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Molecules 2011, 16(5), 4140-4164; doi:10.3390/molecules16054140
Review

Aminolevulinic Acid (ALA) as a Prodrug in Photodynamic Therapy of Cancer

1, 1, 1, 1, 1, 1, 1 and 1,2,*
Received: 3 February 2011 / Accepted: 3 May 2011 / Published: 19 May 2011
(This article belongs to the collection Prodrugs)
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Abstract

Aminolevulinic acid (ALA) is an endogenous metabolite normally formed in the mitochondria from succinyl-CoA and glycine. Conjugation of eight ALA molecules yields protoporphyrin IX (PpIX) and finally leads to formation of heme. Conversion of PpIX to its downstream substrates requires the activity of a rate-limiting enzyme ferrochelatase. When ALA is administered externally the abundantly produced PpIX cannot be quickly converted to its final product - heme by ferrochelatase and therefore accumulates within cells. Since PpIX is a potent photosensitizer this metabolic pathway can be exploited in photodynamic therapy (PDT). This is an already approved therapeutic strategy making ALA one of the most successful prodrugs used in cancer treatment.
Keywords: 5-aminolevulinic acid; photodynamic therapy; cancer; laser; singlet oxygen 5-aminolevulinic acid; photodynamic therapy; cancer; laser; singlet oxygen
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Wachowska, M.; Muchowicz, A.; Firczuk, M.; Gabrysiak, M.; Winiarska, M.; Wańczyk, M.; Bojarczuk, K.; Golab, J. Aminolevulinic Acid (ALA) as a Prodrug in Photodynamic Therapy of Cancer. Molecules 2011, 16, 4140-4164.

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