Azelaic acid is a naturally occurring saturated dicarboxylic acid found in cereal grains. Chemically, azelaic acid is a 1,7-heptanedicarboxylic acid, with the molecular formula C9 H16 O4, a molecular weight of 188.22, and the structural formula:

Azelaic acid was first developed for dermatologic use in the treatment of hyperpigmentation disorders, since the drug was shown in vitro to be a competitive inhibitor of tyrosinase, the key enzyme for melanogenesis. [1]

Coincidentally, it was observed that patients with melasma and coexisting acne exhibited an improvement in both their acne and pigmentation disorder during topical treatment with azelaic acid. This led to subsequent clinical studies as to the usefulness of azelaic acid in the treatment of acne and rosacea.

In 1989, azelaic acid was approved in certain countries for the topical treatment of acne vulgaris.

References

[1] Nazarro-Porro M et al.: Effects of dicarboxylic acids on lentigo maligna. J Invest Dermatol 1979;72:296-305.