Ximino
CLINICAL PHARMACOLOGY
Mechanism of Action
The mechanism of action of Ximino for the treatment of acne is unknown.
Pharmacodynamics
The pharmacodynamics of Ximino for the treatment of acne are unknown.
Pharmacokinetics
Ximino is not bioequivalent to immediate release minocycline products.
Following administration of a single dose of Ximino (135 mg) to healthy male and female adult subjects, the mean (SD) AUC(0-∞) and Cmax were 12.87 (4.04) mcg x hr/mL and 0.68 (0.25) mcg/mL, respectively, under fasting conditions.
When a single dose of Ximino (135 mg) was administered with a high fat meal to the same subjects in the same study in a crossover design, the mean (SD) AUC(0-∞) and Cmaxwere 14.16 (3.10) mcg x hr/mL and 0.85 (0.20) mcg/mL, respectively.
A single-dose, crossover study demonstrated that Ximino (45 mg and 135 mg) exhibited dose-proportional pharmacokinetics.
Minocycline is lipid soluble and distributes into the skin and sebum.
Clinical Studies
The safety and efficacy of minocycline hydrochloride in the treatment of inflammatory lesions of non-nodular moderate to severe acne vulgaris was assessed in two 12-week, multi-center, randomized, double-blind, placebo-controlled, studies in subjects ≥ 12 years. The mean age of subjects was 20 years and subjects were from the following racial groups: White (73%), Hispanic (13%), Black (11%), Asian/Pacific Islander (2%), and Other (2%).
In two efficacy and safety trials, a total of 924 subjects with non-nodular moderate to severe acne vulgaris received minocycline hydrochloride or placebo for a total of 12 weeks, according to the following dose assignments.
Table 3: Clinical Studies Dosing Table
| Subject's Weight (Ibs) | Subject's Weight (kg) | Available Capsule Strength (mg) | Actual mg/kg Dose |
| 99 to 131 | 45 to 59 | 45 | 1 to 0.76 |
| 132 to 199 | 60 to 90 | 90 | 1.5 to 1 |
| 200 to 300 | 91 to 136 | 135 | 1.48 to 0.99 |
The two primary efficacy endpoints were:
- Mean percent change in inflammatory lesion counts from Baseline to 12 weeks.
- Percentage of subjects with an Evaluator's Global Severity Assessment (EGSA) of clear or almost clear at 12 weeks.
Efficacy results are presented in Table 4.
Table 4: Efficacy Results at Week 12
| Study 1 | Study 2 | |||
| Minocycline hydrochloride (1 mg/kg) N = 300 |
Placebo N = 151 |
Minocycline hydrochloride (1 mg/kg) N = 315 |
Placebo N = 158 |
|
| Mean Percent Improvement in Inflammatory Lesions | 43.1% | 31.7% | 45.8% | 30.8% |
| No. (%) of Subjects Clear or Almost Clear on the EGSA* | 52 (17.3%) |
12 (7.9%) |
50 (15.9%) |
15 (9.5%) |
| *Evaluator's Global Severity Assessment | ||||
Minocycline hydrochloride did not demonstrate any effect on non-inflammatory lesions (benefit or worsening).
Last reviewed on RxList: 7/30/2012
This monograph has been modified to include the generic and brand name in many instances.
Additional Ximino Information
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