Actinic Keratosis News and Articles

Return to Library

Recent Actinic Keratosis News and Articles

• \"Methods and Compositions for Improving the Nutritional Content of Mushrooms and Fungi\" in Patent Application Approval Process
• Patent Application Titled \"Continuous Low Irradiance Photodynamic Therapy Illumination System\" Under Review
• New Clinical Oncology Findings from Grant Medical College Described
• Scientists at Ruhr-University Bochum Publish Research in Skin Cancer
• Patent Issued for Ex Vivo Uses of Immunostimulatory Combinations
• PhotoMedex Raises Fourth Quarter 2012 Revenue Forecast
• PhotoMedex Extends Agreement with Ya-Man for the no!no! Brand in Japan
• Patent Issued for Methods and Compositions for Improving the Nutritional Content of Mushrooms and Fungi
• Studies from Institute for Cancer Research and Treatment (IRCCS) Have Provided New Data on Dermatology

Researchers Submit Patent Application, "Methods of Treating Dermatological Disorders and Inducing Interferon Biosynthesis with Shorter Durations of Imiquimod Therapy", for Approval

The patent's assignee for patent serial number 552535 is Medicis Pharmaceutical Corporation.

News editors obtained the following quote from the background information supplied by the inventors: "The compound 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, known as imiquimod and commercially marketed in the U.S. under the brand name Aldara.RTM., is disclosed in U.S. Pat. No. 4,689,338 and described therein as an antiviral agent and as an interferon inducer, which is incorporated herein by reference in its entirety. A variety of formulations for topical administration of imiquimod are also described therein. This U.S. Pat. No. 4,689,338 is incorporated herein by reference in its entirety

"U.S. Pat. No. 4,751,087 discloses the use of a combination of ethyl oleate and glyceryl monolaurate as a skin penetration enhancer for nitroglycerine, with all three components being contained in the adhesive layer of a transdermal patch, wherein this U.S. patent is incorporated herein by reference in its entirety.

"U.S. Pat. No. 4,411,893 discloses the use of N,N-dimethyldodecylamine-Noxide as a skin penetration enhancer in aqueous systems, wherein this U.S. patent is incorporated herein by reference in its entirety.

"U.S. Pat. No. 4,722,941 discloses readily absorbable pharmaceutical compositions that comprise a pharmacologically active agent distributed in a vehicle comprising an absorption-enhancing amount of at least one fatty acid containing 6 to 12 carbon atoms and optionally a fatty acid monoglyceride. Such compositions are said to be particularly useful for increasing the absorption of pharmacologically active bases, wherein this U.S. patent is incorporated herein by reference in its entirety.

"U.S. Pat. No. 4,746,515 discloses a method of using glyceryl monolaurate to enhance the transdermal flux of a transdermally deliverable drug through intact skin, wherein this U.S. patent is incorporated herein by reference in its entirety.

"U.S. Pat. No. 5,238,944 discloses topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine, wherein this U.S. patent is incorporated herein by reference in its entirety."

As a supplement to the background information on this patent application, NewsRx correspondents also obtained the inventors' summary information for this patent: "The present invention provides a substantially non-irritating pharmaceutical formulation for topical and/or transdermal administration of the imiquimod, which formulation comprises:

"a) 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, i.e., imiquimod, in an amount of about 2 percent to about 4 percent by weight based on the total weight of the formulation; and

"b) a pharmaceutically acceptable vehicle for imiquimod, which vehicle comprises a fatty acid, such as isostearic acid, linoleic acid, oleic acid, super purified oleic acid (an oleic acid having low polar impurities such as peroxides) and a combination thereof, in a total amount of about 3 percent to about 45 percent by weight based on the total weight of the formulation. The formulation is further characterized in that when tested in the hairless mouse skin model described in U.S. Pat. No. 5,238,944, the formulation provides a penetration of the agent of at least about 10% (and preferably at least about 15%) of the total amount of the agent contained in the formulation in 24 hours.

"The salient elements of a pharmaceutical formulation according to the invention are (a) imiquimod and (b) a fatty acid, e.g., isostearic, linoleic, super purified oleic or oleic acid and mixtures thereof. A pharmaceutical formulation of the invention can be in any form known to the art, such as a cream, an ointment, a foam, a gel, a lotion or a pressure-sensitive adhesive composition, each form containing the necessary elements in particular amounts and further containing various additional elements.

"A cream of the invention preferably contains about 2 percent to about 4 percent by weight of imiquimod based on the total weight of the cream; about 5 percent to about 25 percent by weight of fatty acid, based on the total weight of the cream; and optional ingredients such as emollients, emulsifiers, thickeners, and/or preservatives.

"An ointment of the invention contains an ointment base in addition to imiquimod and fatty acid. An ointment of the invention preferably contains about 2 percent to about 4 percent by weight imiquimod; about 3 percent to about 45 percent, more preferably about 3 percent to about 25 percent by weight fatty acid; and about 40 percent to about 95 percent by weight ointment base, all weights being based on the total weight of the ointment. Optionally, an ointment of the invention can also contain emulsifiers, emollients and thickeners.

"A pressure-sensitive adhesive composition of the invention contains imiquimod, fatty acid, and an adhesive. The adhesives utilized in a pressure sensitive adhesive composition of the invention are preferably substantially chemically inert to imiquimod. A pressure sensitive adhesive composition of the invention preferably contains about 2 percent to about 4 percent by weight imiquimod; about 10 percent to about 40 percent by weight, more preferably of about 15 percent to about 30 percent by weight, and most preferably about 20 percent to about 30 percent by weight of fatty acid; all weights being based on the total weight of the pressure sensitive adhesive composition.

"Optionally, pressure sensitive adhesive compositions of the invention can also contain one or more skin penetration enhancers. The total amount of skin penetration enhancer(s) present in a pressure sensitive adhesive composition of the invention is preferably about 3 percent to about 25 percent by weight, and more preferably about 3 percent to about 10 percent by weight based on the total weight of the pressure sensitive adhesive composition.

"A pressure sensitive adhesive coated sheet material of the invention can be made from a pressure-sensitive adhesive composition of the invention in the form of an article such as a tape, a patch, a sheet, or a dressing.

"A formulation of the present invention may be used to topically and/or transdermally administer imiquimod for effectively treating viral infections, for example, Type I or Type II Herpes simplex infections, actinic keratosis and superficial basal cell carcinoma for a shorter duration of time and with the same or increased number of applications per week, as compared to current imiquimod topical therapy.

"For example, a formulation of the present invention containing between greater than about 1% and about 5% imiquimod may be applied from three to seven times per week (once per day) for 8 to 12 weeks to treat viral infections, for example, Type I or Type II Herpes simplex infections, actinic keratosis and superficial basal cell carcinoma or to induce interferon biosynthesis. It should be understood that while formulations of the present invention containing between greater than about 1% and about 5% imiquimod are preferred, formulations containing about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0%, 4.25% and 4.5% are more preferred and that formulations containing about 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75% and 4.0% are most preferred.

"As to duration, the present invention contemplates applying an effective amount of imiquimod for a shorter period of time than currently approved by the FDA. More specifically, the present invention contemplates applying an effective amount of imiquimod from three to seven times or more per week to an area in need of imiquimod treatment for about 8 to about 12 weeks, and more preferably between about 4, about 5, about 6 and about 7 times a week for about 8, about 9 or about 10 weeks. More preferably, examples of shorter periods of treatment with low dose imiquimod for treating actinic keratosis and warts, e.g., external genital and perianal, as contemplated by the present invention comprise:

"(a) applying an effective imiquimod dose of the lose dose imiquimod formulations, such as about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0%, 4.25% or 4.5% imiquimod % w/w, to the area affected with actinic keratosis, as follows: applying an effective amount once per day for fourteen (14) consecutive days, followed by no application for fourteen (14) days, followed by again applying an effective amount once per day for fourteen (14) days for a total of twenty-eight (28) doses to treat actinic keratosis;

"(b) applying an effective imiquimod dose of the lose dose imiquimod formulations, such as about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0%, 4.25% or 4.5% imiquimod % w/w, to the area affected with actinic keratosis, as follows: applying an effective amount once per day for twenty one (21) days, followed by no application for twenty one (21) days, followed by again applying an effective amount once per day for twenty one (21) consecutive days for a total of forty-two (42) doses to treat actinic keratosis;

"© applying an effective imiquimod dose of the lose dose imiquimod formulations to the warts, such as about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0%, 4.25% or 4.5% imiquimod % w/w, once per day, each day, for up to 56 consecutive days or 8 consecutive weeks or until clearance is observed, which ever occurs earlier to treat the warts; or

"(d) applying an effective imiquimod dose of a lose dose imiquimod formulation, such as about 2.0%, 2.25%, 2.5%, 2.75%, 3.0%, 3.25%, 3.5%, 3.75%, 4.0%, 4.25% or 4.5% imiquimod % w/w, to a dermatological area, once per day, each day, for:

"(i) up to about 56 consecutive days or about 8 consecutive weeks to induce effective interferon biosynthesis;

"(ii) fourteen (14) days, followed by no application for fourteen (14) days, followed by again applying an effective amount imiquimod dose once per day for fourteen (14) consecutive days for a total of twenty-eight (28) doses to induce effective interferon biosynthesis; or

"(iii) twenty one (21) days, followed by no application for twenty one (21) days, followed by again applying an effective imiquimod dose once per day for twenty one (21) consecutive days for a total of forty-two (42) doses to induce effective interferon biosynthesis.

"While the present invention has identified what it believes to be preferred concentrations of imiquimod, numbers of applications per week and durations of therapy, it should be understood by those versed in this art that any effective concentration of imiquimod in a formulation and any numbers of application per week that can accomplish a reduction in therapy duration to effectively treat Type I or Type II Herpes simplex infections, actinic keratosis and superficial basal cell carcinoma or induce effective interferon biosynthesis is contemplated by the present invention."

For additional information on this patent application, see: Gregory, Jefferson J. Methods of Treating Dermatological Disorders and Inducing Interferon Biosynthesis with Shorter Durations of Imiquimod Therapy. U.S. Patent Serial Number 552535, filed July 18, 2012, and posted November 22, 2012. Patent URL: http://appft.uspto.gov/netacgi/nph-Parser'Sect1=PTO2&Sect2=HITOFF&u=%2Fnetahtml%2FPTO%2Fsearch-adv.html&r=1635&p=33&f=G&l=50&d=PG01&S1=20121115.PD.&OS=PD/20121115&RS=PD/20121115

Keywords for this news article include: Medicis Pharmaceutical Corporation, Patents, Oncology, Cytokines, DNA Viruses, Dermatology, Interferons, Legal Issues, Actinic Keratosis, Viral Skin Diseases, Basal Cell Carcinoma, DNA Virus Infections, Herpes Simplex Virus, Herpesviridae Infections, Intercellular Signaling Peptides and Proteins.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2012, NewsRx LLC