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Topical Aminolevulinic Acid HCl Photodynamic Therapy

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Abstract

▴ Photodynamic therapy (PDT) is the treatment of tumors or dysplasic tissue with drugs that produce cytotoxic metabolites when exposed to light.

▴ Aminolevulinic acid HCl (5-aminolevulinic acid HCl; ALA) is a prodrug that is metabolized intracellularly to form the photosensitizing molecule protoporphyrin (PpIX). When PpIX is activated by light, cytotoxic reactive oxygen species and free radicals are generated.

▴ ALA can diffuse through skin and preferentially localizes in tumors and dysplasic tissue; subsequent exposure of PpIX-loaded tumor cells to light can destroy the tumor.

▴ After application of a 20% solution of ALA to actinic keratosis lesions of the head, PpIX (as measured by skin fluorescence) peaked 11 hours after treatment and the mean clearance half-life was 30 hours.

▴ In phase II trials 10 J/cm2 of blue light (wavelength = 417nm) delivered at 10 mW/cm2 for 1000 seconds was found to provide maximal therapeutic effect on lesions of the head after treatment with 20% ALA.

▴ In phase III trials of ALA PDT in 241 patients with lesions of the head 72% of patients had a complete response to treatment at 12 weeks versus 20% of those treated with vehicle and light alone. Some of these patients had been re-treated at 8 weeks.

▴ In these trials 12% of ALA-treated patients and 37.5% of those receiving vehicle whose lesions had cleared at 8 weeks had relapsed at 12 weeks. When the total number of lesions were considered the recurrence rate was 5 and 27.9% for ALA- and vehicle-treated lesions, respectively.

▴ All patients reported some degree of burning or stinging during PDT but this usually subsided after irradiation was completed and was rarely treatment-limiting. Localized erythema and edema were also common. No other significant adverse effects were noted and treatment was generally well tolerated.

▴ A well designed dermal applicator ensured perilesional skin was spared collateral damage.

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  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Douglas Ormrod & Blair Jarvis

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  1. Douglas Ormrod
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  2. Blair Jarvis
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Correspondence to Douglas Ormrod.

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Ormrod, D., Jarvis, B. Topical Aminolevulinic Acid HCl Photodynamic Therapy. Am J Clin Dermatol 1, 133–139 (2000). https://doi.org/10.2165/00128071-200001020-00009

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