原黄素(Proflavine) - 药物靶点：DNA_在研适应症：口腔肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

2,8-Diaminoacridine、Proflavine hemisulfate

靶点

DNA

作用机制

DNA嵌入剂

治疗领域

肿瘤口颌疾病

在研适应症

口腔肿瘤

非在研适应症

食管腺癌巴雷特食管恶性上皮肿瘤+ [13]

原研机构-

在研机构

National Cancer Institute

非在研机构

Icahn School of Medicine at Mount Sinai

National Institutes of Health

Baylor College of Medicine

最高研发阶段早期临床1期

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

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结构

分子式C13H13N3O4S

InChIKeyWSFHCKWLECYVBS-UHFFFAOYSA-N

CAS号553-30-0

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关联

11

项与原黄素相关的临床试验

NCT05396781 / Completed临床2期IIT

Acceptability and Performance of a Mobile Optical Biopsy Technology for Gastrointestinal Cancer Screening: A Clinical Study in Brazil

The investigators have a current trial in China and the US which provides significant support for the safety, cost-effectiveness, accuracy and efficiency of a high resolution microendoscope (HRME)-guided approach in the hands of experienced clinicians. To improve functionality, portability and broader use of this device by non-experts, the investigators recently developed a prototype marHRME platform with an automated, augmented reality (AR)-interpretation that provides an overlaid endoscopic + micro-endoscopic view, facilitating diagnosis and biopsy targeting.

开始日期2022-01-13

申办/合作机构

Rice University

[+2]

NCT02714439 / Active, not recruiting早期临床1期IIT

Low-Cost Imaging for Cervical Cancer Prevention in the Texas Lower Rio Grande Valley

The purpose of this study is to evaluate a different type of medical equipment called "High-Resolution Microendoscope" (HRME) for the diagnosis of cervical pre-cancerous lesions and cervical cancer. The investigators want to compare patients' clinical findings using the current equipment used in clinic with the clinical findings using new equipment we are testing on this research project. If the new equipment is proven to give comparable findings with current equipment being used, doctors might be able to offer a diagnosis and treat cervical lesions in one visit. It might not be necessary to wait for cervical biopsies to come back before women would receive the indicated treatment. Study subjects are being asked to participate because they have been diagnosed with an abnormal Papanicolaou (Pap) PAP smear, positive human papillomavirus (HPV) test or history of cervical dysplasia and need to have a colposcopic examination to determine the reason for abnormal results and receive treatment.

开始日期2016-10-25

申办/合作机构

University of Texas Medical Branch

[+3]

NCT02206048 / CompletedN/AIIT

Use of High-Resolution Microendoscopy (HRME) in Patients With Adenocarcinoma In-Situ (AIS) of the Cervix

The goal of this clinical research study is to learn if it is possible to get high-resolution microendoscopy (HRME) images of AIS tissue and/or tissue from microinvasive carcinoma right before a biopsy of the cervix. Researchers also want to learn if HRME images can show the difference between cancerous tissue and normal cervical tissue.

开始日期2015-10-02

申办/合作机构

The University of Texas MD Anderson Cancer Center

100 项与原黄素相关的临床结果

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100 项与原黄素相关的转化医学

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100 项与原黄素相关的专利（医药）

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811

项与原黄素相关的文献（医药）

2024-11-01·Photochemistry and Photobiology

Test method for evaluating the photocytotoxic potential of fluorescence imaging products

Article

作者: Frankle, Lucas ; Vig, Shruti ; Huang, Huang‐Chiao ; Pfefer, T. Joshua ; Chen, Yu ; Gaitan, Brandon ; Elespuru, Rosalie

AbstractVarious fluorescence imaging agents are currently under clinical studies. Despite significant benefits, phototoxicity is a barrier to the clinical translation of fluorophores. Current regulatory guidelines on medication‐based phototoxicity focus on skin effects during sun exposure. However, with systemic and local administration of fluorophores and targeted illumination, there is now possibility of photochemical damage to deeper tissues during intraoperative imaging procedures. Hence, independent knowledge regarding phototoxicity is required to facilitate the development of fluorescence imaging products. Previously, we studied a cell‐free assay for initial screening of reactive molecular species generation from fluorophores. The current work addresses a safety test method based on cell viability as an adjunct and a comparator with the cell‐free assay. Our goal is to modify and implement an approach based on the in vitro 3T3 neutral red uptake assay of the Organization for Economic Co‐Operation and Development Test Guideline 432 (OECD TG432) to evaluate the photocytotoxicity of clinically relevant fluorophores. These included indocyanine green (ICG), proflavine, methylene blue (MB), and IRDye800, as well as control photosensitizers, benzoporphyrin derivative (BPD) and rose bengal (RB). We performed measurements at agent concentrations and illumination parameters used for clinic imaging. Our results aligned with prior studies, indicating photocytotoxicity in RB and BPD and an absence of reactivity for ICG and IRDye800. DNA interactive agents, proflavine and MB, exhibited drug/light dose–response curves like photosensitizers. This study provides evidence and insights into practices useful for testing the photochemical safety of fluorescence imaging products.

2024-11-01·Photochemistry and Photobiology

Shades of phototoxicity in fluorescent imaging agents (that are not supposed to be phototoxic)

作者: Greer, Alexander ; Essang, Serah

AbstractThis article is a highlight of the paper by Huang et al. in this issue of Photochemistry and Photobiology. It describes shades of phototoxicity in fluorescent imaging agents that are not intended to be phototoxic. Phototoxicity was assessed using a modified neutral red uptake (NRU) in vitro assay with mean photo‐effects (MPE) for the fluorescent agents IRdye800, indocyanine green (ICG), proflavine, and methylene blue (MB), with comparisons to known phototoxic agents benzoporphyrin derivative (BPD) and rose bengal (RB). The experimental conditions were aimed to mimic clinical settings, using not only visible light, but also near‐infrared light for insight to photosafety and deep tissue damage. Molecular mechanisms underlying the phototoxicities were not sought, but IRdye800 and ICG were mainly deemed to be safe, whereas proflavine and MB would require precautions since phototoxicity can overshadow their utility as fluorescent imaging agents.

2024-05-21·Journal of Biomedical Optics

Use of topical methylene blue to image nuclear morphometry with a low-cost scanning darkfield microendoscope

Article

作者: Carns, Jennifer ; Richards-Kortum, Rebecca R. ; Anandasabapathy, Sharmila ; Hou, Huayu ; Schwarz, Richard A. ; Gillenwater, Ann M.

SignificanceFiber-optic microendoscopy is a promising approach to noninvasively visualize epithelial nuclear morphometry for early cancer and precancer detection. However, the broader clinical application of this approach is limited by a lack of topical contrast agents available for in vivo use.AimThe aim of this study was to evaluate the ability to image nuclear morphometry in vivo with a novel fiber-optic microendoscope used together with topical application of methylene blue (MB), a dye with FDA approval for use in chromoendoscopy in the gastrointestinal tract.ApproachThe low-cost, high-resolution microendoscope implements scanning darkfield imaging without complex optomechanical components by leveraging programmable illumination and the rolling shutter of the image sensor. We validate the integration of our system and MB staining for visualizing epithelial cell nuclei by performing ex vivo imaging on fresh animal specimens and in vivo imaging on healthy volunteers.ResultsThe results indicate that scanning darkfield imaging significantly reduces specular reflection and resolves epithelial nuclei with enhanced image contrast and spatial resolution compared to non-scanning widefield imaging. The image quality of darkfield images with MB staining is comparable to that of fluorescence images with proflavine staining.ConclusionsOur approach enables real-time microscopic evaluation of nuclear patterns and has the potential to be a powerful noninvasive tool for early cancer detection.

100 项与原黄素相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	原黄素	-	DB01123

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
幽门螺杆菌感染	临床前	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
肠道疾病	临床前	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
鳞状上皮内病变	临床前	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
胃癌	临床前	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
鳞状上皮内病变	药物发现	美国	Icahn School of Medicine at Mount Sinai	2015-01-31
食管鳞状细胞癌	药物发现	中国	Baylor College of Medicine	2014-01-31
食管鳞状细胞癌	药物发现	美国	Baylor College of Medicine	2014-01-31
食管腺癌	药物发现	美国	Baylor College of Medicine	2012-09-30
巴雷特食管	药物发现	美国	Baylor College of Medicine	2012-09-30
细菌性心内膜炎	药物发现	美国	Baylor College of Medicine	2012-09-30

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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


NCT02206048 (CTgov)	N/A	宫颈原位腺癌	9	High-Resolution Microendoscopy (HRME) Imaging+Proflavine	醖遞壓鏇鹽糧範鬱製廠(壓鬱願構簾鏇繭窪範遞) = 襯簾顧觸網鹽遞遞膚糧繭齋構鑰襯築膚網願衊 (衊繭襯鏇範糧鏇夢鏇製, 壓積齋獵顧窪鬱構獵願 ~ 憲願遞鹹鬱鹹鏇襯艱獵) 更多	-	2022-07-25