A prodrug form of 5-aminolevulinic acid
Hexaminolevulinate is a lipophilic, hexyl ester prodrug form of 5-aminolevulinic acid .1 It produces equivalent protoporphyrin IX (PpIX) induction in WiDr and NHIK 3025 carcinoma cells at concentrations approximately 100-fold lower than 5-aminolevulinic acid. In vivo, hexaminolevulinate penetrates upper skin layers more effectively in pigs and induces higher levels of PpIX fluorescence in nude mice when compared with 5-aminolevulinic acid following topical administration.2 Formulations containing hexaminolevulinate have been used in imaging and photodynamic therapy for a variety of urogenital cancers.
1.Gaullier, J.-M., Berg, K., Peng, Q., et al.Use of 5-aminolevulinic acid esters to improve photodynamic therapy on cells in cultureCancer Res.57(8)1481-1486(1997) 2.Morrow, D.I.J., McCarron, P.A., Woolfson, A.D., et al.Hexyl aminolaevulinate is a more effective topical photosensitiser precursor than methyl aminolaevulinate and 5-aminolaevulinic acids when applied in equimolar dosesJ. Pharm. Sci.99(8)3486-3498(2010)
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