Azelaic acid: A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentory skin disorders

Adis Drug Information Services, Auckland, New Zealand.
Drugs (Impact Factor: 4.34). 06/1991; 41(5):780-98.
Source: PubMed


Azelaic acid is a naturally occurring saturated dicarboxylic acid which, on topical application (usually as a 20% cream), has been shown to be effective in the treatment of comedonal acne and inflammatory (papulopustular, nodular and nodulocystic) acne, as well as various cutaneous hyperpigmentary disorders characterised by hyperactive/abnormal melanocyte function, including melasma and, possibly, lentigo maligna. In addition, azelaic acid has an antiproliferative and cytotoxic effect on the human malignant melanocyte, and preliminary findings indicate that it may arrest the progression of cutaneous malignant melanoma. The mechanism of this selective cytotoxic action of azelaic acid is unclear, but may possibly be related to its inhibition of mitochondrial oxidoreductase activity and DNA synthesis. In controlled studies, topical azelaic acid demonstrated comparable anti-acne efficacy to topical tretinoin, benzoyl peroxide, erythromycin and oral tetracycline, while in patients with melasma azelaic acid proved at least as effective as topical hydroquinone. On topical application azelaic acid is well tolerated, with adverse effects apparently limited to a generally mild and transient local cutaneous irritation. Thus, topical azelaic acid, employed either as monotherapy or in combination with other treatments, is likely to prove of value in the management of acne and several hyperpigmentary disorders, most notably melasma.

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    • "Tyrosinase 저해물질로 알려진 것에는 ascorbic acid, kojic acid(Lee et al., 2006), hydroquinone(Fitton and Goa, 1991; Parvez et al., 2006), benzoic acid, retinoid, arbutin(Maeda and Fukuda, 1996) 등이 있는데, 특히 kojic acid와 arbutin *Corresponding author: Sang-Dong Lim, Korea Food Research Institute, Seongnam 463-746, Korea. Tel: 82-31-780-9082, Fax: 82-31-780-9160, E-mail: "
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    ABSTRACT: The melanin pigment in human skin is a major defense mechanism against ultraviolet light to the skin, but darken skin color. Tyrosinase is mainly responsible for melanin biosynthesis (melanogenesis) in animals and enzymatic browning (melanosis) in plants. The purpose of this study was to optimize the fermented milk process for the melanin formation inhibition by using Lactobacillus plantarum M23 with tyrosinase inhibitory activity. We used 4-factor-3-level central composite design combining with response surface methodology. Yeast extract concentration (%, ), addition of grape (%, ), incubation temperature (, ) and incubation time (h, ) was used as an independent factor, on the other hand, pH (pH, ), overall palatability (score, ) and tyrosinase inhibitory activity (%, ) was used as a dependant factor. Based on the optimization for the highest tyrosinase inhibitory activity with pH 4.4, the expected data of pH, palatability and tyrosinase inhibitory activity with 14.8 h incubation at by the addition of 0.127% of yeast extract, 2.95% of grape was 4.42, 7.06 and 86.65%, but the real data was 4.35, 6.86 and 84.05%, respectively. Based on the previous results, fermented milk using Lactobacillus plantarum M23 with the tyrosinase inhibitory activity could contribute for the whitening and antiaging of human skin.
    Preview · Article · Oct 2012 · Hangug chugsan sigpum haghoeji = Korean journal for food science of animal resources
    • "Azelaic acid causes inhibition of DNA synthesis and mitochondrial enzymes, thereby inducing direct cytotoxic effects on melanocytes. Moreover, it acts selectively on hyperactive and abnormal melanocytes, thus neither leukoderma nor exogenous oochronosis are associated with its use.[12] In the instant study, the improvement in melasma with twice daily application of azelaic acid 20% cream as measured by mean MASI was statistically significant both during and at the end of treatment. "
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    ABSTRACT: Melasma is an acquired symmetric hypermelanosis characterised by irregular light to gray-brown macules on sun-exposed skin with a predilection for the cheeks, forehead, upper lip, nose and chin. The management of melasma is challenging and requires meticulous use of available therapeutic options. To compare the therapeutic efficacy of low-fluence Q-switched Nd: YAG laser (QSNYL) with topical 20% azelaic acid cream and their combination in melasma in three study groups of 20 patients each. Sixty Indian patients diagnosed as melasma were included. These patients were randomly divided in three groups (group A = 20 patients of melasma treated with low-fluence QSNYL at weekly intervals, group B = 20 patients of melasma treated with twice daily application of 20% azelaic acid cream and group C = 20 patients of melasma treated with combination of both). Study period was of 12 weeks each. Response to treatment was assessed using melasma area and severity index score. The statistical analysis was done using Chi-square test, paired and unpaired student t-test. Significant improvement was recorded in all the three groups. The improvement was statistically highly significant in Group C as compared to group A (P < 0.001) and group B (P < 0.001). This study shows the efficacy of low-fluence QSNYL, topical 20% azelaic acid cream and their combination in melasma. The combination of low-fluence QSNYL and topical 20% azelaic acid cream yields better results as compared to low-fluence QSNYL and azelaic acid alone.
    No preview · Article · Oct 2012 · Journal of Cutaneous and Aesthetic Surgery
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    • "따라서, tyrosinase 저해활성 실험은 미백물질 screening 단계에서 필수적이다[Lee 등, 1999]. Tyrosinase 저해물질로 알 려진 것에는 ascorbic acid, kojic acid [Lee 등, 2006], hydroquinone [Fitton 등, 1991; Parvez 등, 2006], benzoic acid, retinoids, arbutin [Maeda와 Fukuda, 1996] 등이 있는데, 특히 kojic acid와 arbutin은 강한 미백효과를 가지고 있으나 제 품 안전성 및 경제성 등의 문제로 사용에 어려움이 있다 [Imokawa와 Mishima, 1982; Ando 등, 1993; Masuda 등, 1996]. "
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    ABSTRACT: To develop a new natural whitening agent, we investigated the tyrosinase inhibitory effects of Persicaria tinctoria Flower extracts (PTFE). PTFE showed inhibitory activity on mushroom tyrosinase with the values of . We purified two active compounds from PTFE by LH-20 column chromatography and prep-high performance liquid chromatography (HPLC) and identified as quercetin-3-O-rhamnoside (Q3R) and myricetin-3-O-rhamnoside (M3R) by nuclear magnetic resonance (NMR) and liquid chromatography-mass spectrometry (LC-MS) analysis. Q3R and M3R showed tyrosinase inhibitory activities with the values of and , respectively. These results suggest that PTFE and its active compounds reduced melanin formation by the inhibition of tyrosinase activity. Thus, P. tinctoria flower extracts may be a candidate for cosmetic use.
    Preview · Article · Mar 2011 · Journal of Applied Biological Chemistry
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