On the issue of the effectiveness and bioequivalence of isotretinoin Lidose

Abstract

BACKGROUND: Acne is one of the most common types of dermatoses. Systemic isotretinoin treatment, which affects all mechanisms of acne pathogenesis, is the most effective drug for severe acne treatment. This study presents scientific data on the innovative formulation of isotretinoin for acne treatment using the patented Lidose technology. The use of lidose isotretinoin allows for the reduction of the amount of isotretinoin used by the patient by 20% without losing its therapeutic effectiveness. AIM: This study aimed to analyze comparative studies of bioavailability and relevant pharmacokinetic parameters, which made it possible to prove that initial dosages of 8 and 16 mg of lidose isotretinoin (Aknecutan) are bioequivalent to 10 and 20 mg of the usual isotretinoin preparations. The study also aimed to evaluate the efficacy and safety of the drug. MATERIALS AND METHODS: Over the past 7 years, 1044 patients (women, n = 651, 62.4%; men, n = 393, 37.6%) have received acne treatment using new formulations of isotretinoin (lidose isotretinoin, Aknecutan) for moderate to severe acne at a daily dose of 0.4–0.8 per 1 kg of body weight with a total drug dose of 100–120 mg/kg per course of therapy. RESULTS: The study demonstrated the bioequivalence of 8 and 10 mg lidose isotretinoin (Aknecutan) to the usual preparations of 10 and 20 mg isotretinoin, respectively. After therapy, clinical remission was achieved in all patients, which required 7–12 months of treatment, depending on the daily drug dose. Among the side effects, cheilitis and retinoic dermatitis of the face was observed, which were completely resolved by use of moisturizing creams and moisturizing sticks. An increase in the levels of liver enzymes, triglycerides, and lipoproteins was observed in 5–10% of patients, which did not exceed 20–30% of the norm and did not require discontinuation of therapy. After the treatment, these indicators returned to normal levels. Other side effects were extremely rare. Notably, disease relapses are most often caused by a low total dose of the drug or the presence of endocrinological and gynecological diseases. CONCLUSION: The innovative lidose isotretinoin is one of the most highly effective and safe systemic retinoids for the treatment of moderate to severe acne. Comparative studies of bioavailability and corresponding pharmacokinetic parameters have demonstrated the bioequivalence of the new formulation of isotretinoin (Aknecutan) for acne treatment, which fully corresponds to that of the original preparation.