[February 13, 2014]

Anacor Pharmaceuticals Announces Publication of Article Describing Boron-Containing Compounds and Their Relevance to Dermatology

Anacor Pharmaceuticals (NASDAQ:ANAC) announced today that a peer-reviewed article describing the recent progress of boron-based compounds in medicine and the properties of these compounds that support their development for the treatment of various skin disorders will be published in the February 17, 2014 edition of the Journal of Clinical and Aesthetic Dermatology. "From the Test Tube to the Treatment Room: Fundamentals of Boron-Containing Compounds and Their Relevance to Dermatology" is co-authored by James Q. Del Rosso, D.O., F.A.O.C.D., dermatologist in private practice at Las Vegas Skin and Cancer Clinics in Henderson, Nevada and Clinical Professor of Dermatology at Touro University College of Osteopathic Medicine in Henderson, Nevada and Jacob. J. Plattner, Ph.D., Senior Vice President of Research, Anacor Pharmaceuticals.

The authors note that the therapeutic benefit of incorporating boron into a chemical compound is derived from boron's unique physical, chemical and structural properties. Boron has an empty p-orbital which gives it the capacity to form covalent bonds at a target site on a protein, rendering the protein inactive or less active. Several examples of proteins that boron-containing compounds have been found to inhibit include phosphodiesterase-4 (PDE4) thereby reducing the cytokine production in psoriasis and atopic dermatitis; leucyl tRNA synthetase thereby blocking protein synthesis in dermatophytes; and ß-lactamases, thereby reducing resistance to antibiotic therapy.

The authors also note that, until recently, the use of boron in drug development has been widely overlooked. Initilly, boron was incorporated into drug candidates as boronic acid which made the compounds overly reactive resulting in off-target binding and decreasing their potential effectiveness as therapeutic agents. However, since then, researchers found that if they incorporated boron into compounds as part of a cyclic structure rather than as an acid, they were able to produce small boron-based molecules that are highly stable, demonstrate effective target binding and selectivity and exhibit optimal physical properties that allow access to the necessary site of the disease target.

"The use of boron in drug discovery and development is very exciting to dermatology and other fields of medicine. Boron's unique properties allow it to bind to target proteins involved in key pathophysiologic pathways which has opened the door to new potential therapies in dermatology including fungal infections such as onychomycosis, atopic dermatitis, psoriasis, acne, bacterial infections and other skin diseases," said Dr. Del Rosso.

Boron-based compounds currently in development for dermatologic indications include tavaborole, which is being reviewed by the FDA for the treatment of toenail onychomycosis and AN2728, a PDE4 inhibitor which has completed Phase 2 studies in psoriasis and atopic dermatitis. A third compound, AN3365, is being evaluated as a gram-negative antibiotic. All three compounds were discovered and are being developed by Anacor Pharmaceuticals.

About Anacor Pharmaceuticals

Anacor is a biopharmaceutical company focused on discovering, developing and commercializing novel small-molecule therapeutics derived from its boron chemistry platform. Anacor has discovered eight compounds that are currently in development. Its two lead product candidates are topically administered dermatologic compounds - tavaborole, an antifungal for the treatment of onychomycosis, and AN2728, an anti-inflammatory PDE-4 inhibitor for the treatment of atopic dermatitis and psoriasis. In addition to its two lead programs, Anacor has discovered three other wholly-owned clinical product candidates - AN2718 and AN2898, which are backup compounds to tavaborole and AN2728, respectively, and AN3365, an antibiotic for the treatment of infections caused by Gram-negative bacteria. Anacor has also discovered three other compounds that have been out-licensed for further development - one is licensed to Eli Lilly and Company for the treatment of an animal health indication, the second compound, AN5568, also referred to as SCYX-7158, is licensed to Drugs for Neglected Diseases initiative, or DNDi, for human African trypanosomiasis (HAT, or sleeping sickness) and the third compound is licensed to GlaxoSmithKline, LLC for development in tuberculosis. Anacor also has a pipeline of other internally discovered topical and systemic boron-based compounds in development. For more information, visit http://www.anacor.com.

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