Aczone Gel

Aczone Gel

CLINICAL PHARMACOLOGY

Mechanism of Action

The mechanism of action of dapsone gel in treating acne vulgaris is not known.

Pharmacokinetics

An open-label study compared the pharmacokinetics of dapsone after ACZONE Gel (dapsone) , 5%, (110 ± 60 mg/day) was applied twice daily (~BSA 22.5%) for 14 days (n=18) with a single 100 mg dose of oral dapsone administered to a subgroup of patients (n=10) in a crossover design. On Day 14 the mean dapsone AUC0-24 h was 415 ± 224 ng•h/mL for ACZONE Gel (dapsone) , 5%, whereas following a single 100 mg dose of oral dapsone the AUC0- infinity was 52,641 ± 36,223 ng•h/mL. Exposure after the oral dose of 100 mg dapsone was approximately 100 times greater than after the topical ACZONE Gel (dapsone) , 5% dose, twice a day.

In a long-term safety study of ACZONE Gel (dapsone) , 5% treatment, periodic blood samples were collected up to 12 months to determine systemic exposure of dapsone and its metabolites in approximately 500 patients. Based on the measurable dapsone concentrations from 408 patients (M=192, F=216), obtained at month 3, neither gender, nor race appeared to affect the pharmacokinetics of dapsone. Similarly, dapsone exposures were approximately the same between the age groups of 12-15 years (N=155) and those greater than or equal to 16 years (N=253). There was no evidence of increasing systemic exposure to dapsone over the study year in these patients.

Microbiology

In Vivo Activity: No microbiology or immunology studies were conducted during dapsone gel clinical trials.

Drug Resistance: No dapsone resistance studies were conducted during dapsone gel clinical trials. Because no microbiology studies were done, there are no data available as to whether dapsone treatment may have resulted in decreased susceptibility of Propionibacterium acnes, an organism associated with acne, to other antimicrobials that may be used to treat acne. Therapeutic resistance to dapsone has been reported for Mycobacterium leprae, when patients have been treated with oral dapsone.

Clinical Studies

Two randomized, double blind, vehicle controlled, clinical studies were conducted to evaluate ACZONE Gel (dapsone) , 5%, for the treatment of patients with acne vulgaris (N=1475 and 1525). The studies were designed to enroll patients 12 years of age and older with 20 to 50 inflammatory and 20 to 100 non- inflammatory lesions at baseline. In these studies patients applied either ACZONE Gel (dapsone) , 5%, or vehicle control twice daily for up to 12 weeks. Efficacy was evaluated in terms of success on the Global Acne Assessment Score (no or minimal acne) and in the percent reduction in inflammatory, non-inflammatory, and total lesions.

The Global Acne Assessment Score was a 5-point scale as follows:

0      None: no evidence of facial acne vulgaris

1      Minimal: few non-inflammatory lesions (comedones) are present; a few inflammatory lesions (papules/pustules) may be present

2      Mild: several to many non-inflammatory lesions (comedones) are present; a few inflammatory lesions (papules/pustules) are present

3      Moderate: many non-inflammatory (comedones) and inflammatory lesions (papules/pustules) are present; no nodulo-cystic lesions are allowed

4      Severe: significant degree of inflammatory disease; papules/pustules are a predominant feature; a few nodulo- cystic lesions may be present; comedones may be present.

5      The success rates on the Global Acne Assessment Score (no or minimal acne) at Week 12 are presented in Table 4.

Table 4: Success (No or Minimal Acne) on the Global Acne Assessment Score at Week 12

  Study 1* Study 2*
  ACZONE
N=699
Vehicle
N=687
ACZONE
N=729
Vehicle
N=738
Subjects with No or Minimal Acne 291 (42%) 223 (32%) 253 (35%) 206 (28%)
*Analysis excludes subjects classified with minimal acne at baseline

Table 5 presents the mean percent reduction in inflammatory, non-inflammatory, and total lesions from baseline to Week 12.

Table 5: Percent Reduction in Lesions from Baseline to Week 12

  Study 1   Study 2  
  ACZONE
N=745
Vehicle
N=740
ACZONE
N=761
Vehicle
N=764
Inflammatory 46% 42% 48% 40%
Non- Inflammatory 31% 24% 30% 21%
Total 38% 32% 37% 29%

The clinical studies enrolled about equal proportions of male and female subjects. Female patients tended to have greater percent reductions in lesions and greater success on the Global Acne Assessment Score than males. The breakdown by race in the clinical studies was about 73% Caucasian, 14% Black, 9% Hispanic, and 2% Asian. Efficacy results were similar across the racial subgroups.

Last reviewed on RxList: 3/28/2008
This monograph has been modified to include the generic and brand name in many instances.

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