阿普斯特(Apremilast)的适应症和临床效果？

The indications of Apremilast mainly include psoriasis, psoriatic arthritis, etc., and sometimes it can also be used to treat special types of oral ulcers. Apremilast has good clinical effects in treating related indications.

Apremilast is an antirheumatic drug (DMARD) indicated for the treatment of adult patients with active psoriatic arthritis (PsA) who have failed to respond to or are intolerant to previous DMARD therapy, as a single agent or in combination with other drugs, and for the treatment of moderate to severe chronic plaque psoriasis in adults who have failed to respond to, have contraindications to, or are intolerant to other systemic therapies including cyclosporine, methotrexate, or psoralen UVA (PUVA).

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It is an oral small molecule phosphodiesterase 4 (PDE4) inhibitor that was approved by the US Food and Drug Administration (FDA) and EMA in 2014 for the treatment of psoriasis and psoriatic arthritis.

Indications of Apremilast

1. Psoriasis:

Apremilast can regulate the production of inflammatory mediators such as tumor necrosis factor-α, reduce skin inflammatory response, thereby improving the symptoms of psoriasis patients. Patients can see significant improvement within a few weeks of taking the medication.

2. Psoriatic arthritis:

Apremilast can inhibit the enzyme activity of phosphodiacylase 4, reduce the release of inflammatory mediators, thereby reducing the condition of arthritis. Multiple studies have shown that Apremilast can significantly reduce pain and joint swelling, improve motor function, and improve quality of life in patients with psoriatic arthritis.

3. Special types of oral ulcers:

For example, in oral ulcers related to Behcet's disease, Apremilast can regulate the inflammatory response and immune system, reduce the release of inflammatory mediators, and promote the healing of ulcers. Treating mouth ulcers with Apremilast can speed up ulcer healing time and reduce recurrence rates.

In addition, Apremilast can also be used for skin diseases that are ineffective with conventional treatments, such as atopic dermatitis, alopecia areata, etc.

Clinical effect of Apremilast in the treatment of oral ulcers related to Te's disease

In Phase 2 and 3 trials of adults with this chronic debilitating disease, treatment with 30 mg of Apremilast twice daily for 12 weeks reduced the number and pain of oral ulcers and disease activity compared with placebo. These clinical benefits were accompanied by improvements in health-related quality of life.

The benefits of Apremilast were observed in Japanese patients regardless of baseline patient/disease characteristics and were sustained beyond 64 weeks of treatment. Apremilast provides an effective and well-tolerated treatment option for patients with oral ulcers associated with Behcet's disease.

Clinical application of Apremilast in the treatment of psoriasis

Study Purpose: To evaluate the impact of Apremilast 30 mg on the quality of life, efficacy and safety of patients with limited skin involvement who have plaque psoriasis manifestations in specific areas and impaired quality of life.

Research methods: In a phase 4, randomized, placebo-controlled, multinational study, 277 eligible patients with plaque psoriasis uncontrolled by topical therapy were enrolled and divided into the apremilast group (n=185) and the placebo group (n=92). 221 completed week 16, including the apremilast group (n=152) and the placebo group (n=69).

At week 16, significantly more patients receiving apremilast had a DLQI decrease of ≥4 points than those in the placebo group, with 73.3% in the apremilast group and 41.3% in the placebo group. At week 16, significantly greater improvements in affected body surface area (BSA) and PASI were observed with apremilast compared with placebo.

At week 16, Apremilast also showed significant improvements compared with placebo on the Numeric Rating Scale for Pruritus and the Visual Analogue Scale for Skin Discomfort/Pain, with a benefit index of ≥1 being better in 77% of patients compared with 40% in the placebo group.

Study conclusion: Apremilast significantly improved the skin-related quality of life of patients with plaque psoriasis in specific areas whose quality of life was severely impaired. Safety profile was consistent with previous apremilast studies.

Apostle's

The strength of Apremilast is 30 mg per tablet, titrate to the recommended dose of 30 mg twice daily according to the schedule below.

1. Day 1: 10mg in the morning.

2. Day 2: 10mg in the morning and 10mg in the evening.

3. Day 3: 10mg in the morning and 20mg in the evening.

4. Day 4: 20mg in the morning and 20mg in the evening.

5. Day 5: 20mg in the morning and 30mg in the evening.

6. Day 6 and beyond: 30mg twice a day.

Summary

As a new type of oral drug, Apremilast has significant effects on a variety of diseases. It treats and improves diseases by regulating the immune system and inflammatory response. For example, in the treatment of psoriasis, the drug has shown good results, reducing the area and severity of skin lesions, and can improve patients' skin symptoms, including erythema, scales and itching.

References:

1. Deeks ED. Apremilast: A Review in Oral Ulcers of Behçet's Disease. Drugs. 2020 Feb;80(2):181-188. doi: 10.1007/s40265-019-01253-3. PMID: 31933168.

2. Mrowietz U, Barker J, Conrad C, Jullien D, Gisondi P, Flower A, Reddy J, Paris M, Picard H, Jardon S, Augustin M. Efficacy and safety of apremilast in patients with limited skin involvement, plaque psoriasis in special areas and impaired quality of life: Results from the EMBRACE randomized trial. J Eur Acad Dermatol Venereol. 2023 Feb;37(2):348-355. doi: 10.1111/jdv.18689. Epub 2022 Nov 14. PMID: 36300769.

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