近日，吉利德宣布，欧盟委员会（EC）已有条件批准Seladelpar上市，与熊去氧胆酸（UDCA）联用，治疗对UDCA单药应答不足的原发性胆汁性胆管炎（PBC）患者；或者作为单药，治疗对UDCA治疗不耐受的PBC患者。Seladelpar是目前首个且唯一在生化反应、碱性磷酸酶正常化以及瘙痒缓解等方面，相较于安慰剂均取得显著改善效果的疗法。

Current endogenous or synthetic FXR antagonists, such as glyco-ursodeoxycholic acid, target the LBP by competitively blocking the binding of FXR-activating bile acids like chenodeoxycholic acid ...

In this study, the authors first used an AlphaScreen assay to identify a series of tryptophan-based cyclic peptide compounds with FXR-antagonistic activity, specifically those modified with a ...

UDCA has, therefore, been evaluated for the treatment of patients with PSC. Trials of UDCA at low doses (10–15 mg/kg per day and 17–20 mg/kg per day) have yielded inconclusive results in ...

Ocaliva is approved in combination with UDCA in adults who have not responded ... Ocaliva is a potent and selective agonist of the farnesoid X receptor (FXR), which is expressed at high levels ...