Azelaic acid. A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders

Drugs. 1991 May;41(5):780-98. doi: 10.2165/00003495-199141050-00007.

Abstract

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.

Publication types

  • Review

MeSH terms

  • Acne Vulgaris / drug therapy*
  • Dermatologic Agents / pharmacokinetics
  • Dermatologic Agents / pharmacology*
  • Dermatologic Agents / therapeutic use
  • Dicarboxylic Acids / pharmacokinetics
  • Dicarboxylic Acids / pharmacology*
  • Dicarboxylic Acids / therapeutic use
  • Humans
  • Pigmentation Disorders / drug therapy*

Substances

  • Dermatologic Agents
  • Dicarboxylic Acids
  • azelaic acid