Benzyl aminolevulinate(Benzyl aminolevulinate)

概要

基本信息

药物类型

小分子化药

别名

5-ALA benzylester、5-ALA benzylesther、Benzvix

靶点-

作用方式-

作用机制

光敏剂

治疗领域

肿瘤消化系统疾病

在研适应症-

非在研适应症

胃肠道肿瘤

原研机构

Photocure ASA

在研机构-

非在研机构

Photocure ASA

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C12H15NO3

InChIKeyAFFZCQDLQIEQGB-UHFFFAOYSA-N

CAS号163271-21-4

关联

2

项与 Benzyl aminolevulinate 相关的临床试验

NCT02313467

/ CompletedN/AIIT

Topical Application of 1.5% Butenyl ALA Without Light Source Irradiation in the Treatment of Acne: a Double Blinded Randomized Controlled Trial.

In this study, the investigators are going to compare the clinical effect and safety of topical application of 1.5% Butenyl ALA cream formula without light source irradiation in the treatment of acne.

开始日期2014-01-01

申办/合作机构

Seoul National University Hospital

NCT00814528

/ WithdrawnN/AIIT

Photodynamic Therapy Mediated by Topical Application of 5- ALA for the Treatment of Actinic Keratoses

The purpose of this study is to compare the treatment of skin growths called actinic keratoses (AK) with 5-ALA PDT, an FDA-approved treatment, versus treatment with other conventionally used FDA-approved agents such as cryotherapy, Imiquimod, or 5-fluorouracil (5-FU).

开始日期2007-11-01

申办/合作机构

The University of Chicago

100 项与 Benzyl aminolevulinate 相关的临床结果

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100 项与 Benzyl aminolevulinate 相关的转化医学

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100 项与 Benzyl aminolevulinate 相关的专利（医药）

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8

项与 Benzyl aminolevulinate 相关的文献（医药）

2009-12-01·Journal of Dermatological Science2区 · 医学

5-ALA derivative-mediated photoinactivation of Propionibacterium acnes

2区 · 医学

Letter

作者: Robert Gurny ; Norbert Lange ; Marino Andres Campo ; Juro Mikulic ; Nicolas Fotinos ; Jean-Claude Piffaretti ; Maruska Convert

This study quant. determines the capacity of different 5-aminolevulinic acid (5-ALA) derivatives to induce photoactive porphyrins (PAP) formation and subsequently photodynamically inactivate different strains of Propionibacterium acnes.Furthermore, the results were compared to clin. approved compounds such as 5-ALA, Me aminolevulinate (MAL) and hexyl aminolevulinate (HAL) although the latter is currently not approved for dermatol. use.HAL induced only insignificant amounts of porphyrins but the highest PAP formation was observed with benzyl aminolevulinate (BzAL) and DGME at 30 mM.Similar results were obtained with the two clin. strains of P. acnes, E5947 and VA2376.The two moderately liphophilic 5-ALA derivatives, BzAL and DGME, both demonstrated the capacity to induce high PAP formation, efficiently photoinactivate high bacterial fractions, up to 99.99%, and show no dark toxicity at doses up to 30 mM.BzAL and 5-ALA-DGME represent to be potent alternatives to MAL and 5-ALA for the treatment of P. acnes.In the future, their efficiency to target sebaceous glands as well as reduction of the common side effects such as pain, or contact dermatitis should be investigated clin. to further optimize PDT treatment of acne vulgaris.

2006-01-01·Journal of Environmental Pathology, Toxicology and Oncology4区 · 医学

New Derivatives of 5-Aminolevulinic Acid for Photodynamic Therapy: Chemical Synthesis and Porphyrin Production in In Vitro and In Vivo Biological Systems

4区 · 医学

Article

作者: Jo Klaveness ; Aslak Godal ; Qian Peng ; Jahn M. Nesland ; Nils O. Nilsen ; Jon Erik Branden

Photodynamic therapy (PDT) has become a new treatment for several oncological and nononcological disorders. This procedure involves systemic or topical administration of a lesion-localizing photosensitizer or prodrug, followed by irradiation with visible light to cause singlet oxygen-induced damage to the target tissue. 5-aminolevulinic acid (ALA) is an endogenous precursor for several photosensitizing porphyrins formed by heme biosynthesis, and has been studied for PDT with promising results for some superficial diseases of the skin and hollow internal organs. Hydrophilic ALA has a limited ability to penetrate certain biological barriers and has a relatively low selectivity for lesions. In addition, its ability to induce intracellular porphyrins has been shown to be low compared to most esters of ALA. This stimulated a search for lipophilic derivatives of ALA to overcome the shortcomings of ALA. Thirty-two new esters of ALA were prepared and their ability to induce porphyrin formation was assessed in the WiDr human carcinoma cell line in vitro and in the normal skin of Balb/c nude mice in vivo. Branched-chain alkyl esters and substituted benzyl esters were found to be the most efficient porphyrin precursors of the compounds studied.

2004-01-01·Photochemistry and Photobiology3区 · 生物学

Detection of Dysplastic Lesions by Fluorescence in a Model of Chronic Colitis in Rats After Local Application of 5-Aminolevulinic Acid and its Esterified Derivatives ¶

3区 · 生物学

Article

作者: Florian Hausmann ; Jürgen Schölmerich ; Heiko C. Rath ; Ruth Knüchel ; Helmut Messmann ; Petra Rümmele ; Esther Endlicher ; Rene C. Krieg

5-Aminolevulinic acid (ALA) and ALA ester-induced protoporphyrin IX (PPIX) fluorescence are used for photodynamic diagnosis and therapy with promising results. The aim of the present study was to investigate the detection of dysplastic lesions by fluorescence after topical application of ALA and different esterified derivatives in a model of chronic colitis in rats. In female CD rats chronic colitis was induced by oral application of 5% dextrane sulfate sodium. ALA was used at different concentrations (0.072 and 0.036 mol/L). ALA-methylester (m-ALA), ALA-hexylester (h-ALA) and ALA-benzylester (b-ALA) were used at a concentration of 0.003, 0.002 and 0.002 mol/L, respectively. Fluorescence was examined under blue light, and histological findings of fluorescent and nonfluorescent biopsy specimens were recorded. Using ALA at a concentration of 0.072 mol/L, all dysplastic lesions (8/8) showed fluorescence (sensitivity 100%). Specificity was low at 57%. Reducing the concentration to 0.036 mol/L resulted in a sensitivity of only 56% (5/9) with an increase in specificity to 76%. On using h-ALA, sensitivity was 60% (3/5) with a specificity of 51%. Using m-ALA and b-ALA, sensitivity values were 25% and 33%, and values for specificity were 62% and 63%, respectively. Despite a low number of dysplastic lesions, the results of this study indicate that ALA ester-induced PPIX fluorescence has the potential for the detection of premaligant lesions but was not superior to ALA. ALA esters were used in 18- to 36-fold lower concentrations compared with ALA.

100 项与 Benzyl aminolevulinate 相关的药物交易

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