首个治疗银屑病及银屑病关节炎的口服药物：阿普斯特

Psoriatic arthritis (PsA) is a chronic inflammatory musculoskeletal disease related to psoriasis. About 75% of PsA patients develop psoriatic rash first, and most of them develop PsA 5 to 10 years later. About 15% of patients develop PsA first and then psoriatic rash, and about 10% of patients develop both at the same time. Psoriatic arthritis is associated with varying degrees of disability, and delayed diagnosis can also increase the risk of death. Therefore, early diagnosis and early treatment can prevent joint destruction and improve prognosis. It is an oral PDE4 inhibitor. In 2014, the drug was first approved for marketing in the United States under the trade name Otezla. It is the first oral preparation approved by the FDA for the treatment of plaque psoriasis (psoriasis) and psoriatic arthritis.

PDE4 is a PDE subtype that mainly exists in immune cells such as monocytes, T cells, and neutrophils. cAMP is an important second messenger in intracellular signal transduction and is involved in multiple processes of cell proliferation, apoptosis and inflammatory response. The PDE family is involved in the hydrolysis of cAMP. Apremilast blocks the degradation of cAMP in immune cells by inhibiting PDE4, ultimately reducing the inflammatory response of psoriasis and PsA.

In a 24-week clinical trial, 20% of PsA patients took Apremilast 20 mg orally, twice a day, and achieved ACR20, and 30 mg apremilast, twice a day, and 40% achieved ACR20, and the difference was statistically significant compared with the placebo group. 505 patients with active PsA received apremilast treatment. In the 16th week, 20 mg/time orally, twice/d, 29.4% of the patients in the group achieved ACR20, and 42.8% of the patients in the 30 mg/time, twice/d group, both showed that it is of great significance in the treatment of PsA.

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