Cited by 166Photodynamic Therapy Research StudiesPorphyrin Metabolism and DisordersNanoplatforms for cancer theranostics

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Clinical uses of 5-aminolaevulinic acid in photodynamic treatment and photodetection of cancer: A review

Casas, Adriana·2020·Cancer Letters

DOI 10.1016/j.canlet.2020.06.008

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Abstract

ALA-mediated Photodynamic Therapy (ALA-PDT) is one of the most promising fields in Photodynamic therapy (PDT) research for cancer treatment. 5-aminolaevulinic acid (ALA) is the prodrug of the photosensitiser Protoporphyrin IX (PpIX). After ALA administration, cells generate PpIX through the haem biosynthetic pathway. Although the exact reasons for ALA/PpIX selectivity are unknown, it is believed that due to the special regulation of haem enzymes, PpIX is accumulated in the tumours. Both ALA and its derivative ALA Methyl ester, are mainly used in dermatology. Besides, ALA-PDT has been employed for palliative and even curative treatment of endoscopically accessible tumours. Lung, oesophagus, gastric and bladder carcinomas, and also oral premalignant lesions, gynaecological intraepithelial neoplasias and Barrett's oesophagus are the conditions mostly treated with ALA-PDT. However, due to the limited penetration of ALA and light, non-dermatologic uses of ALA-PDT have not moved beyond phase I clinical trials. On the other hand, ALA-induced PpIX fluorescence is successfully employed for the Photodynamic Diagnosis (PDD) or assistance in cytoreductive surgery (Fluorescence-guided Resection, FGR). ALA has been approved for the FGR of high-grade gliomas and ALA Hexyl ester, for fluorescence cystoscopy in the diagnosis of bladder cancer. ALA-FGR is currently applied in brain, bladder, lung, colon cancers, etc. and ALA-PDD for oral premalignancies, gynaecological intraepithelial lesions and peritoneal metastases, among others. Besides, PDT can be applied concomitantly in the same diagnostic procedure. This review aimed to analyse the state of the art of clinical uses of ALA in the areas of treatment and detection in the non-dermatologic oncology fields.

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Authors: Casas, A.
Affiliations: Consejo Nacional de Investigaciones Científicas y Técnicas (AR)
Corresponding author: Casas, Adriana
ORCID: Casas, Adriana
Venue: Cancer Letters
Publisher: Elsevier BV
Published: 2020-10
Volume: 490
Pages: 165-173
ISSN: 0304-3835 (ISSN-L)
DOI: 10.1016/j.canlet.2020.06.008
OpenAlex: W3034955339
Cited by: 164
References: 95
Citations by year: 2026: 18 · 2025: 24 · 2024: 32 · 2023: 27 · 2022: 28 · 2021: 29 · 2020: 4
FWCI: 3.13
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Cancer Letters (publishedVersion)
PubMed (publishedVersion)
Funders: Consejo Nacional de Investigaciones Científicas y Técnicas
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Photodynamic Therapy Research Studies
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Porphyrin Metabolism and Disorders
Physical Sciences › Engineering › Biomedical Engineering › Nanoplatforms for cancer theranostics
Keywords: 5-aminolevulinic acid, photodynamic therapy, protoporphyrin IX, heme biosynthesis, photodynamic diagnosis, fluorescence-guided resection, fluorescence cystoscopy, oral potentially malignant disorders, Barrett's esophagus, bladder cancer, high-grade glioma, peritoneal carcinomatosis, tumor selectivity
MeSH terms: Aminolevulinic Acid, Animals, Humans, Neoplasms, Photochemotherapy, Photosensitizing Agents

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Clinical uses of 5-aminolaevulinic acid in photodynamic treatment and photodetection of cancer: A review

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