Emerging topical drugs for the treatment of rosacea

ABSTRACT

Introduction: Rosacea is a common, chronic and relapsing inflammatory skin disease of the centrofacial area. Despite advancing knowledge on its pathogenesis, diagnosis, and treatment, some major unknowns still remain, including systematic evidence-based guidelines useful both for clinical assessment and therapeutic management. Topical treatment is regarded as a first-line option for mild to moderate rosacea and includes traditional and new FDA-approved prescription drugs, as well as off-label alternative topical agents.

Areas covered: Since improved awareness of rosacea pathogenetic mechanisms has led to the development of new potential therapeutic agents, a search was performed on the ClinicalTrial.gov registry. The results identified several investigational topical drugs able to target one or more of the pathogenetic factors of rosacea.

Expert opinion: The main unmet needs in the topical treatment of rosacea remain the management of vasomotor flushes and telangiectasias, as well as of troublesome symptoms such as burning and/or stinging. No single agent effective on all rosacea phenotypes is available so far, and preventive treatments capable of halting disease progression have not been identified yet. Finally, data on long-term efficacy and tolerability are still incomplete, especially for drugs more recently introduced in the market.

KEYWORDS:

• Emerging drugs
• mechanism-based treatment
• new treatments
• pharmacotherapy
• rosacea
• topical treatment

Abbreviation

AMP = Antimicrobial Peptide

AzA = Azelaic Acid

BPO = Benzoyl Peroxide

BT = Brimonidine Tartrate

CEA = Clinician Erythema Assessment

ETR = Erythematotelangiectatic Rosacea

FDA = Food and Drug Administration

GPCR = G-Protein Coupled Receptor

IGA = Investigator Global Assessment

IL = Interleukin

ILC = Inflammatory Lesion Count

IVM = Ivermectin

MMPs = Matrix Metalloproteinases

MnP = Manganese Porphyrin

MTZ = Metronidazole

NF-κB = Nuclear Factor-kappa B

NOD = Nucleotide-binding Oligomerization Domain

Nrf2 = Nuclear Factor Erythroid 2-related Factor 2

OH = Oxymetazoline Hydrochloride

PAR-2 = Protease-Activated Receptor-2

PDE-4 = Phosphodiesterase-4

PPR = Papulo–Pustular Rosacea

PSA = Patient’s Self-Assessment

QoL = Quality of Life

RCTs = Randomized Controlled Trials

ROS = Reactive Oxygen Species

SS = Sodium Sulfacetamide

SSS = Sodium Sulfacetamide Sulfur

STAT-3 = Signal Transducer and Activator of Transcription -3

TLR-2 = Toll-Like Receptors-2

TLSP = Trypsin-Like Serine Protease

TNF-α = Tumor Necrosis Factor alpha

TRP = Transient Receptors Potential

TRPV-4 = Transient Receptor Potential Vanilloid-4

TXA = Tranexamic Acid

UV = ultraviolet

VEGF = Vascular Endothelial Growth Factor

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

A reviewer on this manuscript has disclosed a relationship with the following affiliations: Galderma, Ortho Dermatologics, Vyne Therapeutics, and SolGel. Another reviewer on this manuscript has disclosed that they are a consultant, researcher, and speaker for many companies with rosacea products including EPI Health, Galderma, LeoPharma, and Vyne Therapeutics. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Additional information

Funding

This paper was not funded.