Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC 50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research

2023年6月29日 · Cilofexor (GS-9674) 是一款 Gilead Sciences 开发用于原发性硬化性胆管炎 (PSC) 和非酒精性脂肪性肝炎 (NASH)治疗的口服使用非甾体类法尼索X受体（FXR）激动剂。 此前在没有肝硬化的原发性硬化性胆管炎（PSC）患者中进行的一项 phase 2期试验表明，使用非甾 …

In a phase II double-blind, placebo-controlled study, we tested the safety and efficacy of cilofexor (formerly GS-9674), a nonsteroidal farnesoid X receptor agonist in patients without cirrhosis with large-duct PSC. Patients were randomized to receive cilofexor 100 mg (n = 22), 30 mg (n = 20), or placebo (n = 10) orally once daily for 12 weeks.

Cilofexor (also known as GS-9674) is a nonsteroidal farnesoid X receptor (FXR) agonist in clinical trials for the treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), [1] [2] [3] and primary sclerosing cholangitis (PSC).

2023年3月15日 · Cilofexor (formerly GS-9674) is a potent and selective nonsteroidal FXR agonist . In preclinical models of liver fibrosis, cilofexor demonstrated anti-inflammatory and antifibrotic effects, reducing hepatic fibrosis and portal hypertension [ 28 , 29 ].

Background and aims: We evaluated the safety and efficacy of cilofexor (formerly GS-9674), a small-molecule nonsteroidal agonist of farnesoid X receptor, in patients with nonalcoholic steatohepatitis (NASH).

2022年8月4日 · The nonsteroidal farnesoid X receptor agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with primary sclerosing cholangitis

Cilofexor(GS-9674) 是一种强效、选择性口服法呢醇 X 受体 (FXR)激动剂，EC50 为 43 nM。 它在临床前肝纤维化模型中表现出抗炎、抗纤维化作用和降低门脉压力，对原发性硬化性胆管炎 (PSC) 和非酒精性脂肪性肝炎 (NASH) 研究显示出潜在的治疗益处。

背景与目的我们评估了非酒精性脂肪性肝炎（NASH）患者cilofexor（原名GS-9674）（一种法呢类X受体的小分子非甾体激动剂）的安全性和有效性。 方法和结果在这项双盲，安慰剂对照的2期临床试验中，通过磁共振成像诊断的140例非肝硬化性NASH患者的质子密度脂肪分数（MRI-PDFF）≥8％，磁共振测得的肝硬度≥2.5kPa弹性成像（MRE）或历史肝活检被随机分配，接受口服头孢克索100 mg（n = 56），30 mg（n = 56）或安慰剂（n = 28），每天一次，持续24周 …

Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC 50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.