Bazedoxifene, a selective estrogen receptor modulator is thought to have effective anti-tumoral properties for pancreatic cancer via IL-6 pathway (GP130/STAT3) inhibition.
The objective is to measure IL-6 (GP130/STAT3)-pathway modification on metastasis biopsy of patients with metastatic pancreatic adenocarcinoma before and after treatment with bazedoxifene in addition to chemotherapy.
This study is a single-center, prospective, nonrandomized trial.

开始日期2022-02-01

申办/合作机构

Hopital Fribourgeois

EUCTR2021-005247-78-CZ

/ Not yet recruiting临床2期

A 2-Part, Open-label, Non-randomized (Part A) and Randomized, Double-blinded, Placebo-controlled (Part B) multicentric, international study with adaptive design to evaluate safety and tolerability of bazedoxifene, concentrated solution for nebulization (BAZE-X1) in addition to Standard of Care in hospitalized COVID-19 patients suffering from moderate to severe Pneumonia.

开始日期2022-01-19

申办/合作机构-

NCT04821141

/ Recruiting临床2期IIT

Randomized IIB Study of the Effect of Bazedoxifene Plus Conjugated Estrogens on Breast Imaging and Tissue Biomarkers in Peri or Post-Menopausal Women at Increased Risk for Development of Breast Cancer

Women at risk for development of breast cancer and experiencing vasomotor menopausal symptoms (hot flashes) will be randomized to bazedoxifene (BZA) plus conjugated estrogens (CE) for 6 months versus a wait list control. Two risk factors for development of breast cancer will be studied pre-study and after 6 months: fibroglandular volume (FGV) on mammogram as assessed by Volpara software and proliferation by Ki-67 immunocytochemistry in benign breast tissue acquired by random periareolar fine needle aspiration (RPFNA). Change in biomarkers will be compared between groups.

开始日期2021-12-14

申办/合作机构

University of Kansas

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100 项与醋酸巴多昔芬相关的临床结果

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100 项与醋酸巴多昔芬相关的转化医学

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100 项与醋酸巴多昔芬相关的专利（医药）

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538

项与醋酸巴多昔芬相关的文献（医药）

2025-12-01·JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Deploying the drug repurposing approach for the identification of selective monoamine oxidase-B inhibitors against neurological disabilities: an in Silico and in vitro approach

Article

作者: Bansal, Nisha ; Babu, M Arockia ; Mohany, Mohamed ; Alam, Prawez ; Fareed, Mohammad ; Al-Rejaie, Salim S ; Singh, Thakur Gurjeet

Monoamine oxidase-B (MAO-B) plays a regulatory role in controlling the activity of monoamine neurotransmitters, especially dopamine. Its overexpression leads to a decreased concentration of dopamine in the brain, converts MPTP to MPP + (a potential toxin for dopaminergic neurons), and increases hydrogen peroxide and ROS levels in gliosis, leading to neurodegeneration. Thus, MAO-B becomes a key target enzyme for neurological disabilities such as PD and AD. In this study, we used drug repurposing to explore the pool of USFDA-approved and Pharmacopeial drugs (3619 drugs) and performed HTVS (high-throughput virtual screening) using both ADME parameters with emphasis on their ability to cross the BBB and considering the prerequisites of a generated pharmacophore model for MAO-B. The fetched 656 ligands were subjected to SP and XP dockings, MMGBSA, and dynamics analysis to identify the top 10 leads with maximum plausibility to interact with MAO-B. The analysis presented Bazedoxifene and Epicatechin as lead compounds with a higher affinity towards MAO-B than MAO-A. The in-silico work was further validated using in vitro biological analysis that includes MAO inhibitory activity, reversibility studies, and intracellular ROS inhibition studies. Epicatechin and bazedoxifene displayed moderate MAO-B inhibitory activities with IC₅₀ values of 11.14 ± 0.53 µM and 13.11 ± 0.21 µM, with more than sixfold and fourfold selectivity over MAO-A, respectively. Thus, this study can open the avenue to the development of Bazedoxifene and Epicatechin as potential pharmacophores for the design and development of selective and reversible MAO-B inhibitors with higher efficacy for the management of neurological disabilities.

2025-09-01·SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

Surface-enhanced Raman spectroscopy facilitates the detection of multiple metabolic modulators

Article

作者: Yang, Tao ; Li, Yuanyuan ; Ma, Yueyue ; Xia, Zhichao ; Zhou, Na ; Luo, Xiaojun ; Shen, Yushi

Metabolic regulators can improve the athletic ability of athletes by regulating body metabolism, but it is not conducive to fair competition, so it is listed as a prohibited substance. At the same time, the State General Administration of Sport ordered major event organizers to test food for food-borne stimulants. Surface-enhanced Raman scattering (SERS) spectroscopy has been widely used because of its excellent sensitivity and strong spectral characteristics. Based on the available information, SERS spectrum data of metabolic regulators in food-related fields were lacking. In this study, we used gold dodecahedron nanoparticles as SERS active substrate and successfully captured the characteristic peaks of 6 metabolic regulatory factors. A low cost and stable SERS detection technique for detecting trimetazidine in milk samples with good recovery rate was proposed. Therefore, this method can not only protect the food safety of large-scale sports events, but also have broad application prospects in the food field.

2025-08-01·MOLECULAR DIVERSITY

Integrating traditional QSAR and read-across-based regression models for predicting potential anti-leishmanial azole compounds

Article

作者: Priya, Ananya ; Sharma, Anupama ; Nandi, Rajat ; Kumar, Diwakar

Leishmaniasis, a neglected tropical disease caused by various Leishmania species, poses a significant global health challenge, especially in resource-limited regions. Visceral Leishmaniasis (VL) stands out among its severe manifestations, and current drug therapies have limitations, necessitating the exploration of new, cost-effective treatments. This study utilized a comprehensive computational workflow, integrating traditional 2D-QSAR, q-RASAR, and molecular docking to identify novel anti-leishmanial compounds, with a focus on Glycyl-tRNA Synthetase (LdGlyRS) as a promising drug target. A feature selection process combining Genetic Function Approximation (GFA)-Lasso with Multiple Linear Regression (MLR) was used to characterize 99 azole compounds across ten structural classes. The baseline MLR model (MOD1), containing seven simple and interpretable 2D features, exhibited robust predictive capabilities, achieving an R²_train value of 0.82 and an R²_test value of 0.87. To further enhance prediction accuracy, three qualified single models (two MLR and one q-RASAR) were used to construct three consensus models (CMs), with CM2 (MAE_test = 0.127) demonstrating significantly higher prediction accuracy for test compounds than the MOD1. Subsequently, Support Vector Regression (SVR) and Boosting yielded 0.88 (R²_train), 0.86 (R²_test), 0.92 (R²_train), and 0.82 (R²_test), respectively. Molecular docking highlighted interactions of potent azoles within the QSAR dataset with critical residues in the LdGlyRS active site (Arg226 and Glu350), emphasizing their inhibitory potential. Furthermore, the pIC50 values of an accurate external set of 2000 azole compounds from the ZINC20 database were simultaneously predicted by CM2 + SVR + Boosting models and docked against the LdGlyRS, which identified Bazedoxifene, Talmetacin, Pyrvinium, Enzastaurin as leading FDA candidates, whereas three novel compounds with the database code ZINC000001153734, ZINC000011934652, and ZINC000009942262 displayed stable docked interactions and favourable ADMET assessments. Subsequently, Molecular Dynamics (MD) simulations for 100 ns were conducted to validate the findings further, offering enhanced insights into the stability and dynamic behaviour of the ligand-protein complexes. The integrated approach of this study underscores the efficacy of 2D-QSAR modelling. It identifies LdGlyRS as a promising leishmaniasis target, offering a robust strategy for discovering and optimizing anti-leishmanial compounds to address the critical need for improved treatments.

项与醋酸巴多昔芬相关的新闻（医药）

2025-06-26

·药事纵横

维生素的隐藏技能：制药辅料界的多面手

辅料是药物制剂中除活性药物以外的其他成分，其添加的目的在于便于制剂的生产、增强制剂稳定性、调节释放以及提高生物利用度等。提起维生素大家首先想到的其是维持人体健康的重要营养元素，但其实在药物制剂中它已作为功能性辅料应用于包括口服、外用、注射等多种剂型中（见表1），本文主要概述了维生素作为辅料在制剂中发挥的作用。1、注射用剂型中的维生素维生素C：在制剂中主要以抗坏血酸、抗坏血酸钠、抗坏血酸棕榈酯形式存在，作用为抗氧剂、pH调节剂。抗坏血酸在奥卡西平肌肉注射混悬液、注射用多西环素、维替泊芬脂质体中作为抗氧剂使用；在一些含有放射性药物的制剂中，抗坏血酸钠和抗坏血酸可防止放射性药物分解，且无需在制剂基质中添加其它的稳定剂或缓冲剂；除作为抗氧剂，维生素C还可作为 pH 调节剂，用于需要非碱性介质的注射用溶液。维生素E：在罗米地辛静脉注射液和氟维司群注射液中，维生素E作为抗氧剂使用。维生素E还可用于静脉给药的脂质体，如免疫缺陷患者使用的抗真菌药两性霉素B脂质体，在此类制剂中维生素E能降低膜流动性，从而改善脂质堆积并减少渗透性，其构成脂质体外壳的一部分，有助于将API封装在脂质体内，提高制剂的稳定性及疗效。有研究表明维生素E还可添加至某些流感疫苗的佐剂中，发挥免疫刺激的协同作用，使得制剂产生更高的抗体应答。维生素B3：烟酰胺作为辅料加入到门冬胰岛素制剂中，可以与锌离子络合抑制，使得六聚体结构松散，其进入体内后解聚速度加快，从而促进制剂吸收。2、固体剂型中的维生素2.1固体制剂维生素C（抗坏血酸）在固体口服制剂中起到稳定剂和抗氧剂的作用，例如在辛伐他汀片剂中，辛伐他汀的共轭双键和羟基易氧化降解，而抗坏血酸的加入可提高其稳定性。此外，维生素C还在多种固体口服药物作为抗氧化剂使用，如治疗2型糖尿病的沙格列汀、治疗银屑病的阿维A酸、十一酸睾酮和治疗骨质疏松的醋酸巴多昔芬等。维生素E（α-生育酚）用于多种口服剂型，以提高API的稳定性、溶解度或分散性。免疫抑制剂西罗莫司和治疗高血压及前列腺增生的多沙唑嗪片剂均含有α-生育酚，以增强 API的稳定性。此外，维生素E衍生物聚乙二醇琥珀酸酯（TPGS）也用于固体口服剂型，例如慢性偏头痛药物阿托吉泮的片剂含有 TPGS作为分散剂，用于治疗丙型肝炎的两种抗病毒药普瑞巴韦和格卡瑞韦的组合制剂也含有TPGS，后者是一种固体口服分散体，TPGS作为增溶剂，可延缓或抑制药物再结晶。某些 B族维生素也被用作固体口服药物的辅料。维生素B1（硫胺素或硫胺素一水合物）被列入乙肝药物恩替卡韦和抗抑郁药氟西汀的辅料清单中，但其具体作用尚不明确；维生素B2（核黄素）用作抗癫痫药奥卡西平和沙丙蝶呤的着色剂；维生素B3（烟酰胺）在固体制剂中用作助溶剂，通过非胶束增溶作用提高疏水性物质的溶解度，多种难溶性双氯芬酸制剂中也含有烟酰胺，推测用于提高API溶解度。2.2半固体制剂维生素E（α-生育酚）及其衍生物TPGS在半固体口服剂型中具有多重功能，α-生育酚作为抗氧化剂添加至半固体制剂的油相中，例如在免疫抑制剂环孢素的软胶囊制剂中，该处方中α-生育酚作为油相成分，用于减轻环孢素诱导的肾毒性；对于高不稳定性脂溶性痤疮药物异维A酸（软明胶胶囊），α-生育酚与丁基羟基茴香醚（BHA）联用比单独使用BHA或BHT更能提高稳定性。TPGS也可提高低渗透性API的生物利用度，例如安普那韦因生物利用度低导致患者需服用大量制剂，而TPGS通过改善其溶解度和渗透性，使剂量降低从而提高患者的依从性。2.3液体制剂维生素C（抗坏血酸及其衍生物）在液体口服剂型中主要发挥三大作用：（1）抗氧化与稳定性调控：作为抗氧化剂稳定药物成分（如利司扑兰、雷帕霉素），防止活性成分氧化分解；（2）提高生物利用度：通过调节胃 pH 值（增加酸度），提高伊曲康唑等药物的吸收效率，尤其适用于胃酸不足的HIV患者；（3）pH 调节与缓冲作用：在口服疫苗中构建碳酸氢盐 - 抗坏血酸缓冲体系，抵御胃部较低的pH对疫苗活性的破坏（如霍乱、布鲁氏菌病疫苗）。3、局部给药剂型中的维生素维生素在局部给药中作为辅料主要发挥以下作用：（1）活性成分与皮肤改善：化妆品和医用局部制剂中添加的维生素既可以作为活性成分改善皮肤状况，也可作为非活性成分发挥防止酸败或皮肤调理作用；（2）提高制剂稳定性：维生素E（α-生育酚及其酯类）防止脂质基质氧化和光降解，例如在维A酸的乳膏中加入维生素 E（α-生育酚）可改善其光稳定性，在卡巴拉汀透皮贴中α- 生育酚的抗氧化特性用于确保卡巴拉汀在透皮贴剂中的稳定性，用于治疗帕金森病的罗替戈汀透皮贴剂含有维生素 C（抗坏血酸棕榈酸酯）和维生素 E（α- 生育酚），其作为抗氧化剂提高产品的稳定性。（3）促吸收：维生素 B5（泛醇）作为辅料或佐剂用于局部制剂，右旋泛醇可改善皮肤水合作用和渗透性，从而促进原料药的经皮吸收。4、维生素作为辅料的注意事项在药物制剂中选择维生素作为辅料，需考虑其在应用条件下的物理化学稳定性，以及药物、辅料与其之间的相互作用。维生素C：通常与碱性溶质、重金属及某些活性成分（如盐酸去氧肾上腺素、马来酸吡咯胺、水杨酰胺、亚硝酸钠、水杨酸钠、水杨酸可可碱、阿替洛尔）不相容；其调节 pH 的特性可能导致与某些 API 不相容，例如青霉素G 的注射溶液与抗坏血酸反应；辅料中的痕量污染物也需考虑，如用作填充剂的蔗糖粉可能含痕量金属，催化抗坏血酸的非酶促褐变。B族维生素：维生素 B1（硫胺素）干燥状态吸湿性强，在高湿环境下长期暴露会转化为水合物，水溶液 pH<5时稳定（除非加热至 140℃），可发生氧化和还原反应；维生素 B2（核黄素）溶液对光和还原剂敏感（尤其在碱性条件下），但耐氧化，酸性溶液中更稳定；维生素 B3（烟酸）除高温外通常稳定；维生素 B6（吡哆醇）对光敏感，与酸形成盐，在中性或碱性溶液中加热易分解；维生素B12（氰钴胺）吸湿性强，水溶液稳定，但可被硫醇还原，高温（>120℃）和极端 pH（<3或> 8）下分解；维生素B7（生物素）的结晶状态对热和空气稳定，但暴露于紫外线、氧化剂、强酸和强碱时不稳定。维生素D：对紫外线、热、空气和矿物酸敏感，重金属离子会加剧敏感性。维生素E：避光避氧时稳定，接触氧气并同时暴露于光、热和金属离子时易氧化，酯化可增强稳定性。维生素E衍生物（如TPGS）可能与API（如四氢大麻酚）反应，导致药物不稳定。从剂量与安全性方面考虑，长期用药需确保维生素辅料总剂量不超过耐受上限，避免毒性风险，另外某些维生素（如维生素B1衍生物、维生素B6）无辅料使用历史，在选择使用时可能被要求按照新辅料进行评估。总体而言，维生素是一类理想的辅料，能够显著提升注射、口服和局部用制剂的安全性和有效性。原文出自：Anne-Cécile V. Bayne, Pessi J , Bird J K ,et al.Vitamins as excipients in pharmaceutical products[J].European Journal of Pharmaceutical Sciences, 2025, 206(000).文章DOI:10.1016/j.ejps.2025.107020.药事纵横投稿须知：稿费已上调，欢迎投稿

放射疗法疫苗

2025-02-06

·化学经纬

书籍分享||新药化学全合成路线手册

内容介绍本书归纳和综述了新药的化学合成路线。覆盖范围为近5年美国FDA批准上市的新分子实体药共109个。针对每一个药物，本书给出了药物简介，药物化学结构信息，产品上市信息，药品专利保护和市场独占权保护信息，化学全合成路线和参考文献等。这些合成路线大多是目前制药工业中正在使用的化学合成工艺，有较高的实用性和学术价值。对参与反应的起始原料、中间体、反应产物都给出了详细的化学结构。每一步化学合成反应都给出了重要的化学试剂、催化剂、所使用的溶剂、合成反应条件及文献出处等。本书的特点是：作者从浩如烟海的科技文献中，精心挑选出最新、最有实用价值的合成方法，汇编成化学合成路线图，内容简洁，深入浅出，逻辑性强，容易理解，以最少的篇幅表达最多的技术信息，可帮助读者很快找到他们需要的药物合成方法及最可靠的原始科学论文。读者对象： 1.任何从事与化学合成、药物合成、精细化工相关专业的科研人员、企业管理人员。 2.有机化学专业、药学专业、生物制药专业等大专院校的高年级学生、研究生、教师及科研人员。 3.从事客户委托的药物原料与药物中间体合成的科研人员、企业管理人员。编辑推荐对于制药企业而言,一个好的药物全合成路线, 可以大大缩短生产周期,简化生产工艺,降低生产成本,节约能源,减少或消除对环境的化学污染与排放。本书为了顺应我国近年来生物制药及医药工业飞速发展的潮流编写的，详细介绍了近五年美国FDA批准上市的所有（109个）新分子实体药的化学全合成路线。这些全合成路线多数是国外制药厂目前正在使用的工艺，其经济效益及社会效益都是极为显著，因此本书既有较高的科学价值又有很大的实用性。作者简介陈清奇，旅美药学家和化学家，担任美国MedKoo生物医药科研公司总裁，同时兼任美国数家生物制药公司的技术顾问，中国国内数个大学的客座教授。研究领域为药物化学，纳米医学体外诊断技术。书籍目录 Abiraterone Acetate（醋酸阿比特龙）001 Aclidinium Bromide（阿克利溴铵）006 Afatinib（阿法替尼）009 Alcaftadine（阿卡他定）014 Alogliptin（阿格列汀）017 Apixaban（阿哌沙班）022 Apremilast（阿普斯特）028 Avanafil（阿伐那非）033 Axitinib（阿西替尼）038 Azilsartan Kamedoxomil（阿齐沙坦酯钾盐）044 Bazedoxifene（巴多昔芬）048 Bedaquiline（贝达喹啉）053 Belinostat（贝利司他）060 Boceprevir（波西普韦）064 Bosutinib（博舒替尼）071 Cabozantinib（卡博替尼）075 Canagliflozin（卡格列净）078 Carfilzomib（卡非佐米）083 Ceftaroline Fosamil（头孢洛林酯）087 Ceftolozane（噻呋特啰嗪）094 Ceritinib（色瑞替尼）098 Clobazam（氯巴占）101 Cobicistat（可比司他）104 Crizotinib（克里唑蒂尼）112 Dabigatran Etexilate Mesylate（甲磺酸达比加群酯）118 Dabrafenib（达拉菲尼）123 Dapagliflozin（达格列净）127 Dasabuvir（达沙布韦）132 Deferiprone（去铁酮）136 Dienogest（地诺孕素）138 Dolutegravir（度鲁特韦）141 Droxidopa（屈昔多巴）145 Efinaconazole（艾氟康唑）149 Eliglustat（依利格鲁司特）152 Elvitegravir（埃替格韦）155 Empagliflozin（依帕列净）161 Enzalutamide（恩杂鲁胺）166 Eribulin Mesylate（甲磺酸艾日布林）168 Eslicarbazepine Acetate（艾利西平醋酸酯）175 Estradiol Valerate（雌二醇戊酸酯）180 Ezogabine（依佐加滨）185 Finafloxacin（非那沙星）193 Fingolimod Hydrochloride（盐酸芬戈莫德）197 Florbetapir F 18（氟比他匹）205 Flutemetamol F 18（富特米他）211 Gabapentin Enacarbil（加巴喷丁恩那卡比）214 Gadobutrol（钆布醇）218 Gadoterate Meglumine（钆特酸葡甲胺）224 Ibrutinib（依鲁替尼）227 Icatibant（艾替班特）232 Idelalisib（艾代拉里斯）234 Indacaterol （茚达特罗）236 Ingenol Mebutate（巨大戟醇甲基丁烯酸酯）240 Ioflupane 123I（碘[123I]氟潘）242 Ivacaftor（依瓦卡特）247 Ledipasvir（雷迪帕韦）250 Linaclotide（利那洛肽）259 Linagliptin（利拉利汀）261 Lomitapide（洛美他派）267 Lorcaserin（氯卡色林）270 Lucinactant（芦西纳坦）274 Luliconazole（卢立康唑）276 Lurasidone（鲁拉西酮）279 Macitentan（马西替坦）283 Miltefosine（米替福新）286 Mipomersen Sodium（米泊美生钠）290 Mirabegron（米拉贝隆）292 Naloxegol（纳罗克格）296 Netupitant（奈妥吡坦）299 Nintedanib（尼达尼布）303 Olaparib（奥拉帕尼）307 Olodaterol（奥达特罗）311 Omacetaxine Mepesuccinate（高三尖杉酯碱）315 Ombitasvir（艾姆伯韦）319 Ospemifene（奥培米芬）323 Paritaprevir（帕瑞它韦）327 Pasireotide（帕瑞肽）331 Peramivir（帕拉米韦）333 Perampanel（吡仑帕奈）337 Pirfenidone（吡非尼酮）343 Pomalidomide（泊马度胺）345 Ponatinib（泊那替尼）351 Regorafenib（瑞戈非尼）355 Rilpivirine（利匹韦林）357 Riociguat（利奥西呱）366 Rivaroxaban（利伐沙班）370 Roflumilast（罗氟司特）378 Ruxolitinib（鲁索替尼）384 Simeprevir（司美匹韦）388 Sofosbuvir（索非布韦）396 Suvorexant（苏沃雷生）401 Tafluprost（他氟前列腺素）405 Tasimelteon（他司美琼）409 Tavaborole（它瓦波罗）413 Tedizolid Phosphate（磷酸特地唑胺）415 Telaprevir（替拉瑞韦）418 Teriflunomide（特立氟胺）426 Ticagrelor（替格瑞洛）430 Tofacitinib（托法替尼）438 Trametinib（曲美替尼）443 Umeclidinium（芜地溴铵）447 Vandetanib（凡德他尼）450 Vemurafenib（威罗菲尼）456 Vilanterol（维兰特罗）460 Vilazodone Hydrochloride（盐酸维拉佐酮）463 Vismodegib（维莫德吉）468 Vorapaxar（沃拉帕沙）470 Vortioxetine（沃替西汀）473 附录1本书使用的期刊名称缩写表477 附录2专利文献代码481 附录3美国药品专利中的用途代码定义484 附录4美国药品市场独占权代码定义530 附录5美国FDA于2010—2014批准上市的药物名单563 英文索引607 中文索引611 CAS登记号索引613 下载方式现在，这份资料分享给大家。小编在公众号设置了自动回复功能，在公众号后台回复关键词：新药全合成 ●书籍分享||有机氧化反应原理与应用 ●书籍分享||有机卤化反应原理及应用 ●推荐合成书籍【有机缩合反应原理与应用】 ●推荐合成书籍【有机环合反应原理与应用】 ●书籍分享||有机还原反应原理与应用 ●ChemDraw使用让你从化学菜鸟变成老鸟 ●干货分享||有机合成: 策略与控制 ●干货分享||有机合成工艺研发-副反应抑制法 ●基础有机化学(邢其毅)第3、4版教材+习题解析 ●ChemDrawV20最新版详细安装图文教程 ●干货分享||核磁共振二维谱 ●书籍分享||全合成中的经典:更多的目标、战略和方法 ●书籍分享||实用药物化学 ●书籍分享||基于模仿创新的小分子药物发明 ●书籍分享||制药工艺开发-目前的化学与工程挑战 ●书籍分享||手性合成:不对称反应及其应用(第5版) ●书籍分享||新药研发案例研究--明星药物如何从实验室走向市场 ●书籍分享||英汉·汉英化学化工词汇 ●书籍分享||有机化学结构与功能（第四版） ●书籍分享||过渡金属有机化学(原著第6版） ●重磅书籍分享||不对称催化基础 ●书籍分享||药物设计学-唐赟

上市批准高管变更

2024-09-10

·drugs

Review Weighs Treatments for Genitourinary Symptoms of Menopause

TUESDAY, Sept. 10, 2024 -- Vaginal estrogen, vaginal dehydroepiandrosterone (DHEA), oral ospemifene, and vaginal moisturizers may be beneficial for some genitourinary symptoms of menopause (GSM), according to a review published online Sept. 10 in the Annals of Internal Medicine . Elisheva R. Danan, M.D., M.P.H., from the University of Minnesota in Minneapolis, and colleagues examined the effectiveness and harms of vaginal estrogen, nonestrogen hormone therapies, and vaginal moisturizers for treatment of GSM in a systematic review of randomized controlled trials (RCTs). A total of 46 RCTs assessing vaginal estrogen, nonestrogen hormones, vaginal moisturizers, or multiple interventions were identified from 11,993 citations. The researchers found that vaginal estrogen may improve vulvovaginal dryness, dyspareunia , the most bothersome symptom, and treatment satisfaction compared with placebo or no treatment. Vaginal DHEA may improve dryness, dyspareunia, and distress, bother, or interference from genitourinary symptoms compared with placebo; oral ospemifene may improve dryness, dyspareunia, and treatment satisfaction; and dryness may also be improved by vaginal moisturizers (all low certainty of evidence [COE]). No benefit or uncertain effects (low and very low COE, respectively) may be provided by vaginal testosterone, systemic DHEA, vaginal oxytocin, and oral raloxifene or bazedoxifene. Reporting was limited by studies of short duration that were insufficiently powered to assess infrequent serious harms. "Future studies would be strengthened by standard definitions of symptoms and uniform diagnostic criteria for GSM, a common set of validated outcome measures and reporting standards, and attention to clinically relevant patient populations and intervention comparisons," the authors write.

临床结果

100 项与醋酸巴多昔芬相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	醋酸巴多昔芬	G03XC02	DB06401

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
绝经期后骨质疏松	欧盟	Pfizer Europe MA EEIG	2009-04-17
绝经期后骨质疏松	冰岛	Pfizer Europe MA EEIG	2009-04-17
绝经期后骨质疏松	列支敦士登	Pfizer Europe MA EEIG	2009-04-17
绝经期后骨质疏松	挪威	Pfizer Europe MA EEIG	2009-04-17

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
子宫内膜增生	临床3期	美国	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	阿根廷	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	澳大利亚	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	智利	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	哥伦比亚	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	丹麦	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	芬兰	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	匈牙利	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	墨西哥	Pfizer Inc.	2009-01-01
子宫内膜增生	临床3期	新西兰	Pfizer Inc.	2009-01-01

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临床结果

适应症

分期

评价

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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


NCT02237079 (BIM, CTgov)	临床4期	葡萄糖耐受不良 \| 肥胖	17	Placebo Oral Tablet	艱膚繭願觸鏇餘夢艱鑰(憲糧憲壓憲壓壓觸簾餘) = 築襯艱窪鏇選觸獵顧窪蓋鑰壓觸窪糧齋齋壓構 (夢淵鬱蓋鹹選膚獵衊選, 鹽願醖獵鏇繭範廠夢廠 ~ 製選鑰觸艱糧醖鹽築遞) 更多	-	2023-06-26
NCT02448771 (Pubmed)	临床2期	HR阳性乳腺癌	36	Bazedoxifene plus Palbociclib	願淵夢遞齋範齋鹹鑰蓋(蓋觸蓋廠膚糧廠遞觸簾) = 獵蓋構蓋襯淵積構獵憲鑰醖艱鏇積壓淵鏇淵鑰 (築衊襯選鬱築築膚簾蓋 ) 更多	积极	2022-10-10
NCT02602704 (Pubmed \| Arthritis Res Ther)	临床4期	类风湿关节炎	114	Bazedoxifene + calcium and vitamin D	範壓憲醖願夢顧膚鬱製(憲繭鏇築齋廠築築醖膚) = 鬱鬱壓艱衊網餘餘窪艱憲積遞餘鹽鹽壓窪醖憲 (簾壓製築簾襯築鑰獵選 )	-	2021-07-02
NCT02602704 (Pubmed \| Arthritis Res Ther)	临床4期	类风湿关节炎	114	Calcium and vitamin D only	範壓憲醖願夢顧膚鬱製(憲繭鏇築齋廠築築醖膚) = 觸齋製積鹽壓醖鬱網壓憲積遞餘鹽鹽壓窪醖憲 (簾壓製築簾襯築鑰獵選, 0.0003 ~ 0.026)	-	2021-07-02
NCT02448771 (CTgov)	临床1/2期	HR阳性乳腺癌 \| 转移性乳腺癌 \| 浸润性乳腺癌	36	Bazedoxifene+Palbociclib	簾選網簾網壓範構淵構 = 壓繭廠網構窪壓淵鑰鏇獵糧襯網遞壓鑰築窪鏇 (簾顧鑰鏇壓醖糧夢艱範, 築願艱膚壓餘餘範蓋鏇 ~ 簾壓鬱壓窪構膚餘願鑰) 更多	-	2021-07-01
PD1-05 (SABCS2019)	临床1/2期	HR阳性乳腺癌 ER+ \| HER2-	36	Bazedoxifene 40mg + Palbociclib 125mg	蓋鹹鹹網鹽製蓋顧構鑰(憲夢獵網蓋顧廠鹹壓範) = 蓋窪醖鏇齋顧鹽壓鹹鏇窪餘窪餘觸鏇範餘顧顧 (壓膚醖鹽衊衊繭窪鏇鹽, 23 ~ 49) 更多	积极	2019-02-15
WCO_IOF_ESCEO2015	临床4期	绝经期后骨质疏松	24	Bazedoxifene 20 mg	簾襯膚襯膚選構獵衊網(淵鬱簾遞鏇觸鏇願願簾) = 艱憲願遞觸獵夢齋積遞鬱獵鹽鹹襯範積艱觸積 (構鹽窪憲願餘鹹膚範衊 )	-	2015-04-17
NCT00808132 (Selective estrogens, Menopause, And Response to Therapy-5, CTgov)	临床3期	子宫内膜增生 \| 绝经期后骨质疏松	1,886	Bazedoxifene (Bazedoxifene 20 mg / Conjugated Estrogens 0.45 mg)	蓋蓋網壓築觸顧簾鑰壓 = 糧憲獵醖遞鹹鑰製餘獵夢積遞膚壓壓鑰糧醖衊 (選夢夢夢壓壓餘壓鹽選, 鹹鬱醖齋繭鏇築遞築蓋 ~ 夢齋製夢繭餘醖繭襯構) 更多	-	2013-12-20
	临床3期	子宫内膜增生 \| 绝经期后骨质疏松	1,886	Bazedoxifene (Bazedoxifene 20 mg / Conjugated Estrogens 0.625 mg)	蓋蓋網壓築觸顧簾鑰壓 = 繭夢鏇壓鬱遞糧齋艱鏇夢積遞膚壓壓鑰糧醖衊 (選夢夢夢壓壓餘壓鹽選, 艱膚鹽願鹽獵構醖壓鹽 ~ 鏇窪餘製築餘餘築積窪) 更多	-	2013-12-20
NCT00205777 (CTgov)	临床3期	骨质疏松性骨折 \| 骨质疏松症	7,609	Bazedoxifene (Bazedoxifene 20 mg (Core+SE I))	繭壓醖製築餘鏇衊選夢 = 積醖遞積壓艱夢鏇選壓憲簾獵襯網衊衊餘鹹淵 (壓繭蓋糧憲窪獵範蓋願, 鏇艱鹽積顧獵憲觸製廠 ~ 鏇鹹築齋顧繭衊淵遞廠) 更多	-	2013-04-10
NCT00205777 (CTgov)	临床3期	骨质疏松性骨折 \| 骨质疏松症	7,609	Bazedoxifene (Bazedoxifene 40 mg (Core))	繭壓醖製築餘鏇衊選夢 = 衊選網醖簾願製鹹鹹餘憲簾獵襯網衊衊餘鹹淵 (壓繭蓋糧憲窪獵範蓋願, 構壓壓築膚憲觸夢醖選 ~ 蓋顧夢夢範夢膚淵選觸) 更多	-	2013-04-10
NCT00238745 (Pubmed \| J Bone Miner Res)	临床2期	绝经期后骨质疏松	429	Bazedoxifene 20 mg	簾網廠鑰遞願壓憲觸鏇(顧鏇廠醖餘夢憲願觸簾) = 鏇選齋積艱壓築網鹹膚鏇齋範網構遞廠窪鏇遞 (網壓網壓艱齋積憲餘選 )	-	2011-03-01
NCT00238745 (Pubmed \| J Bone Miner Res)	临床2期	绝经期后骨质疏松	429	Bazedoxifene 40 mg	簾網廠鑰遞願壓憲觸鏇(顧鏇廠醖餘夢憲願觸簾) = 醖艱繭淵餘衊選構遞齋鏇齋範網構遞廠窪鏇遞 (網壓網壓艱齋積憲餘選 )	-	2011-03-01