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Dr. Geoffrey Nase, PhD
Rosacea Research Specialist

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Table of Contents

> SansRosa Treatment  -- First topical to address rosacea redness & flushing

> Introduction

> Time-release lipsomal drug delivery system

> Other active ingredients?

> New information sheds light on SansRosa's active ingredient

 

SansRosa Treatment -- First Topical to Address Erythema & Flushing

SansRosa Pharmaceutical Development Inc. has received $250,000 from Bioadvance to fund the first topical rosacea treatment for facial redness and flushing. San Rosa's first product is a novel treatment for rosacea that will represent a breakthrough as the first effective therapy for Subtype I rosacea sufferers. It is a new form of a compound previously approved for a different inflammatory skin disorder. The product, designated SR101, when applied topically to rosacea skin eliminates skin redness rapidly restoring normal skin color. SR101 will be a topical, once-a-day, rapid onset product that will minimize the possibility of side effects from systemic administration. The therapeutic potential of this compound has been documented in an initial pilot study initiated by an investigator at the Mayo Clinic This product is in Phase I Clinical Development for rosacea. So far, the results have shown great promise.

  • Interview with Dr. Gary Kurtzman -- Chief Investigative Officer of Rosacea Treatment
  • Interview with Dr. Hal Brodenson -- Chief Investigator of Rosacea Treatment
  • SansRosa's Proposed Mechanism of Action on Rosacea Erythema

 

Intoduction

Based on early reports from the Research and Development sector, it is suggested that the main ingredient used to reduce rosacea redness will be a phenylephrine agonist derivative --   similar to the phenyephrine constrictor drops you find for red eye and the phenylephrine based hemmorhoidal gel.  However, using advanced tecnhology they will only be using certain phenylephrine alpha (1) receptor agonists to selectively activate certain receptors to ensure that the rebound phenomenon does not occur.

To explain, phenylephrine alpha (1) receptor agonists act on four different receptors in blood vessels to cause constriction.  Two receptors are known to be the main culprits in the rebound phenomenon; while the other two are good constrictors, but do not show the tendency towards rebound vasodilation.  The four agonists are:

  • Phenylephrine alpha (1A) agonist
  • Phenylephrine alpha (1B) agonist
  • Phenylephrine alpha (1C) agonist
  • Phenylephrine alpha (1D) agonist

The ones that do not cause the rebound phenomenon are:

  • Phenylephrine alpha (1B) agonist
  • Phenylephrine alpha (1D) agonist

 

These agonists cause gentle constiction of blood vessels which results in reduced facial redess and attenuation of flushing tiggers without altering oxygen levels or nutrient delivery.

 

Special Time-Released Liposomal Hydrogel Delivery System for Fast Release and 24 Hour Sustained Release

Reports also indicate that the action on blood vessels will take place immediately and be long lasting (24 hours) which should be of great benefit to rosacea sufferers.  The special time-released  liposomes will release 25% of the active drug immediately when it is activated by heat from blood vessels and the inner liposomal layer will slowly release the remaining 75% of the drug over the next 23 hours for sustained release.

The hydrogel liposomes are very friendly to skin and melt right through the epidermis without damaging epidermal cells.  Also, the polymer technology allows the liposomes to penetrate extremely deep so that it should have an efffect on superficial vessels and medium depth vessels.

 

Other Active Ingredients?

It is safe to assume that the Research and Development team did not tell me everything due to the competitive market.  I was lead to believe there would be one or two 'secret' complimentary ingredients to enhance the action of this topical rosacea drug.  We most certainly wont hear the exact details on these until the product is on the market. 

This is good news for rosacea sufferers.

 

New Information Sheds Light on SansRosa Anti-Redness Topical

Due to the early stages of development, companies need to sometimes keep drug information secret until patents are approved and their drug is safe from other companies.  This does lead to incomplete information sometimes, especially when it is cutting-edge information presented years before it will hit the shelves.  The only infrormation that I can reveal is now it seems the main active ingredient is not a phenylephrine derivative; it is a selective alpha-2 receptor agonist.   I am not sure if it will act on both alpha-2A and alpha-2C receptors, or just act on one receptor subtype. The alpha-2 receptor agonist was chosen primarily due to its long history of use in humans and becuase this group of receptors was the least likely to cause side effects and rebound dilation.   I just wanted to update everyone with the latest information.  This may also help reduce the symptoms of ocular rosacea, but I dont think that will be a main focus until the facial skin preparation is available.





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