pharmaceutical company, today announced that the U.S. Food and Drug Administration (FDA) has issued a public reminder to healthcare providers that PEDMARK (sodium thiosulfate injection) is not substitutable with other sodium thiosulfate products as explicitly directed in its prescribing label. PEDMARK is the first and only FDA approved therapy indicated to reduce the risk of ototoxicity (e.g., permanent hearing loss) associated with cisplatin in pediatric patients 1 month of age and older with localized, non-metastatic solid tumors. The FDA stated in the public communication that it is aware that some providers may be preparing other sodium thiosulfate (STS) products for patient use in place of PEDMARK, including diluting STS products approved for other uses to match the strength of PEDMARK. The FDA reminded health care providers that as stated in PEDMARK’s prescribing information, PEDMARK is not substitutable with other sodium thiosulfate products. The FDA stated that such substitutions pose potential health risks, including: Potassium chloride exposure which, at high doses, can lead to increased risk of acute cardiac events and other serious adverse reactions. Potassium chloride is not present in PEDMARK. Overexposure to boric acid (a boron compound), can cause health risks including headache, hypothermia, restlessness, weariness, renal injury, dermatitis, alopecia, anorexia and indigestion. Although PEDMARK also contains boric acid, it is at a lower concentration than other STS products. Overexposure to sodium nitrite, which can lead to health risks including methemoglobinemia. Sodium nitrite is co-packaged with sodium thiosulfate as a separate vial in some products; it is not present in PEDMARK. The public communication was issued by the FDA’s Professional Affairs and Stakeholder Engagement Staff within the Center for Drug Evaluation and Research, Office of Communications. The FDA encourages those with any questions to contact FDAOncology@fda.hhs.gov. About Fennec Pharmaceuticals Fennec Pharmaceuticals Inc. is a specialty pharmaceutical company focused on the development and commercialization of PEDMARK® and Pedmarqsi to reduce the risk of platinum-induced ototoxicity in pediatric patients. Further, PEDMARK received FDA approval in September 2022 and European Commission Marketing Authorization in June 2023 for Pedmarqsi. PEDMARK has received Orphan Drug Exclusivity in the U.S. for seven years of market protection and Pedmarqsi has received Pediatric Use Marketing Authorization in Europe which includes eight years plus two years of data and market protection. Fennec has a license agreement with Oregon Health and Science University (OHSU) for exclusive worldwide license rights to intellectual property directed to sodium thiosulfate and its use for chemoprotection, including the reduction of risk of ototoxicity induced by platinum chemotherapy, in humans. For more information, please visit . Investors: Robert Andrade Chief Financial Officer Fennec Pharmaceuticals Inc. +1 919-246-5299 Corporate and Media: Lindsay Rocco Elixir Health Public Relations +1 862-596-1304 lrocco@elixirhealthpr.com

孤儿药引进/卖出上市批准

100 项与硼酸相关的药物交易

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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
脑瘫	药物发现	印度	Bangalore Medical College & Research Institute	2015-07-31
自然流产	药物发现	加拿大	University of British Columbia	2014-04-30
念珠菌病	药物发现	加拿大	University of British Columbia	2014-04-30
囊肿	药物发现	加拿大	University of British Columbia	2014-04-30
子宫内膜炎	药物发现	加拿大	University of British Columbia	2014-04-30
淋病	药物发现	加拿大	University of British Columbia	2014-04-30
继发感染	药物发现	加拿大	University of British Columbia	2014-04-30
手术伤口感染	药物发现	加拿大	University of British Columbia	2014-04-30
子宫颈发育不良	药物发现	加拿大	University of British Columbia	2014-04-30
细菌性阴道炎	药物发现	加拿大	University of British Columbia	2014-04-01