氘可来昔替尼是银屑病患者的新选择
Mechanism of action
It is an oral, selective, allosteric tyrosine kinase 2 (TYK2) inhibitor. TYK2 inhibitors are a new class of small molecules with a unique mechanism of action. TYK2 is an intracellular kinase that mediates the signaling of interleukin 23 (IL-23) and other cytokines involved in the pathogenesis of psoriasis. Deuterated colexitinib highly selectively binds to TYK2, thereby inhibiting IL-23, IL-12, and type 1 interferon (IFN) signaling and their downstream functions, and can control the inflammatory process of plaque psoriasis.
Among these subjects, the average proportion achieving PASI75 (more than 75% reduction in psoriasis area and severity index) at week 16 was 65.1%. Patients treated with deuterated colexitinib 6 mg once daily had a higher rate of PASI 75 remission and static Physician Global Assessment (sPGA) score of 0 or 1 compared with patients treated with apremilast 30 mg orally twice daily.
Deuterated colexitinib is the first oral TYK2 inhibitor approved for adult patients with moderate to severe plaque psoriasis who are suitable for systemic therapy or phototherapy, showing consistent efficacy and safety.
Dosage
The recommended dose of deuterated colexitinib is 6 mg once daily. If no improvement is seen after 24 weeks, discontinuation of treatment should be considered. No dose adjustment is required for elderly patients 65 years of age or older or patients with renal insufficiency, but due to limited clinical experience, patients over 75 years of age should take it with caution. No dose adjustment is required for mild or moderate hepatic impairment, and use is not recommended for severe hepatic impairment.
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