Finacea Information
Finacea (Azelaic) Description
Finacea (Azelaic) (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 C HO, 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 (Azelaic) 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.
Finacea (Azelaic) Clinical Pharmacology
The mechanism(s) by which azelaic acid interferes with the pathogenic events in rosacea are unknown.
Finacea (Azelaic) Clinical Studies
Finacea (Azelaic) Gel, 15%, was evaluated 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 (Azelaic) 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 evaluability 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
Primary efficacy assessment was based on the intent-to-treat (ITT) population with last observation carried forward (LOCF).
Both studies demonstrated a statistically significant difference in favor of Finacea (Azelaic) Gel, 15%, over its vehicle in reducing the number of inflammatory papules and pustules associated with rosacea (Table 1) and with success on the IGA in the ITT-LOCF population at the end of treatment.
Although some reduction of erythema which was present in patients with papules and pustules of rosacea occurred in clinical studies, efficacy for treatment of erythema in rosacea in the absence of papules and pustules has not been evaluated.
Finacea (Azelaic) Gel, 15%, was superior to the vehicle with regard to success based on the investigator's global assessment of rosacea on a 7-point static score at the end of treatment, (ITT population; Table 2).
Finacea (Azelaic) Indications And Usage
Finacea (Azelaic) Gel, 15%, is indicated for topical treatment of inflammatory papules and pustules of mild to moderate rosacea. Although some reduction of erythema which was present in patients with papules and pustules of rosacea occurred in clinical studies, efficacy for treatment of erythema in rosacea in the absence of papules and pustules has not been evaluated. Patients should be instructed to avoid spicy foods, thermally hot foods and drinks, alcoholic beverages and to use only very mild soaps or soapless cleansing lotion for facial cleansing.
Finacea (Azelaic) Contraindications
Finacea (Azelaic) Gel, 15%, is contraindicated in individuals with a history of hypersensitivity to propylene glycol or any other component of the formulation.
Finacea (Azelaic) Warnings
Finacea (Azelaic) Gel, 15%, is for dermatologic use only, and not for ophthalmic, oral or intravaginal use.
There have been isolated reports of hypopigmentation after use of azelaic acid. Since azelaic acid has not been well studied in patients with dark complexion, these patients should be monitored for early signs of hypopigmentation.
Finacea (Azelaic) Precautions
Contact with the eyes should be avoided. If sensitivity or severe irritation develops with the use of Finacea (Azelaic) Gel, 15%, treatment should be discontinued and appropriate therapy instituted.
In a transgenic mouse study, chronic use of Finacea (Azelaic) Gel led to an increased number of animals with papillomas at the treatment site (see PRECAUTIONS: ). The clinical relevance of the findings in animal studies to humans is not clear.
Systemic long-term animal studies have not been performed to evaluate the carcinogenic potential of azelaic acid. In a 26-week dermal carcinogenicity study using transgenic (Tg.AC) mice, Finacea (Azelaic) Gel, 15%, and the gel vehicle, when applied once or twice daily, did not increase the number of female Tg.AC animals with papillomas at the treatment site. No statistically significant increase in the number of animals with papillomas at the treatment site was observed in male Tg.AC animals after once daily application. After twice daily application, Finacea (Azelaic) Gel, 15%, and the gel vehicle induced a statistically significant increase in the number of male animals with papillomas at the treatment site when compared to untreated males. This suggests that the positive effect may be associated with the vehicle application. The clinical relevance of the findings in animals to humans is not clear.
Azelaic acid was not mutagenic or clastogenic in a battery of (Ames assay, HGPRT in V79 cells {Chinese hamster lung cells}, and chromosomal aberration assay in human lymphocytes) and (dominant lethal assay in mice and mouse micronucleus assay) genotoxicity tests.
Oral administration of azelaic acid at dose levels up to 2500 mg/kg/day (162 times the maximum recommended human dose based on body surface area) did not affect fertility or reproductive performance in male or female rats.
Finacea (Azelaic) Adverse Reactions
Overall, treatment related adverse events, including burning, stinging/tingling, dryness/tightness/scaling, itching, and erythema/irritation/redness, were 19.4% (24/124) for Finacea (Azelaic) Gel, 15%, and 7.1% (9/127) for the active comparator gel at 15 weeks.
In two vehicle controlled, and one active controlled U.S. clinical studies, treatment safety was monitored in 788 patients who used twice daily Finacea (Azelaic) Gel, 15%, for 12 weeks (N=333) or for 15 weeks (N=124), or the gel vehicle (N=331) for 12 weeks.
Finacea (Azelaic) Gel, 15%, and its vehicle caused irritant reactions at the application site in human dermal safety studies. Finacea (Azelaic) Gel, 15%, caused significantly more irritation than its vehicle in a cumulative irritation study. Some improvement in irritation was demonstrated over the course of the clinical studies, but this improvement might be attributed to subject dropouts. No phototoxicity or photoallergenicity were reported in human dermal safety studies.
In patients using azelaic acid formulations, the following additional adverse experiences have been reported rarely: worsening of asthma, vitiligo depigmentation, small depigmented spots, hypertrichosis, reddening (signs of keratosis pilaris), and exacerbation of recurrent herpes labialis.
Post-marketing safety-Skin: facial burning and irritation; Eyes: iridocyclitis on accidental exposure with Finacea (Azelaic) Gel, 15%, to the eye (see ).
Finacea (Azelaic) Overdosage
Finacea (Azelaic) Gel, 15%, is intended for cutaneous use only. If pronounced local irritation occurs, patients should be directed to discontinue use and appropriate therapy should be instituted (See ).
Finacea (Azelaic) Dosage And Administration
A thin layer of Finacea (Azelaic) Gel, 15%, should be gently massaged into the affected areas on the face twice daily, in the morning and evening. Patients should be reassessed if no improvement is observed upon completing 12 weeks of therapy.
Finacea (Azelaic) How Supplied
Finacea (Azelaic) Gel, 15%, is supplied in tubes in the following size:
Finacea (Azelaic) Gel, 15% – 50 g tube – NDC 10922-825-02
Store at 25°C (77°F); excursions permitted between 15–30°C (59–86°F) [see USP Controlled Room Temperature].
Distributed under license;
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© 2010, Intendis, Inc. All rights reserved. July 2010
Manufactured by Intendis Manufacturing S.p.A., Segrate, Milan, Italy
Distributed by:
IntendisMorristown, NJ 07962
Intendis is part of the Bayer Group
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Finacea (Azelaic)
