PubMed pushed out an interesting abstract in the last couple of days. A bit of digging reveals what looks to be a running mate for COL-118/Sansrosa. COL-118 and Oxymetazoline appear to be promoted by separate groups of researchers.
This is good news for rosacea sufferers as it means there may well be a choice between 2 topicals that can help address the redness and flushing of rosacea.
With the publishing of this new paper, Successful Treatment of the Erythema and Flushing of Rosacea Using a Topically Applied Selective {alpha}1-Adrenergic Receptor Agonist, Oxymetazoline, a new, but similar to COL-118/Sansrosa topical, has become more public.
An attempt to treat ETR rosacea using an over-the-counter drug known to possess vasoconstrictive properties was undertaken. A commercially available preparation of oxymetazoline hydrochloride, 0.05%, solution was applied once daily to the affected area of the face.
Patient 1 and her physician (1 of us) (A.L.O.) noted a decrease in facial erythema within 1 hour of drug application, and a dramatic improvement within 2 to 3 hours. This effect was sustained throughout the entire day. After a 7:30 AM application of the drug, the patient noted an improvement in the chronic “baseline”erythema, and experienced a marked reduction in his transient flares. His erythema continued to be controlled in the early afternoon, at his normal time of peak erythema, and he experienced no stinging or burning
Baseline photograph of patient 1 immediately prior to application of oxymetazoline, 0.05%, solution (A) and 3 hours after topical application (B), demonstrating marked improvement in macular erythema and fine telangiectasias.
Oxymetazoline is classified as a alpha-1 Adregenic Receptor Agonist, whereas COL-118/Sansrosa is a alpha-2 Adregenic Receptor Agonist.
Whilst COL-118 is further along the development path towards general availability, this paper raises the hope that oxymetazoline may also become available `on-label’ for rosacea treatment.
It is worthwhile listing some similarities and differences between these 2 redness reducing relatives.
| COL-118/Sansrosa | Oxymetazoline | |
| Status | Phase III trials to start in 2008 | First academic paper published |
| Patent Authors | Jack Dejovin, Thomas Rossi. | Stuart Shanler |
| Patent Link | WO/2004/105703 | 20050165079 |
| Commercial Owners | Collagenex Pharmaceuticals | Aspect Pharmaceuticals (under construction) |
| Related Names | brimonidine tartrate | Oxymetazoline HCl |
| Related Topical Products | Alphagan P | Afrin, Vicks Sinex, Visine L.R. |
| Potential Negative Side Effects | psychosis, heart problems, rebound redness | rebound redness, hypertension, palpitation |
The Sansrosa patent also has references to oxymetazoline, so there appears to be some overlap in at least some of their invention claims.
I would urge rosacea sufferers to use caution when using OTC or prescription drugs off label. It is a far safer option to wait for the FDA to approve any possible new topical redness treatments. Please be very wary until these drugs have been proven safe and effective in treating the redness and flushing of rosacea.
great news
The safety profile for brimonidine tartrate and oxymetazoline HCl supports use under eyelids which generally provides more absorption into the blood than skin tissue. I am encouraged.
Hi Charles,
As brimonidine tartrate is the active ingredient in the Glaucoma eye drops known as Alphagan P, I would imagine that there is quite a lot known about how this behaves in and around the eye.
davidp.
David,
How does Alphagan P work for ocular rosacea? i imagine if it has the same effect as col-118 (same ingriedient) then surely it must be effective for the inflammation assosiated with ocular rosacea? I
Hi Mark,
I think that is a great question that is yet to be answered. As a treatment for Glaucoma, Alphagan P is of course used in the eye. The list of possible side effects from using Alphagan P is long. I would suggest that Opthalmic use of Alphagan P is only for severe disease.
Here is the list of possible side effects, in decreasing order of prevalence. (from http://www.alphaganp.com/ALPHGANP.pdf).
“allergic conjunctivitis, conjunctival hyperemia, eye pruritus, burning sensation, conjunctival folliculosis, ocular allergic reaction, visual disturbance, allergic reaction,blepharitis, blepharoconjunctivitis, blurred vision, cataract, conjunctival edema, conjunctival hemorrhage, conjunctivitis, eye discharge, eye dryness, eye irritation, eye pain, eyelid edema, eyelid erythema, follicular conjunctivitis, foreign body sensation, keratitis, lid disorder, photophobia, rhinitis, stinging, superficial punctate keratopathy, tearing, visual field defect, vitreous detachment, vitreous disorder, vitreous floaters, and worsened visual acuity, corneal erosion.”
It is an interesting question as to whether Galderma/Collagenex would be interested in developing and marketing COL-118 or indeed Alphagan P (owned by Allergan) as an ocular rosacea treatment.
davidp.
Man….I’m ready to start putting those eye drops right on my face! I am not waiting till 2010 to see if it works.
If you can put something like that in your eyes! I’m sure a drop on my cheeks won’t be the worst thing. Heck…I can go out side and be subjected to worse elements on my face. I wonder if I can purchase those eye drops out of the country…like maybe Canada??
Anyone have a thought on that!??
Regards to all
southerngulfhome
I have found an online website that has brand name Alphagan P. I am seriously tempted to give it a go just to see what kind of results i am likely to get. 5ml (the amount the drops come in) won’t last more than a few applications though so….
As for slopping Alphagan P on your face, here is a list of the known possible side effects from the systemic absorption of brimonidine (brimonidine tartrate):
fatigue, dangerously low blood pressure, dangerously high blood pressure rebound, coronary problems
long-lasting rebound redness, increased flushing
damage to facial blood vessels, increased blood flow the face (reactive hyperemia), skin irritation, _psychosis_
Certainly people who have tried it do report rebound redness and so ceased using it.
take care out there !
davidp.
I haven’t read any posts from people actually using the same substance as will be on sanrosa. I have read the threads on the nasal spray and agree that people do seem to get rebound flushing. Could you possibly direct me to where people have tried Alphagan P?
Thanks,
Mark
HI, can I use a spray bottle of Dristan with oxymetazoline for roseate treatment
Ben
Hi, how can I use oxymetozoline on my face for roseacea treatment? Should use eyedrops or nasal spray for treatment
Thanks
Ben
In generic equivalent drugs active ingredients will be the same but inactive ingredients will not be same. In that case what is the severity of the side effects.
For those who are taking Alphagan p /Brimonidine Eye Drops for severity conditions you can find the list of drugs that interact with alphagan p and increase the intensity of the side effects at International Drug Mart
How can I get Brimonidine Eye Drops in Canada? Nobody can ship this Item in Canada…
Is there any indication as to when the Sansrosa drug will be FDA approved? This trial has been going on now for several years. What is holding up the marketing in the US? You would think that since there are growing numbers of people suffering from this horrible and unsightly condition that some resolution could occur soon. Is it all about the pharmaceutical industry wanting their huge profit structure in place first? It just isn’t fair to those of us who have had to battle this condition for so long without little or no success for its cure any time soon. It just plain is frustrating.
Hi Suzanne,
Sansrosa is still in the large Phase 3 trial stage. It is in the process of being proven safe for long term use as well as proving that the improvements seen in earlier trials can be replicated on a larger scale.
After that, when Galderma is ready to file for final approval (around 100,000 pages) it can be around 18 months later that the FDA grants approval – if it all. My best guess is mid 2014 at the earlier. See my reasoning here Final FDA Approval of Sansrosa, expect 15 months post Phase III.
I’m sure that Galderma would love to sell it as soon as they are allowed to.
dp.