New rosacea treatments offer hope

New, exciting treatments for rosacea are on the horizon. Several new topicals will become available, including SR101, which SansRosa Pharmaceuticals has developed to reduce triggers and to treat rosacea redness and flushing.

SR101 is a new form of an alpha-2 adrenergic receptor agonist compound that has been used for the treatment of certain eye disorders. When applied topically, it eliminates skin redness rapidly through a constrictor response, restoring facial skin to its normal color. SR101 will be a topical, once-a-day, rapid-onset product. The therapeutic potential of this compound has been documented in initial pilot studies at the Mayo Clinic and in placebo-controlled split-face studies. So far, the results show great promise with no rebound dilation.

New topical from dapsone

This may also be the first topical to successfully treat rosacea with coexisting acne without aggravating the underlying vascular disorder. This is extremely important because most topical anti-acne products are much too harsh for rosacea-sensitive skin, resulting in increased facial redness and flushing.

Transdermal delivery systems

New transdermal delivery systems also are changing the way we can treat rosacea topically. Restoraderm (CollaGenex) is a patented transdermal drug delivery system formulated with lipids. It offers rapid penetration and absorption into the stratum corneum of hydrophilic and hydrophobic medications.

A new solvent microparticle (SMP) delivery system (Atrix Laboratories) delivers highly insoluble drugs through the skin in a non-irritating, time-released fashion. Since many medications that could help treat rosacea redness and flushing are insoluble, they could not be used in the past. The SMP technology first delivers an unencapsulated drug followed by encapsulated microparticles of the drug, providing delayed release of agents into the dermal tissue for sustained 24-hour treatment.

Chemically modified oral antibiotic

Research has shown that certain antibiotics can be chemically modified to retain non-antibiotic properties and enhance their anti-inflammatory actions. CollaGenex is developing various chemically modified antibiotics termed IMPACSthat inhibit inflammatory proteases and cytokines.

Periostat (CollaGenex)and Oracea(CollaGenex) have proven anti-inflammatory actions in rosacea, but according to Klaus Theobald, M.D., a new, second-generation, chemically modified oral antibiotic may change the face of rosacea. This antibiotic retains non-antimicrobial actions at high doses and has already been tested on rosacea sufferers in small multi-center studies with excellent results.

This oral antibiotic derivative downregulates inducible nitric oxide (a powerful dilator), VEGF (a powerful dilator with strong angiogenic properties), and cell adhesion molecules (gateways to dermal inflammation) - all substances proven to play an intimate role in rosacea redness, flushing and triggers.

Future treatments

Several biotechnology and pharmaceutical companies are racing to develop the first topical biologic response modifier for skin redness and flushing. Three of the most exciting agents that show great promise in preliminary studies are focused on normalizing dysfunctional smooth muscle cells in blood vessels of rosacea skin.

These include selective agonists of kinase enzymes in the smooth muscle wall, intercellular gap junction blockers that stop conducted dilation, and uncoupling G-proteins to prevent countless dilator triggers from reaching the intercellular Ca++ stores in smooth muscle cells of rosacea blood vessels.

Jeffrey Nase, Ph.D., is a rosacea research specialist and consultant at Indiana University School of Medicine. He holds a doctorate in physiology and specialized in microvascular physiology in his post-doctoral training.