MedKoo product information:

 Aminolevulinic Acid Hydrochloride

Description of aminolevulinic acid: Aminolevulinic Acid is a topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid (ALA) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Levulan photodynamic therapy is a treatment method for certain skin conditions developed by DUSA Pharmaceuticals. The active ingredient is δ-aminolevulinic acid (ALA). U.S. Food and Drug Administration (FDA) approval for actinic keratosis was received in December 1999.

Treatment protocol: A 20% solution of ALA is applied to the lesions, and after a 6 hour wait to allow proper penetration of the skin, the treatment area is irradiated with blue light for 15 minutes. This generates reactive oxygen species in the skin that can lead to cell death. The treated areas are sensitive to light, and patients must protect themselves against bright sunshine for up to 40 hours after treatment. Patients must stop using topical acne medicine and avoid steam rooms, hot showers, and generally protect the skin in every way possible for up to one week after treatment. (source: http://en.wikipedia.org/wiki/Levulan).

Levulan is also prescribed for the treatment of acne but this is an off-label use, which means it is not approved by the FDA. On October 2008 Dusa Pharmaceuticals announced that it was no longer developing Levulan for the treatment of acne after the phase II results failed to show statistically significant results.  (source: http://en.wikipedia.org/wiki/Levulan).

The LEVULAN KERASTICK (aminolevulinic acid) for Topical Solution applicator is a two component system consisting of a plastic tube containing two sealed glass ampules and an applicator tip. One ampule contains 1.5 mL of solution vehicle comprising alcohol USP (ethanol content = 48% v/v), water, laureth-4, isopropyl alcohol, and polyethylene glycol. The other ampule contains 354 mg of ALA HCl as a dry solid. The applicator tube is enclosed in a protective cardboard sleeve and cap. The 20% topical solution is prepared just prior to the time of use by breaking the ampules and mixing the contents by shaking the LEVULAN KERASTICK (aminolevulinic acid) applicator. The term “ALA HCl” refers to unformulated active ingredient, “LEVULAN KERASTICK (aminolevulinic acid) for Topical Solution” refers to the drug product in its unmixed state, “LEVULAN KERASTICK (aminolevulinic acid) Topical Solution” refers to the mixed drug product (in the applicator tube or after application), and “LEVULAN KERASTICK (aminolevulinic acid) ” refers to the applicator only.

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2: Warren CB, Karai LJ, Vidimos A, Maytin EV. Pain associated with aminolevulinic acid-photodynamic therapy of skin disease. J Am Acad Dermatol. 2009 Dec;61(6):1033-43. Review. PubMed PMID: 19925929.

3: Recio ED, Zambrano B, Alonso ML, de Eusebio E, Martín M, Cuevas J, Jaén P. Topical 5-aminolevulinic acid photodynamic therapy for the treatment of unilesional mycosis fungoides: a report of two cases and review of the literature. Int J Dermatol. 2008 Apr;47(4):410-3. Review. PubMed PMID: 18377612.

4: Tonn JC, Stummer W. Fluorescence-guided resection of malignant gliomas using 5-aminolevulinic acid: practical use, risks, and pitfalls. Clin Neurosurg. 2008;55:20-6. Review. PubMed PMID: 19248665.

5: Harvie SE. Aminolevulinic acid and photodynamic combination therapy in the treatment of actinic keratoses: caring for the patient. Dermatol Nurs. 2007 Feb;19(1):31-4, 39. Review. PubMed PMID: 17330552.

6: Gold MH. Aminolevulinic acid photodynamic therapy for hidradenitis suppurativa. Dermatol Clin. 2007 Jan;25(1):67-73. Review. PubMed PMID: 17126743.

7: Richey DF. Aminolevulinic acid photodynamic therapy for sebaceous gland hyperplasia. Dermatol Clin. 2007 Jan;25(1):59-65. Review. PubMed PMID: 17126742.

8: Alexiades-Armenakas M. Aminolevulinic acid photodynamic therapy for actinic keratoses/actinic cheilitis/acne: vascular lasers. Dermatol Clin. 2007 Jan;25(1):25-33. Review. PubMed PMID: 17126739.

9: Blume JE, Oseroff AR. Aminolevulinic acid photodynamic therapy for skin cancers. Dermatol Clin. 2007 Jan;25(1):5-14. Review. PubMed PMID: 17126737.

10: Casas A, Batlle A. Aminolevulinic acid derivatives and liposome delivery as strategies for improving 5-aminolevulinic acid-mediated photodynamic therapy. Curr Med Chem. 2006;13(10):1157-68. Review. PubMed PMID: 16719777.

11: Gold MH. Aminolevulinic acid photodynamic therapy: medical evidence for its expanded use. Expert Rev Med Devices. 2006 May;3(3):357-71. Review. PubMed PMID: 16681457.

12: Fotinos N, Campo MA, Popowycz F, Gurny R, Lange N. 5-Aminolevulinic acid derivatives in photomedicine: Characteristics, application and perspectives. Photochem Photobiol. 2006 Jul-Aug;82(4):994-1015. Review. PubMed PMID: 16542112.

13: Zakhary K, Ellis DA. Applications of aminolevulinic Acid-based photodynamic therapy in cosmetic facial plastic practices. Facial Plast Surg. 2005 May;21(2):110-6. Review. PubMed PMID: 16049896.

14: Hexyl aminolevulinate: 5-ALA hexylester, 5-ALA hexylesther, aminolevulinic acid hexyl ester, hexaminolevulinate, hexyl 5-aminolevulinate, P 1206. Drugs R D. 2005;6(4):235-8. Review. PubMed PMID: 15991884.

15: Donnelly RF, McCarron PA, Woolfson AD. Drug delivery of aminolevulinic acid from topical formulations intended for photodynamic therapy. Photochem Photobiol. 2005 Jul-Aug;81(4):750-67. Review. PubMed PMID: 15790300.

16: Fukuda H, Casas A, Batlle A. Aminolevulinic acid: from its unique biological function to its star role in photodynamic therapy. Int J Biochem Cell Biol. 2005 Feb;37(2):272-6. Review. PubMed PMID: 15474973.

17: Gold MH, Goldman MP. 5-aminolevulinic acid photodynamic therapy: where we have been and where we are going. Dermatol Surg. 2004 Aug;30(8):1077-83; discussion 1083-4. Review. PubMed PMID: 15274696.

18: Itkin A, Gilchrest BA. delta-Aminolevulinic acid and blue light photodynamic therapy for treatment of multiple basal cell carcinomas in two patients with nevoid basal cell carcinoma syndrome. Dermatol Surg. 2004 Jul;30(7):1054-61. Review. PubMed PMID: 15209801.

19: Collaud S, Juzeniene A, Moan J, Lange N. On the selectivity of 5-aminolevulinic acid-induced protoporphyrin IX formation. Curr Med Chem Anticancer Agents. 2004 May;4(3):301-16. Review. PubMed PMID: 15134506.

20: Bissonette R, Bergeron A, Liu Y. Large surface photodynamic therapy with aminolevulinic acid: treatment of actinic keratoses and beyond. J Drugs Dermatol. 2004 Jan-Feb;3(1 Suppl):S26-31. Review. PubMed PMID: 14964758.

21: Gupta AK, Ryder JE. Photodynamic therapy and topical aminolevulinic acid: an overview. Am J Clin Dermatol. 2003;4(10):699-708. Review. PubMed PMID: 14507231.

22: Casas A, Batlle A. Rational design of 5-aminolevulinic acid derivatives aimed at improving photodynamic therapy. Curr Med Chem Anticancer Agents. 2002 Jul;2(4):465-75. Review. PubMed PMID: 12678731.

23: Friesen SA, Hjortland GO, Madsen SJ, Hirschberg H, Engebraten O, Nesland JM, Peng Q. 5-Aminolevulinic acid-based photodynamic detection and therapy of brain tumors (review). Int J Oncol. 2002 Sep;21(3):577-82. Review. PubMed PMID: 12168102.

24: Taylor EL, Brown SB. The advantages of aminolevulinic acid photodynamic therapy in dermatology. J Dermatolog Treat. 2002;13 Suppl 1:S3-11. Review. PubMed PMID: 12060511.

25: Karbownik M, Reiter RJ. Melatonin protects against oxidative stress caused by delta-aminolevulinic acid: implications for cancer reduction. Cancer Invest. 2002;20(2):276-86. Review. PubMed PMID: 11901547.

26: Sasaki K, Watanabe M, Tanaka T, Tanaka T. Biosynthesis, biotechnological production and applications of 5-aminolevulinic acid. Appl Microbiol Biotechnol. 2002 Jan;58(1):23-9. Review. PubMed PMID: 11831472.

27: Lang K, Lehmann P, Bolsen K, Ruzicka T, Fritsch C. Aminolevulinic acid: pharmacological profile and clinical indication. Expert Opin Investig Drugs. 2001 Jun;10(6):1139-56. Review. PubMed PMID: 11772241.

28: Cappugi P, Campolmi P, Mavilia L, Prignano F, Rossi R. Topical 5-aminolevulinic acid and photodynamic therapy in dermatology: a minireview. J Chemother. 2001 Oct;13(5):494-502. Review. PubMed PMID: 11760213.

29: Ormrod D, Jarvis B. Topical aminolevulinic acid HCl photodynamic therapy. Am J Clin Dermatol. 2000 Mar-Apr;1(2):133-9; discussion 140-1. Review. PubMed PMID: 11702313.

30: Nishikawa S, Murooka Y. 5-Aminolevulinic acid: production by fermentation, and agricultural and biomedical applications. Biotechnol Genet Eng Rev. 2001;18:149-70. Review. PubMed PMID: 11530687.

31: Kelada SN, Shelton E, Kaufmann RB, Khoury MJ. Delta-aminolevulinic acid dehydratase genotype and lead toxicity: a HuGE review. Am J Epidemiol. 2001 Jul 1;154(1):1-13. Review. PubMed PMID: 11427399.

32: Messmann H. 5-Aminolevulinic acid-induced protoporphyrin IX for the detection of gastrointestinal dysplasia. Gastrointest Endosc Clin N Am. 2000 Jul;10(3):497-512. Review. PubMed PMID: 10899260.

33: Barr H. Barrett's esophagus: treatment with 5-aminolevulinic acid photodynamic therapy. Gastrointest Endosc Clin N Am. 2000 Jul;10(3):421-37. Review. PubMed PMID: 10899256.

34: Fuchs J, Weber S, Kaufmann R. Genotoxic potential of porphyrin type photosensitizers with particular emphasis on 5-aminolevulinic acid: implications for clinical photodynamic therapy. Free Radic Biol Med. 2000 Feb 15;28(4):537-48. Review. PubMed PMID: 10719235.

35: Fink-Puches R, Wolf P, Kerl H. Photodynamic therapy of superficial basal cell carcinoma by instillation of aminolevulinic acid and irradiation with visible light. Arch Dermatol. 1997 Dec;133(12):1494-5. Review. PubMed PMID: 9420532.

36: Peng Q, Warloe T, Berg K, Moan J, Kongshaug M, Giercksky KE, Nesland JM. 5-Aminolevulinic acid-based photodynamic therapy. Clinical research and future challenges. Cancer. 1997 Jun 15;79(12):2282-308. Review. PubMed PMID: 9191516.

37: Peng Q, Berg K, Moan J, Kongshaug M, Nesland JM. 5-Aminolevulinic acid-based photodynamic therapy: principles and experimental research. Photochem Photobiol. 1997 Feb;65(2):235-51. Review. PubMed PMID: 9066303.

38: Kennedy JC, Marcus SL, Pottier RH. Photodynamic therapy (PDT) and photodiagnosis (PD) using endogenous photosensitization induced by 5-aminolevulinic acid (ALA): mechanisms and clinical results. J Clin Laser Med Surg. 1996 Oct;14(5):289-304. Review. PubMed PMID: 9612195.

39: Bechara EJ. Oxidative stress in acute intermittent porphyria and lead poisoning may be triggered by 5-aminolevulinic acid. Braz J Med Biol Res. 1996 Jul;29(7):841-51. Review. PubMed PMID: 9070373.

40: Marcus SL, Sobel RS, Golub AL, Carroll RL, Lundahl S, Shulman DG. Photodynamic therapy (PDT) and photodiagnosis (PD) using endogenous photosensitization induced by 5-aminolevulinic acid (ALA): current clinical and development status. J Clin Laser Med Surg. 1996 Apr;14(2):59-66. Review. PubMed PMID: 9484077.

41: Schoenfeld N, Mamet R, Leibovici L, Lanir A. Alcohol-induced changes in urinary aminolevulinic acid and porphyrins: unrelated to liver disease. Alcohol. 1996 Jan-Feb;13(1):59-63. Review. PubMed PMID: 8837936.

42: Hermes-Lima M. How do Ca2+ and 5-aminolevulinic acid-derived oxyradicals promote injury to isolated mitochondria? Free Radic Biol Med. 1995 Sep;19(3):381-90. Review. PubMed PMID: 7557553.

43: O'Neill GP, Söll D. Transfer RNA and the formation of the heme and chlorophyll precursor, 5-aminolevulinic acid. Biofactors. 1990 Oct;2(4):227-35. Review. PubMed PMID: 2282139.

44: Bernard A, Lauwerys R. Metal-induced alterations of delta-aminolevulinic acid dehydratase. Ann N Y Acad Sci. 1987;514:41-7. Review. PubMed PMID: 3327436.