Apremilast: target synthetic drug for the treatment of psoriatic arthritis and psoriasis

Abstract

Apremilast (AP), a phosphodiesterase-4 inhibitor, is a novel drug for the treatment of psoriasis (Ps) and psoriatic arthritis (PsA). AP therapy affects the decrease in the activity of inflammatory changes due to reducing the level of proinflammatory cytokines. The clinical trials showed positive effects on Ps, for example ESTEEM 1 trial (Efficacy and Safety Trial Evaluating the Effects of apreMilast in psoriasis), in which AP therapy led to a decrease of PASI index in patients with moderate to severe plaque Ps: 75% improvement in PASI was significantly more frequent in patients taking AP at a dose of 30 mg twice daily (33%) than in patients receiving placebo (PL) (5%) (p = 0.0001) in 16 weeks. In the PALACE 1 study, 20% improvement in the ACR criteria (ACR20) was reported significantly more frequently at the 16th week of AP treatment in patients taking AP at 20 and 30 mg twice daily than in patients receiving PL (in 30.4%, 38.1% and 19% of cases, p = 0.0166 and p = 0.0001, respectively). After 52-week AP therapy, ACR20 was achieved in 63.0% of patients taking the drug at a dose of 20 mg twice a day, and in 54.6% of patients receiving 30 mg twice a day. According to the randomized controlled clinical trial (PALACE 1, 2, 3, 4), the most frequent adverse reactions (AR) included diarrhoea, nausea, headache, upper respiratory tract infections and nasopharyngitis. The most ARs were mild and moderate, and the frequency of discontinuation of therapy due to ARs was low. The PALACE studies, which enrolled 1493 patients, showed the efficacy and safety of AP in the treatment of PsA with moderate disease activity.