May 3, 2016
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Finacea Gel




CLINICAL PHARMACOLOGY

Mechanism Of Action

The mechanism(s) by which azelaic acid interferes with the pathogenic events in rosacea are unknown.

Pharmacodynamics

The pharmacodynamics of azelaic acid in association with the treatment of rosacea are unknown.

Pharmacokinetics

The percutaneous absorption of azelaic acid after topical application of FINACEA Gel could not be reliably determined. Mean plasma azelaic acid concentrations in rosacea subjects treated with FINACEA Gel twice daily for at least 8 weeks are in the range of 42 to 63.1 ng/mL. These values are within the maximum concentration range of 24.0 to 90.5 ng/mL observed in rosacea subjects treated with vehicle only. This indicates that FINACEA Gel does not increase plasma azelaic acid concentration beyond the range derived from nutrition and endogenous metabolism.

In vitro and human data suggest negligible cutaneous metabolism of 3H-azelaic acid after topical application of 20% azelaic acid cream. Azelaic acid is mainly excreted unchanged in the urine, but undergoes some -oxidation to shorter chain dicarboxylic acids.

Clinical Studies

FINACEA Gel was evaluated for the treatment of mild to moderate papulopustular rosacea in two multicenter, randomized, double-blind, vehicle-controlled, 12-week clinical trials having identical protocols and involving a total of 664 (active: 333; vehicle: 331) subjects aged 21 to 86 years (mean age = 49). Overall, 92.5% of subjects were Caucasian and 73% of subjects were female. Enrolled subjects had mild to moderate rosacea with a mean lesion count of 18 (range 8 to 60) inflammatory papules and pustules. The following subjects were excluded: a) those without papules and pustules; b) those with nodules, rhinophyma, or ocular involvement and c) those with a history of hypersensitivity to propylene glycol or to any other ingredients of the study drug. FINACEA Gel or its vehicle were to be applied twice daily for 12 weeks; no other topical or systemic medication affecting the course of rosacea and/or evaluability was to be used during the studies. Subjects were instructed to avoid spicy foods, thermally hot food/drink and alcoholic beverages during the study. Subjects were also instructed to use only very mild soaps or soapless cleansing lotion for facial cleansing.

The primary efficacy endpoints included both 1) change from baseline in inflammatory lesion counts as well as 2) success defined as a score of “clear” or “minimal” with at least a 2-step reduction from baseline on the Investigator's Global Assessment (IGA), defined as follows below:

CLEAR: No papules and/or pustules; no or residual erythema; no or mild to moderate telangiectasia

MINIMAL: Rare papules and/or pustules; residual to mild erythema; mild to moderate telangiectasia

MILD: Few papules and/or pustules; mild erythema; mild to moderate telangiectasia

MILD TO MODERATE: Distinct number of papules and/or pustules; mild to moderate erythema; mild to moderate telangiectasia

MODERATE: Pronounced number of papules and/or pustules; moderate erythema; mild to moderate telangiectasia

MODERATE TO SEVERE: Many papules and/or pustules, occasionally with large inflamed lesions; moderate erythema; moderate degree of telangiectasia

SEVERE: Numerous papules and/or pustules, occasionally with confluent areas of inflamed lesions; moderate or severe erythema; moderate or severe telangiectasia

Primary efficacy assessment was based on the “intent-to-treat” (ITT) population with the “last observation carried forward” (LOCF).

Both trials demonstrated a statistically significant difference in favor of FINACEA Gel over its vehicle in both reducing the number of inflammatory papules and pustules associated with rosacea (Table 2) as well as demonstrating success on the IGA in the ITT-LOCF population at the end of treatment.

Table 2: Inflammatory Papules and Pustules (ITT population)*

  Study One FINACEA Gel, 15%
N=164
Study One VEHICLE
N=165
Study Two FINACEA Gel, 15%
N=167
Study Two VEHICLE
N=166
Mean Lesion Count Baseline 17.5 17.6 17.9 18.5
End of Treatment* 6.8 10.5 9.0 12.1
Mean Percent Reduction End of Treatment* 57.9% 39.9% 50.0% 38.2%
*ITT population with last observation carried forward (LOCF)

Although some reduction of erythema which was present in subjects with papules and pustules of rosacea occurred in clinical trials, efficacy for treatment of erythema in rosacea in the absence of papules and pustules has not been evaluated.

FINACEA Gel was superior to the vehicle with regard to success based on the IGA of rosacea on a 7-point static score at the end of treatment (ITT population; Table 3).

Table 3: Investigator's Global Assessment at the End of Treatment*

  Study One FINACEA Gel, 15%
N=164
Study One VEHICLE
N=165
Study Two FINACEA Gel, 15%
N=167
Study Two VEHICLE
N=166
Clear, Minimal or Mild at End of Treatment (% of Subjects) 61% 40% 61% 48%
*ITT population with last observation carried forward (LOCF)

Last reviewed on RxList: 1/6/2016
This monograph has been modified to include the generic and brand name in many instances.

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