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Mode of Action

As shown in numerous preclinical and clinical studies, azelaic acid displays three pharmacological properties:

• Antikeratinizing effect
  Antikeratinizing effect Azelaic acid has a normalizing effect on the disturbed terminal differentiation of keratinocytes in the follicular infundibulum. When azelaic acid was added to human keratinocytes in culture, it produced a dose-dependent inhibition of DNA and protein synthesis. [1] It thus normalizes the disturbed follicular keratinization that leads to the formation of comedones in acne patients. The reduction in the count of comedones has subsequently been demonstrated in various clinical studies.
• Antimicrobial effect
  Azelaic acid has a significant antibacterial effect on the follicular Propionibacterium acnes and Staphylococcus epidermidis (in vitro). [2] This effect is primarily bactericidal but may in vivo be modified to a bacteriostatic one. Studies have shown that in acne patients two or three months of topical treatment with azelaic acid reduces the intrafollicular microbial colonization by more than 97.7%. [3] Whereas propionibacterium acne bacteria are frequently resistant against topical antibiotics such as erythromycin and/or clindamycin, there are no indications that propionibacterium acne may become resistant against azelaic acid. [3]
  
  In addition it has been shown that azelaic acid is effective in inhibiting the growth of antibiotic resistant p. acne bacteria. [5]
• Anti-inflammatory effect
  In addition to an indirect effect on inflammation by reducing the growth and activity of Propionibacterium acnes, azelaic acid also reveals direct anti-inflammatory activities by reducing the production and release of reactive oxygen species from neutrophils. [4] This direct anti-inflammatory property is considered to be the basis for the clinical effect of azelaic acid in treating rosacea.

For further information see

• Azelaic acid formulation in rosacea
• Azelaic acid formulation in acne

References

1. [1] Mayer-da-Silva A, Gollnick H, Detmar M, Gassmuller J, Parry A, Muller R, Orfanos CE. Effects of azelaic acid on sebaceous gland, sebum excretion rate and keratinization pattern in human skin. An in vivo and in vitro study. Acta Derm Venereol Suppl (Stockh) 1989;143:20-30.
2. [2] Holland KT et al.: The effect of azelaic acid on cutaneous bacteria. J Dermatol Treat 1989;1:17-19.
3. [3] Cunliffe WJ: The Clinical Efficacy of Azelaic Acid in the Treatment of Acne. Rev Contemp Pharmacother 1993;4:433-439.
4. [4] Carmichael AS et al.: Topical azelaic acid in the treatment of rosacea. J Dermatol Treat 1993;4(1):19-24.
5. [5] Farmery MR, Jines CE, Eady EA, Cove JH, Cunliffe WJ: In vitro activity of azelaic acid, benzoyl peroxide and zinc acetate against antibiotic-resistant propionibacteria from acne patients. J Dermatol Treat 1994; 5: 63-65.

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