阿普斯特的作用机制及在银屑病中的应用

Introduction: Apremilast is an oral phosphodiesterase 4 (PDE4) inhibitor. Its mechanism of action mainly involves regulating intracellular signaling pathways, thereby exerting anti-inflammatory effects. Apremilast continues to have an important role in the treatment of psoriasis, particularly in providing patients with more treatment options. Apremilast can significantly improve skin lesions in patients with psoriasis, including reducing symptoms such as skin erythema, scale and itching.

The mechanism of action of Apremilast

It is a selective inhibitor of phosphodiesterase 4 (PDE4), which blocks the conversion of cyclic adenosine monophosphate (cAMP) into AMP, further leading to the accumulation of cyclic adenosine monophosphate (cAMP) in cells. Inhibition of PDE4 is selective for the innate immune response, leading to reduced production of inflammatory mediators such as CX-CL9, CX-CL10, IFN-γ, TNF-α, IL-2, IL-8, IL-12, and IL-23 and further reducing the inflammatory response. It has been reported that PDE4 inhibition reduces the inflammatory response to produce therapeutic effects and clinical improvement in psoriatic arthritis, plaque psoriasis, and Behcet's disease, but the specific mechanism of apremilast is unknown.

Contraindications

1. Subjects who have confirmed allergies to Apremilast or any component of the pharmaceutical preparation are contraindicated in treatment with Apremilast.

2. Reproductive studies in animal models during pregnancy have shown that treatment with Apremilast increases the risk of fetal miscarriage. To date, no reproductive studies of apremilast treatment during human pregnancy have been reported. Pregnancy planning and prevention is recommended for women of childbearing potential. It is recommended that women of childbearing potential use contraception during treatment with Apremilast.

3. Breastfeeding women are contraindicated in receiving treatment.

4. It is also prohibited to receive live vaccines while receiving Apremilast treatment to avoid reducing the therapeutic effect of the vaccine.

Apremilast in Psoriasis

The efficacy of Apremilast in moderate to severe psoriasis has been confirmed in pivotal trials, in the The 16-week PASI-75 response rate was 30%, and this effect lasted until week 52, improving the patient's quality of life and achieving rapid improvement in pruritus. Apremilast has shown good safety and tolerability in both clinical trials and clinical practice series. Two phase III randomized controlled trials showed that apremilast significantly improved psoriasis lesions, including scalp and nail lesions, after 16 weeks of treatment. In addition, a phase III RCT also showed that apremilast treatment for 16 weeks was significantly more effective in treating PsA than placebo.

Adverse reactions

The most common adverse reactions of Apremilast are diarrhea, nausea, upper respiratory tract infection, nasopharyngitis, tension headache, and headache. The incidence of adverse events recorded in clinical practice series is lower compared with clinical trials. After adverse reactions occur, you can consult a medical practitioner to determine whether treatment is needed.