Patent: Rapamycin / Sirolimus to treat Telangiectasia

Written by on May 4, 2013 in patents, Red Face of Rosacea, telangectasia with 0 Comments


There are very few existing rosacea treatments for the broken blood vessels and general red face of rosacea. Historically laser and IPL are the only proven treatments for this rosacea subtype.

In the last couple of years rosacea sufferers have been encouraged by the development of 2 new drugs that could help treat these symptoms (brimonidine and oxymetazoline). These 2 drugs are slowly making their way through the drug development process. Recently we learnt that Sansrosa has been submitted for final FDA approval.

Patent applications can sometimes give a glimpse into the far distances to see new drugs being considered. Patent applications may also show other things like companies staking out intellectual turf. So even though patent application might show interesting developments they might also reveal pure fantasy as far as new drugs are concerned.

Having said all that, a new patent application has emerged that looks interesting as it appears to point to a new drug that could be useful as a treatment for the redness and broken blood vessels of rosacea.

A word of caution is definitely needed here. A patent application is not a clinical trial or medical advice. This application lists a sole participant in custom made topical application of Rapamune.

Rapamune is a serious drug used to help stop organ transplant rejection. The safety information for Rapamune is a cracker. It is not often that the word death is used in typical prescriptions for rosacea treatments!

Topical Rapamycin / Sirolimus Patent

Methods of treating skin conditions exhibiting telangiectasia

Inventors Jeffrey Sugarman

Agent: Dow Pharmaceutical Sciences – Petaluma, CA, US
USPTO Applicaton #: #20130102572

Abstract: The present application relates to methods of preventing or treating skin disorders exhibiting telangiectasia, for example, rosacea exhibiting an erythematotelangiectatic subtype. Exemplary methods comprise administering to a patient a formulation comprising a therapeutically effective amount of an mTOR inhibitor, such as rapamycin, wherein the mTOR inhibitor is the only active agent in the formulation. Suitably, the formulations are topical formulations administered to the face.

Rapamycin (sirolimus), is a macrocyclic triene antibiotic produced by Streptomyces hygroscopicus (see U.S. Pat. No. 3,929,992) that has been shown to prevent the formation of humoral (IgE-like) antibodies in response to an albumin allergic challenge (Martel, R., Can. J. Physiol. Pharm. 55: 48 (1977)), inhibit murine T-cell activation (Staruch, M., FASEB 3: 3411 (1989)), and prolong survival time of organ grafts in histoincompatible rodents (Morris, R., Med. Sci. Res. 17: 877 (1989)).

Rapamycin has been approved by the FDA to prevent rejection of organ transplants, particularly kidney transplants. It has been suggested for use in treating skin conditions, however, limited to immunoinflammatory skin diseases. See U.S. Pat. No. 5,286,730, the disclosure of which is incorporated by reference herein.

[0007] In embodiments, methods are provided for treating a skin condition exhibiting telangiectasia comprising administering to a patient a formulation comprising a therapeutically effective amount of an mTOR inhibitor. Suitably, the mTOR inhibitor is the only active agent in the formulation. The methods suitably reduce the telangiectasia and/or erythema.

[0008] In exemplary embodiments, the mTOR inhibitor is rapamycin.

[00010] Suitably the mTOR inhibitor is present in the formulation at a concentration of about 0.5% to about 10% by weight, for example about 1% to about 8% by weight.


[00095] Topical Rapamycin Ointment 1%: 40mg of rapamycin was obtained using 40 tablets of RAPAMUNE® (Wyeth-Ayerst) containing 1 mg of rapamycin each. The tablets were crushed using a mortar and pestle and then sifted to remove the colored pieces of tablet coating material. The rapamycin was next extracted from the crushed tablets with three sequential aliquots of acetone by shaking well in a tightly closed glass jar. The aliquots were passed through a filter paper to exclude the tablet excipients, and the filtrate was air dried for at least 8 hours on a glass plate. The resulting pure rapamycin was then incorporated into 4 grams of petrolatum and mixed until homogeneous.


[000157] 4. Evaluator performed the IGA for ETR which revealed an IGA of 2 (mild). This represents an improvement of the IGA from a 3 (moderate) to a 2 (mild) in just 2 weeks

[000161] The subject is to be evaluated at specified periods over the course of I , 3, 6, 9, 12, 24, and 48/or months, etc. An improvement from the IGA of 3 (moderate) to 2 (mild) to 1 (almost clear) to 0 (clear) over the study period, and potentially maintaining this improvement, is an indication of the surprising and unexpected reduction in IGA demonstrated by the present formulations

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

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