Synthetic GMP azelaic acid for derm treatments OR Synthetic GMP azelaic acid speeds regulatory approval for dermatology therapeutics

PCI Synthesis has developed and commercialized the world’s first synthetic form of medical grade azelaic acid, which is in the class of dicarboxylic acid medications. These are a group of interesting organic compounds, some of which can act as both a food and a medicine.

Medicinal uses of dicarboxylic acids

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There are several dicarboxylic acids. In higher plants, dicarboxylic acids (DA) are components of the natural protective polymers cutin and suberin, which serve as a support biopolyester that waterproofs the leaves and fruits, regulating the flow of nutrients and minimizing the harmful impact of pathogens. Found to be safe and effective in animals and humans, dicarboxylic acids have been proposed in treatment of type 2 diabetes, where they have been found to improve glycemic control, probably by enhancing insulin sensitivity and reduced hepatic gluconeogenesis and glucose output.

One dicarboxylic acid, sebacic acid, is named from the Latin sebum, or tallow, in reference to its use in candle manufacturing. It is also a small component of royal jelly, a yellowish material secreted by the glands of worker bees to nourish the queen bee. As a food, it is essential for her longevity. On the medicinal side, royal jelly’s estrogen-like effects modulate estrogen receptor functions.

Azelaic acid for treatment of acne, rosacea, hyperpigmentation

A third DA compound, azelaic acid, is the best known. It is widely used to treat human skin conditions including mild to moderate acne, rosacea, melasma and hyperpigmentation. It is available in prescription and non-prescription strengths

For treating both comedonal and inflammatory acne, azelaic acid’s bacteriostatic and bactericidal properties work against a variety of aerobic and anaerobic micro-organisms that infect skin pores on acne-bearing skin. It also reduces the production of keratin, a natural substance that promotes the growth of acne bacteria.

In addition, azelaic acid has the ability to reduce inflammation, making it useful as a treatment for rosacea. An active ingredient in topical gel, it clears the bumps and swelling associated with rosacea’s characteristic facial redness.

An ingredient in several over-the-counter medications, azelaic acid reduces the synthesis of melanin and is consequently used to reduce melasma and other causes of hyperpigmentation.  It has been recommended as an alternative to hydroquinone, another skin lightener that is, however, considered potentially carcinogenic.

The first synthetic GMP azelaic acid – no animal products

Like other dicarboxylic acids, azelaic acid has industrial applications in the manufacture of rubber, and is readily available for those uses. However, a fully derived synthetic form that contains no animal products has not been available in pharmaceutical grade until now.

Azelaic acid is more desirable for topical drugs than other dicarboxylic acids due to its greater solubility. As a result, in the last decade we have received numerous requests for the ingredient.

When synthesizing azelaic acid 10 years ago, we were obtaining raw material from China, then recrystallizing it and, on occasion, changing the particle size as requested by sponsors for their various applications. While that process met all regulations then, the times – and regulations – have changed. Generally, medications derived from animal products have met with more resistance due to the following objections:

• Conflict with religious beliefs
• Animal welfare concerns
• Vegetarianism
• Potential for veterinary drug residue
• Changes in regulatory requirements

To circumvent these issues, and to offer pharmaceutical companies the ability to produce a differentiated product for today’s more demanding patients, scientists at PCI Synthesis have developed a completely synthetic process, along with associated analytics, that has been scaled and validated.

This is novel chemistry and is the first fully synthetic azelaic acid in the world. It is both fully EMA and FDA compliant.  All the analytics have been developed and meet all the latest requirements.