From the Guidelines
Azelaic acid is a naturally occurring dicarboxylic acid that serves as an effective treatment for several skin conditions, particularly acne, rosacea, and hyperpigmentation, with a recommended application of a thin layer to affected areas twice daily after cleansing, as supported by recent studies 1.
Key Points
- Azelaic acid is available in prescription strengths of 15-20% and over-the-counter formulations of 10% or less, typically as creams, gels, or foams.
- It works through multiple mechanisms: antimicrobial properties, reducing inflammation, normalizing skin cell turnover, and inhibiting tyrosinase to help fade dark spots.
- Side effects are generally mild and include temporary stinging, dryness, or redness upon application.
- Azelaic acid is considered safe during pregnancy and doesn't increase sun sensitivity, making it a versatile option for many skin types, as noted in guidelines 1.
Mechanism of Action
Azelaic acid exerts anti-inflammatory activity on the cathelicidin pathway, which is upregulated in rosacea-affected skin, as reported in a study published in 2024 1.
Clinical Evidence
A 12-week, double-blind, randomized, parallel-group, vehicle-controlled study enrolled 664 subjects and found that inflammatory lesions in the actively treated group decreased significantly, with investigators’ rating of marked improvement or complete remission achieved in 51% of patients 1.
Recommendations
Based on the most recent and highest quality study 1, azelaic acid is recommended for the treatment of acne, rosacea, and hyperpigmentation, due to its efficacy and safety profile.
Important Considerations
- Azelaic acid may cause minor local irritation, particularly in the first few weeks of treatment, as noted in a study published in 2024 1.
- It is essential to follow the recommended dosing and application instructions to minimize side effects and maximize efficacy, as outlined in guidelines 1.
From the FDA Drug Label
The exact mechanism of action of azelaic acid is not known. Azelaic acid has been shown to possess antimicrobial activity against Propionibacterium acnes and Staphylococcus epidermidis. A normalization of keratinization leading to an anticomedonal effect of azelaic acid may also contribute to its clinical activity.
Azelaic acid is a topical medication with antimicrobial and anticomedonal properties. Its exact mechanism of action is unknown, but it is believed to inhibit microbial cellular protein synthesis and normalize keratinization, leading to a reduction in microcomedo formation. 2
From the Research
Definition and Properties of Azelaic Acid
- Azelaic acid is a naturally occurring saturated dicarboxylic acid 3, 4, 5, 6, 7
- It has anti-inflammatory, antioxidant, and antimicrobial properties, making it effective against Propionibacterium acne 3, 7
- Azelaic acid is an inhibitor of tyrosinase, mitochondrial respiratory chain enzymes, and DNA synthesis, and it scavenges harmful free radicals and inhibits the production of reactive oxygen species by neutrophils 3
Therapeutic Applications of Azelaic Acid
- Azelaic acid is used in the treatment of various types of acne, including rosacea and acne vulgaris 3, 4, 5, 6, 7
- It is also used to treat hyperpigmentation disorders, such as melasma and post-inflammatory hyperpigmentation 3, 4, 6, 7
- Azelaic acid has anti-proliferative and cytotoxic effects on various cancer cells, making it a potential therapeutic agent for skin cancer 3, 4
Pharmacokinetics and Formulations of Azelaic Acid
- Azelaic acid is available in topical formulations, including gels and creams, with concentrations ranging from 5% to 20% 3, 5, 7
- The use of liposomal technology allows for greater control over the pharmacokinetics and pharmacodynamics of azelaic acid formulations 3
- Topical azelaic acid is well tolerated, with side effects limited to mild and transient local skin irritation 3, 4, 5, 7