FINACEA- azelaic acid gel
FINACEA- azelaic acid
Intendis Inc.
Finacea®
(azelaic acid) Gel, 15%
For Dermatologic Use Only-Not for Ophthalmic, Oral, or Intravaginal Use
Rx only
DESCRIPTION
FINACEA® (azelaic acid) Gel, 15%, contains azelaic acid, a naturally occurring saturated dicarboxylic acid. Chemically, azelaic acid is 1,7-heptanedicarboxylic acid, with the molecular formula C9 H16 O4, a molecular weight of 188.22, and the structural formula:
Azelaic acid is a white, odorless crystalline solid that is poorly soluble in water at 20°C (0.24%), but freely soluble in boiling water and in ethanol.
Each gram of FINACEA Gel, 15%, contains 0.15 gm azelaic acid (15% w/w) as the active ingredient in an aqueous gel base containing benzoic acid (as a preservative), disodium EDTA, lecithin, medium-chain triglycerides, polyacrylic acid, polysorbate 80, propylene glycol, purified water, and sodium hydroxide to adjust pH.
CLINICAL PHARMACOLOGY
The mechanism(s) by which azelaic acid interferes with the pathogenic events in rosacea are unknown.
Pharmacokinetics:
The percutaneous absorption of azelaic acid after topical application of FINACEA Gel, 15%, could not be reliably determined. Mean plasma azelaic acid concentrations in rosacea patients treated with FINACEA Gel, 15%, 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 patients treated with vehicle only. This indicates that FINACEA Gel, 15%, 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 20% cream after topical application. Azelaic acid is mainly excreted unchanged in the urine, but undergoes some ß-oxidation to shorter chain dicarboxylic acids.
CLINICAL STUDIES
FINACEA Gel, 15%, was eva luated for the treatment of mild to moderate papulopustular rosacea in 2 clinical trials comprising a total of 664 (333 active to 331 vehicle) patients. Both trials were multicenter, randomized, double-blind, vehicle-controlled 12-week studies with identical protocols. Overall, 92.5% of patients were Caucasian and 73% of patients were women, and the mean age was 49 (range 21 to 86) years. Enrolled patients had mild to moderate rosacea with a mean lesion count of 18 (range 8 to 60) inflammatory papules and pustules. Subjects without papules and pustules, with nodules, rhinophyma, or ocular involvement, and a history of hypersensitivity to propylene glycol or to any other ingredients of the study drug were excluded. FINACEA Gel, 15%, 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 eva luability was to be used during the studies. Patients were instructed to avoid spicy foods, thermally hot foods and drinks, and alcoholic beverages during the study, and to use only very mild soaps or soapless cleansing lotion for facial cleansing.
The primary efficacy endpoints were both
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1.
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change from baseline in inflammatory lesion counts and
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2.
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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):
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CLEAR:
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No papules and/or pustules; no or residual erythema; no or mild to moderate telangiectasia
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MINIMAL:
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Rare papules and/or pustules; residual to mild erythema; mild to moderate telangiectasia
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MILD:
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Few papules and/or pustules; mild erythema; mild to moderate telangiectasia
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MILD TO MODERATE:
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Distinct number of papules and/or pustules; mild to moderate erythema; mild to moderate telangiectasia
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MODERATE:
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Pronounced number of papules and/or pustules; moderate erythema; mild to moderate telangiectasia
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MODERATE TO SEVERE:
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Many papules and/or pustules, occasionally with large inflamed lesions; moderate erythema; moderate degree of telangiectasia
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SEVERE:
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Numerous papule |
