阿普斯特片治疗银屑病效果怎样？

The treatment of psoriasis is effective.

Apremilast is an oral selective small molecule phosphodiesterase 4 (PDE4) inhibitor that can regulate pro-inflammatory factors and anti-inflammatory factors and restore immune balance in the body. Patients have higher medication compliance, avoiding the difficulty of clinical management and uncontrollable adverse reactions of traditional treatment methods; oral administration is safer, with mild adverse reactions, and can effectively improve the quality of life of psoriasis patients.

About Apremilast Tablets

Apremilast Tablets is the first oral phosphodiesterase-4 (PDE4) inhibitor for the treatment of rheumatoid arthritis and psoriasis. It was first approved for marketing in the United States in 2014 and in Europe in 2015. PDE4 can promote the hydrolysis of cyclic adenosine monophosphate (cAMP), an important second messenger that regulates inflammatory responses, into nucleoside 5-monophosphate (AMP). Inhibiting PDE4 can prevent the hydrolysis of cAMP into AMP, leading to an increase in intracellular cAMP levels and affecting multiple downstream pathways.

For more information about Apremilast tablets, please refer to: This film article also details other information about Apremilast tablets.

The role of Apremilast tablets

Apremilast tablets are a PDE4 inhibitor with the following mechanism of action and characteristics:

1. Inhibit PDE4: Apremilast tablets block the degradation of cAMP by inhibiting phosphodiesterase 4 (PDE4), thereby increasing intracellular cAMP levels.

2. Activation of protein kinase A: After the intracellular cAMP level increases, cAMP-dependent protein kinase A is activated, which in turn promotes the phosphorylation of cAMP response $ binding protein.

3. Inhibit the transcriptional activity of NF-kB: Activating the phosphorylation state of transcription factor-1 can inhibit the transcriptional activity of nuclear factor-kB (NF-kB) and reduce the production of pro-inflammatory factors.

4. Anti-inflammatory effect: Through the above mechanism, Apremilast tablets can reduce the synthesis of pro-inflammatory factors (such as TNF-α, IL-2, IL-12, IL-23) and inflammatory chemokines (such as CXCL9, CXCL10), thereby producing anti-inflammatory effects.

5. Reduce the synthesis of TNF-α: In vitro experimental studies have shown that Apremilast tablets can also reduce the synthesis of TNF-α in peripheral blood mononuclear cells, keratinocytes and natural killer (NK) cells, further reducing the inflammatory response.

The effect of Apremilast tablets in the treatment of psoriasis

Clinical research on Apremilast tablets includes a small clinical observation, three phase II clinical trials and one phase III clinical trial.

In this small clinical study, there were 19 patient groups, 17 of whom completed the trial. On the 29th day of treatment, the epidermal thickness decreased by an average of 20.5% compared with baseline. In responding cases, dermal and epidermal T cells decreased by 28.8% and 42.6%, respectively, and CD11c cells decreased by 18.5% and 40.2%, respectively. Fourteen of 19 (73.7%) patients demonstrated improvement in psoriasis area and severity (PASI) scores. Apremilast has been shown to successfully and safely treat some psoriasis patients.

The first Phase II clinical trial was a 12-week, multi-center, double-blind, placebo-controlled, parallel group, dose comparison study [1]. 259 patients with moderate and severe psoriasis were randomly divided into a placebo group, apremilast 20mg QD group or apremilast 20mg BID group at a ratio of 1:1:1. The results showed that more subjects (24.4%) in the apremilast 20 mg BID group achieved the goal of a ≥75% reduction in the Psoriasis Area and Severity Index (PASI-75), which was a significant difference compared with 10.3% on placebo (P=0.023). Both the apremilast 20 mg QD group and the placebo group achieved PASI-75 at 12 weeks, 9/87 (10.3%). At 12 weeks, the psoriasis area and severity (PASI) score decreased from baseline by 17.4% in the placebo group, 30.3% in the apremilast 20 mg QD group (P = 0.021 compared with placebo), and 52.1% in the apremilast 20 mg BID group (P < 0.001 compared with placebo).

Summary

The advantages of apremilast are:

1. Effective in both PsA and psoriasis: apremilast has shown significant efficacy in the treatment of psoriatic arthritis (PsA) and psoriasis, and can effectively relieve symptoms and improve patients' quality of life.

2. Oral administration to improve patient compliance: apremilast is administered orally, which is more convenient than injection or intravenous administration and can improve patients' medication compliance.

3. No increased risk of tuberculosis or opportunistic infections was found: In clinical trials, apremilast was not found to increase the risk of tuberculosis or opportunistic infections and is relatively safe.

4. No laboratory pre-screening or continuous monitoring is required: Compared with some other drugs, apremilast does not require continuous monitoring of laboratory parameters when used, reducing patient inconvenience.

5. Short half-life, treatment can be interrupted in time: apremilast has a short half-life, making it easier for patients to interrupt treatment if necessary during treatment.

It should be noted that due to the large individual differences between PsA patients, individualized treatment principles should be followed during treatment, and personalized treatment should be carried out based on the patient's specific situation, disease severity, drug response and other factors.

References

[1]Li Lei, Li Xinfang. Research progress of phosphodiesterase inhibitor apremilast in the treatment of psoriasis [J]. Chinese Medical Science, 2017, 7(14): 25-28.

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