Know all about the functions and effects of Apremilast/Apremilast tablets, so you can use the medicine more wisely!

Apremilast is an oral phosphodiesterase 4 (PDE4) inhibitor. It is mainly used to treat moderate to severe silver plaque psoriasis, psoriatic arthritis (PSA) and has been gradually expanded to other inflammatory immune diseases in recent years. This drug was developed by the American company Celgene and was approved by the FDA in 2014. Its unique mechanism of action and relatively mild safety make it an important bridge between traditional immunosuppressants and biological agents, and it plays an increasingly critical role in the management of chronic inflammatory diseases.

From a pharmacological mechanism, apremilast inhibits the activity of intracellular PDE4 enzymes and regulates cAMP (cyclic adenosine monophosphate) levels, thereby indirectly reducing the release of pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α), interleukins (IL-23, IL-17), etc., while also enhancing the expression of anti-inflammatory factors such as IL-10. This mechanism is different from the "global suppression" of traditional immunosuppressive drugs. It is a "targeted regulatory" anti-inflammatory method, so it can effectively alleviate inflammation without significantly inhibiting the overall function of the immune system. Because of this, it has shown better clinical safety and tolerance, especially for patients who are not suitable for the use of biologics or who do not respond well to other drugs.

In terms of psoriasis treatment, Apremilast has been included in the treatment guidelines of many countries and is suitable for patients with moderate to severe plaque psoriasis who cannot receive phototherapy or systemic treatment, or who are ineffective or intolerant to other drugs. Multiple randomized controlled clinical trials have shown that after 16 weeks of continuous treatment with apremilast, patients can achieve a significant clinical response of PASI 75 (skin lesions improved by 75%), and some patients can further achieve PASI 90 or close to complete clearance. Compared with traditional methotrexate or cyclosporine drugs, apremilast is less likely to cause liver and kidney toxicity and does not require intensive laboratory monitoring. It is particularly important for the management of long-term chronic diseases. In addition, studies have shown that the drug is also effective in treating refractory psoriasis subtypes such as itching, scalp psoriasis, and skin lesions on hands and feet.

In terms of psoriatic arthritis (PsA), the efficacy of apremilast has also been verified in multiple phase III clinical trials. Not only does it relieve joint pain and swelling, it also improves physical function and quality of life and slows the progression of joint destruction. Compared with nonsteroidal anti-inflammatory drugs (NSAIDs) or conventional DMARDs (such as leflunomide), apremilast is an oral targeted small molecule drug suitable for patients who wish to avoid injection therapy. It is easy to use and has high feasibility of long-term management, and is especially suitable for patients with mild to moderate active arthritis or those who cannot receive biological agents.

In addition to psoriasis and psoriatic arthritis, Apremilast has also been explored internationally for the treatment of other chronic inflammatory diseases, such as Behcet's disease, oral ulcers, scleroderma, atopic dermatitis, ulcerative colitis, etc. In Behcet's disease, the U.S. FDA has approved it for the treatment of recurrent oral ulcers, and real-world studies in multiple regions have shown that it can reduce the frequency of recurrences, relieve pain, and greatly improve patients' quality of life. In areas such as inflammatory bowel disease, it is still in the clinical research stage, but early data shows its potential for regulating mucosal inflammation.

Reference materials:https://go.drugbank.com/drugs/DB05676