[Mechanism of action of tezepelumab (TEZSPIRE®) and clinical trial results in |asthma].

ABSTRACT

Tezepelumab (TEZSPIRE® Subcutaneous Injection 210 |mg), a biologic medicine with a novel mechanism, was approved in Japan in September 2022 for the treatment of bronchial asthma. Tezespire auto-injector was approved in Japan in August 2023 as an additional dosage. It is indicated for severe or refractory patients whose asthmatic symptoms cannot be controlled by currently available treatment. Tezepelumab binds to the epithelial cytokine thymic stromal lymphopoietin (TSLP) and disrupts TSLP signaling via the heterodimeric receptor. In the Phase 3 NAVIGATOR trial, the annual asthma exacerbation rate was significantly reduced by tezepelumab when administered subcutaneously every 4 weeks over a 52-week period to patients with uncontrolled, severe asthma who had received medium- or high-dose inhaled glucocorticoids. Its efficacy in reducing asthma exacerbations was observed regardless of blood eosinophil (bEOS) count, fractional exhaled nitric oxide (FeNO) levels, or serum total IgE at baseline. Significant improvements were noted in lung function, health-related quality of life, and change from baseline in asthma control. Reductions in the levels of inflammatory biomarkers (bEOS, FeNO, and IgE) was also noted. Clinical pharmacology trials demonstrated the efficacy of tezepelumab in improving airway hyperresponsiveness. In this article, we reviewed pharmacological characteristics, pharmacokinetics, clinical efficacy, and the safety profile of tezepelumab.