Vaniqa Ingredients and Composition
Vaniqa is a cream containing 13.9% (139 mg/g) of anhydrous eflornithine hydrochloride as eflornithine hydrochloride monohydrate (150 mg/g).
Other ingredients include: ceteareth-20, cetearyl alcohol, dimethicone, glyceryl stearate, methylparaben, mineral oil, PEG-100 stearate, phenoxyethanol, propylparaben, stearyl alcohol and water.
Vaniqa Structural Formula and Composition
Chemically, eflornithine hydrochloride is (+) -2-(difluoromethyl) ornithine monohydrochloride monohydrate, with the empirical formula C6H12F2N2O2• HCl•H2O, a molecular weight of 236.65 and the structural formula shown.
Anhydrous eflornithine hydrochloride has an empirical formula C6H12F2N2O2•HCl and a molecular weight of 218.65.
Clinical Pharmacology: Pharmacodynamics
There are no studies examining the inhibition of the enzyme ornithine decarboxylase (ODC) in human skin following the application of topical eflornithine. However, there are studies in the literature that report the inhibition of ODC activity in skin following oral eflornithine. It is postulated that topical eflornithine hydrochloride irreversibly inhibits skin ODC activity. This enzyme is necessary in the synthesis of polyamines. Animal data indicate that inhibition of ornithine decarboxylase inhibits cell division and synthetic functions, which affect the rate of hair growth. Vaniqa (eflornithine hydrochloride) Cream, 13.9% has been shown to retard the rate of hair growth in non-clinical and clinical studies.
Clinical Pharmacology: Pharmacokinetics
The mean percutaneous absorption of eflornithine in women with unwanted facial hair, from a 13.9% w/w cream formulation, is < 1% of the radioactive dose, following either single or multiple doses under conditions of clinical use, that included shaving within 2 hrs before radiolabeled dose application in addition to other forms of cutting or plucking and tweezing to remove facial hair. Steady state was reached within four days of twice-daily application. The apparent steady-state plasma t1/2 of eflornithine was approximately 8 hours. Following twice-daily application of 0.5 g of the cream (total dose 1.0 g/day; 139 mg as anhydrous eflornithine hydrochloride), under conditions of clinical use in women with unwanted facial hair (n=10), the steady-state Cmax, Ctrough and AUC12hr were approximately 10 ng/mL, 5 ng/mL, and 92 ng•hr/mL, respectively, expressed in terms of the anhydrous free base of eflornithine hydrochloride. At steady state, the dose-normalized peak concentrations (Cmax) and the extent of daily systemic exposure (AUC) of eflornithine following twice-daily application of 0.5 g of the cream (total dose 1.0 g/day) is estimated to be approximately 100- and 60-fold lower, when compared to 370 mg/day once-daily oral doses. This compound is not known to be metabolized and is primarily excreted unchanged in the urine.