Graceway Pharmaceuticals

Pharmacological Class:

Immune response modifier

Active Ingredient(s):

Imiquimod 3.75%; topical cream; contains parabens.

Indication(s):

Actinic keratoses on face and balding scalp in immunocompetent patients.

Pharmacology:

Actinic keratosis is a precancerous skin condition that results from long-term exposure to harmful UV rays. The lesions are small, reddish, sometimes scaly or rough, and often appear in areas exposed to the sun. Some may develop into squamous cell carcinoma.

The mechanism of action of imiquimod in treating actinic keratoses is not known. It activates immune cells, and the topical application of 5% imiquimod was shown to increase markers for cytokines and immune cells (eg, CD3, CD4, CD8, CD11c, CD68).

This formulation is indicated for treating palpable or visible actinic keratosis lesions on the face or balding scalp. Where there are visible lesions, often there are more lesions just below the surface of the skin. These may berevealed during therapy. Zyclara treats both extant and newly revealed lesions.

Clinical Trials:

Two double-blind, randomized, vehicle-controlled studies were conducted that involved 319 subjects with actinic keratosis. The studies enrolled Caucasian adults with 5 to 20 typical visible or palpable lesions on the face or scalp. The study cream was applied to either the entire face or balding scalp once daily for 2 weeks, then no treatment for 2 weeks, then one more 2-week treatment period. During an 8-week follow-up period, patients returned for clinical observation and monitoring. Efficacy was assessed by total (baseline and newly revealed) lesion counts at the 8-week post-treatment visit. Complete clearance required absence of any lesions. Partial clearance was defined as the percentage of patients in whom the number of baseline lesions was reduced by at least 75%, and the rate was measured relative to the baseline lesion count.

In Study 1, 25.9% of patients using the active drug experienced a complete clearance, compared to 2.5% for vehicle; 45.7% of patients on the study drug had a partial clearance, compared to 18.8% for vehicle. In Study 2, 45.6% of patients given the study drug experienced a complete clearance, and 73.4% had a partial clearance, compared to 10.1% and 26.6% for vehicle, respectively.

Legal Classification:

Rx

Adults:

≥18yrs: Apply thin film to affected area (face or balding scalp) and rub in once daily at bedtime; leave on for 8 hours, wash off with mild soap and water. Treat for two 2-week cycles separated by a 2-week no-treatment cycle. Max two packets per application and one treatment course per area. Apply to intact skin only; Interrupt if severe reaction occurs; do not extend treatment cycle due to missed doses or rest periods. Wash hands before/after application.

Children:

<18yrs: not recommended.

Warnings/Precautions:

Immunosuppressed. Auto-immune conditions. Not for treating xeroderma pigmentosum, superficial basal cell carcinoma, external genital warts. Sun sensitivity. Avoid eyes, lips, nose, mouth, mucous membranes, sun or UV light (use sunscreen daily). Do not occlude. Pregnancy (Cat.C). Nursing mothers.

Interaction(s):

Avoid concomitant other forms of imiquimod.

Adverse Reaction(s):

Local inflammation (eg, erythema, crusting, erosion, weeping, edema), pruritus, flaking, scaling, dryness, flu-like symptoms (eg, headache, fatigue, nausea, fever, chills, myalgia), transient increase in lesion counts; exacerbation of skin inflammatory conditions (eg, graft vs. host disease), chest pain, lymphadenopathy, hypo- or hyperpigmentation.

How Supplied:

Single-use packets—28

Last Updated:

4/29/2010