阿普斯特:为银屑病患者提供新的治疗选择

Introduction: Apremilast is an oral phosphodiesterase 4 (PDE4) inhibitor that provides a new treatment option for patients with psoriasis. Apremilast exerts anti-inflammatory and anti-psoriasis effects by inhibiting the activity of PDE4 enzyme and regulating intracellular signaling pathways. Studies have shown that Apremilast can significantly improve the symptoms of psoriasis patients, including skin redness, scales and itching. In addition, Apremilast can also improve the quality of life of patients and reduce the psychological impact of psoriasis on patients.

Indications

It is a small molecule phosphodiesterase 4 (PDE4) inhibitor approved by the FDA for the treatment of plaque psoriasis in adult patients who are candidates for phototherapy or systemic therapy, and psoriatic arthritis in adult patients with moderately to severely active disease. Apremilast is the first and only oral drug approved by the FDA for the treatment of oral ulcers associated with Behcet's disease. Apremilast is also used off-label to treat a variety of skin diseases that are unresponsive or ineffective to conventional therapies (systemic corticosteroids or immunosuppressants), including hidradenitis suppurativa, atopic dermatitis, and alopecia areata.

The efficacy of Apremilast in the treatment of psoriasis

The efficacy of Apremilast in the treatment of psoriasis was evaluated in two multicenter, randomized, double-blind, placebo-controlled Phase 3 trials of comparable design, in which patients were randomized to receive Apremilast 30 mg twice daily or placebo for 16 weeks. In both studies, 33% of patients in the apremilast group achieved PASI-75 remission at week 16, which was significantly higher than the 5% in the placebo group. Significantly more patients receiving apremilast had an sPGA score of 0 or 1 compared with placebo. Apremilast also achieved significant results in terms of percentage change from baseline in affected BSA and PASI scores and percentage of patients achieving PASI-50.

The titration schedule helps prevent adverse gastrointestinal side effects that may occur during the first few weeks of initial treatment. If the patient has impaired renal function (CrCl <30 mL/min), the dose is 10 mg on days 1-3, 20 mg on days 4 and 5, and maintenance therapy is 30 mg once daily in the morning thereafter. If a dose is missed, patients are advised to discuss with their doctor and pharmacist when to take Apremilast.