阿普斯特片是什么药？

It is an oral small molecule PDE-4 inhibitor. In 2014, the U.S. Food and Drug Administration (FDA) approved Apremilast as the first and only oral PDE4 small molecule inhibitor for the treatment of adult patients with moderate to severe plaque psoriasis who are suitable for phototherapy and systemic therapy. The original research company of Apremilast is Celgene of the United States, and the trade name on the market is Otezla.

What does Apremilast tablets do?

Apremilast is a novel oral, small molecule phosphodiesterase 4 (PDE4) inhibitor. Apremilast can inhibit PDE4 activity, increase intracellular cyclic adenosine monophosphate (cAMP) levels, further regulate the expression of tumor necrosis factor (TNF-α), I1-23 and other inflammatory cytokines, and ultimately inhibit the inflammatory response.

The efficacy of Apremilast tablets

Clinical studies on Apremilast include a small clinical observation and three phase II clinical trials and one phase III [1]. In this small-scale clinical study, 19 patients were enrolled, 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 tablets have been shown to successfully and safely treat some patients with psoriasis.

Adverse reactions of Apremilast tablets

PDE4 is also the major phosphodiesterase isoenzyme expressed in the central nervous system, so nausea and vomiting are common after drug use. The new PDE4 inhibitor, Apremilast, had fewer side effects and was well tolerated in phase I and II clinical studies. The most commonly reported adverse events were headache, nausea, and pharyngitis.

References

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

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