Avermectin Milbemycin Eyewash for Ocular Rosacea

Written by on March 7, 2012 in Galderma, Ivermectin, Ocular Rosacea, patents with 0 Comments

This recently published patent is interesting for a couple of reasons. Firstly there is renewed interest in Ivermectin because of Galderma’s large trial of Topical Ivermectin 1% Cream (CD5024) for facial rosacea. Secondly there are few official treatments for ocular rosacea, so a provable treatment such as outlined in this patent could show promise.

A word of caution is needed here of course. Patents represent aspirational ideas. They don’t prove that a product exists or will ever exists – they are just inventors attempting to protect their intellectual property.

How Does Ivermectin Work?

The most easily found research on Ivermectin’s efficacy relate to its ability to eliminate demodex mites. Certainly the recently unearthed patents relating to Ivermectin all refer to the anti-parasitic effects as being important in their operation.

“The present invention also features formulation of ivermectin into pharmaceutical compositions useful for the treatment of ophthalmic pathologies, particularly ophthalmic pathologies due to Demodex folliculorum, and more particularly ocular rosacea.”

I have think that there is something else about Ivermectin that hasn’t surfaced yet. Surely all of the effort being invested in Topical and Ophthalmic Ivermectin based treatments aren’t all predicated on eradicating demodex mites are they? Stay tuned for further Ivermectin revelations!

What is Ivermectin?

Ivermectin is a mixture of two compounds belonging to the class of the avermectins, 5-O-demethyl-22,23-dihydroavermectin A1a and 5-O-demethyl-22,23-dihydroavermectin A1b. They are also known under the names of 22,23-dihydroavermectin B1a and 22,23-dihydroavermectin B1b.

Ivermectin comprises at least 80% of 22,23-dihydroavermectin B1a and less than 20% of 22,23-dihydroavermectin B1b. This active agent forms part of the class of the avermectins, a group of macrocyclic lactones produced by the bacterium Streptomyces avermitilis (Reynolds J. E. F. (Ed), (1993) Martindale, The Extra Pharmacopoeia, 29th Edition, Pharmaceutical Press, London).

So there you go, aren’t you glad you asked 🙂


Administration of at least one compound of the family of the avermectins or of the family of the milbemycins, notably ivermectin, is useful for the treatment of ophthalmic pathologies, including ocular rosacea.

United States Patent Application 20120053140

Publication Date: 03/01/2012

Filing Date: 06/14/2011

Assignee: Galderma S.A. (Cham, CH)

Inventors: Kaoukhov, Alexandre (Juan les Pins, FR), Villard, Christophe (Le Tignet, FR), Bouissou, Philippe (Roquefort Les Pins, FR)

[1] A method for the treatment of symptoms of ocular rosacea in the eye(s), said symptoms being selected from the group consisting of a feeling of burning of the eye, a feeling of smarting of the eye, a feeling of dryness of the eye, an increased sensitivity to light, blurred vision, and a complication of ocular rosacea in the cornea, said method comprising topically administering to the eye(s) of an individual in need of such treatment, a thus effective amount of ivermectin, formulated into an eyewash composition with a pharmaceutically acceptable vehicle therefor, wherein ivermectin is the sole active ingredient for treating said symptoms of ocular rosacea in said eyewash, said eyewash being sterile, non-irritating and compatible with eye tissue.

The term “avermectins” means in particular a compound selected from among ivermectin, invermectin, avermectin, abamectin, doramectin, eprinomectin, emamectin and selamectin.

The term “milbemycins” means in particular a compound selected from among lepimectin, milbemectin, milbemycin oxime and moxidectin, nemadectin.

Another related patent, also by Kaoukhov and assigned to Galderma details Topical Ivermectin combined with Metrogel.

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About the Author: David Pascoe started the Rosacea Support Group in October 1998. .

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