Lower dosage strength pharmaceutical compositions forumlated with 3.75% imiquimod

Abstract

Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described.

Description

[0001]This application is a continuation of copending U.S. application Ser. No. 12 / 636,613, filed Dec. 11, 2009, which application claims the benefit of U.S. Provisional Application Ser. No. 61 / 205,145 filed Jan. 15, 2009, U.S. Provisional Application Ser. No. 61 / 144,731 filed Jan. 14, 2009, U.S. Provisional Application Ser. No. 61 / 139, 536 filed Dec. 19, 2008, the teaching of all of which are incorporated herein by reference.FIELD OF THE INVENTION[0002]The present invention relates to pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, also known as (aka) 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, aka imiquimod, to treat actinic keratosis with shorter durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”). More specifically, the present invention is directed to lower dosage strengt...

AI Technical Summary

Benefits of technology

"The present invention provides new and improved methods for treating actinic keratosis using a topical cream formulation of imiquimod called BAY 85®. The invention offers several advantages over the current treatment with FDA-approved Aldara® 5% imiquimod cream, including a larger treatment area, a shorter treatment period, a simplified dosing regimen, and a lower incidence of application site reactions. The invention also provides a more intuitive dosing regimen and a lower dosage strength of imiquimod, which may reduce the risk of irritation and increase the number of lesions treated per treatment area. Overall, the invention offers a more effective and tolerable treatment for actinic keratosis."

Problems solved by technology

In addition, the cellular damage can even extend to the dermis, the layer of skin beneath the epidermis.

Additionally, the skin often becomes wrinkled, mottled, and discolored from chronic sun exposure.

However, even younger adults may develop actinic keratosis when living in geographic areas that are exposed to high-intensity sunlight year round, such as Florida and Southern California.

Actinic keratosis has become a significant health care issue in the United States of America.

Notwithstanding FDA approval, Aldara® 5% imiquimod cream treatment is not without limitation, including an unsimplified and lengthy dosing regimen.

Inconsistencies in both compliance and therapeutic results frequently occur with the treatment of actinic keratosis with FDA-approved Aldara® 5% imiquimod cream due to the lengthy treatment period, i.e., 16 weeks, the complicated dosing regimen, i.e., twice weekly, and the high incidence of application site reactions.

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