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更新于：2026-09-05
Cilofexor tromethamine
更新于：2026-09-05
概要
基本信息
在研机构- |
最高研发阶段终止临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C32H33Cl3N4O8 |
InChIKeyCUWTTWVBVUZPAP-UHFFFAOYSA-N |
CAS号2253764-93-9 |
关联
12
项与 Cilofexor tromethamine 相关的临床试验NCT04060147
A Proof-of-Concept, Open-Label Study Evaluating the Safety and Tolerability of Cilofexor in Subjects With Primary Sclerosing Cholangitis (PSC) and Compensated Cirrhosis
NCT03987074
A Proof of Concept, Open-Label Study Evaluating the Safety, Tolerability, and Efficacy of Monotherapy and Combination Regimens in Subjects With Nonalcoholic Steatohepatitis (NASH)
ACTRN12619000655145
A Phase 1 Open-Label, Parallel-Group, Two-Treatment, Single-Dose Study to Evaluate the Pharmacokinetics of GS-9674 and GS-0976 in Subjects with Normal Renal Function and Severe Renal Impairment
100 项与 Cilofexor tromethamine 相关的临床结果
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100 项与 Cilofexor tromethamine 相关的转化医学
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100 项与 Cilofexor tromethamine 相关的专利（医药）
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75
项与 Cilofexor tromethamine 相关的文献（医药）2026-04-01Liver International
An Update on Bile Acid‐Regulated Signalling in the Pathogenesis of Metabolic Dysfunction‐Associated Steatotic Liver Disease
Review
作者: Wang, Li ; Wen, Yi ; Wang, Lu ; Wang, Hong‐Lian ; Chen, Chen ; Zhao, Chang‐Ying ; Shi, Jiang‐Shan ; Wu, Li‐Juan
ABSTRACT:
Metabolic dysfunction‐associated steatotic liver disease (MASLD) is a common metabolic disorder with rising global incidence without effective treatment. Emerging evidence highlights bile acids (BAs) as pivotal signalling molecules that modulate genes involved in their own metabolism and lipid homeostasis in hepatic and extrahepatic tissues, thereby influencing MASLD pathogenesis. These regulatory effects are primarily driven by the activation of nuclear receptors, including the farnesoid X receptor (FXR), vitamin D receptor (VDR), pregnane X receptor (PXR), and by the membrane‐bound G protein‐coupled receptors such as Takeda G protein‐coupled receptor 5 (TGR5) and sphingosine‐1‐phosphate receptor 2 (S1PR2). The distinct roles of these BA receptor‐dependent signalling pathways in lipid homeostasis underscore their importance in MASLD development. Pharmacological strategies targeting BA‐regulated pathways, particularly the FXR activation, have shown promise in MASLD treatment. Several FXR agonists, including obeticholic acid (OCA), cilofexor, and tropifexor, have progressed to clinical trials, demonstrating potential therapeutic efficacy. Additionally, recent studies identified several natural compounds—such as hyperoside, kaempferol, and salidroside—that exhibited direct or indirect FXR‐modulating properties, suggesting their potential utility for novel anti‐MASLD drug development. Further research into BA signalling mechanisms and the exploration of targeted therapies may provide novel and effective MASLD therapy.
2026-04-01ALIMENTARY PHARMACOLOGY & THERAPEUTICS
Network Meta‐Analysis: Comparison of Pharmacological Therapies in Compensated Metabolic Dysfunction‐Associated Steatohepatitis Cirrhosis for Fibrosis Regression and
MASH
Resolution
Review
作者: Al‐Sharif, Lubna ; Antunes, Vanio L. J. ; Huang, Daniel Q. ; Souza, Matheus ; Loomba, Rohit ; Wong, Shi Yin
ABSTRACT:
Background and Aims:
The burden of metabolic dysfunction‐associated steatohepatitis (MASH) cirrhosis is rapidly rising globally. There are several therapeutic agents under clinical development for the treatment of cirrhosis due to MASH; however, their relative efficacy has not been systematically assessed. This systematic review and network meta‐analysis was performed to compare the histological efficacy of available therapeutic agents for compensated MASH cirrhosis.
Methods:
PubMed and Cochrane Library databases were searched from inception to May 25, 2025, for randomised controlled trials (RCTs) evaluating pharmacological treatments in patients with biopsy‐proven compensated MASH cirrhosis (F4c). The primary endpoint was fibrosis regression of at least one stage without MASH worsening, and the secondary endpoint was MASH resolution. Treatment comparisons were conducted via network meta‐analysis, and ranking probabilities were estimated using the surface under the cumulative ranking (SUCRA) curve analysis.
Results:
Nine RCTs with 3266 participants met the eligibility criteria. Efruxifermin was the only intervention significantly superior to placebo for ≥ 1‐stage fibrosis improvement without worsening of MASH. The highest‐ranked interventions for fibrosis improvement were efruxifermin (SUCRA: 77.44), cilofexor + firsocostat (SUCRA: 72.38) and aldafermin (SUCRA: 71.27). For MASH resolution, efruxifermin, semaglutide + cilofexor + firsocostat and semaglutide were significantly superior to placebo. Efruxifermin (SUCRA: 81.38), semaglutide + cilofexor + firsocostat (SUCRA: 74.07) and semaglutide (SUCRA: 63.88) had the highest probability of ranking best for MASH resolution.
Conclusion:
This network meta‐analysis provides relative rank‐order estimates of the histological efficacy of available pharmacological therapies for compensated MASH cirrhosis. These data may have implications for the design of future clinical trials.
2026-01-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
FXR-targeted drug discovery: Recent advances and therapeutic perspectives
Review
作者: Zhou, Xiangyang ; Cao, Yu ; Shan, Lianhai ; Mao, Wu-Yu ; Shang, Weidong ; Li, Qian ; Liu, Zihang
Farnesoid X Receptor (FXR), a pivotal member of the nuclear receptor superfamily, plays a central role in the regulation of crucial physiological processes. These processes encompass bile acid homeostasis, inflammatory responses, fibrosis, as well as lipid and glucose metabolism. Given its extensive physiological functions, FXR has become an extremely promising therapeutic target for bile acid metabolism disorders. In recent years, the progress in medicinal chemistry has significantly expedited the development of FXR agonists. In 2016, obeticholic acid (OCA) received approval from FDA for marketing. As the first small-molecule drug targeting FXR for primary biliary cholangitis (PBC), its approval has spurred the advancement of multiple FXR agonists with diverse chemical structures into clinical trials. Notable candidates include Tropifexor (for non-alcoholic steatohepatitis, NASH), Cilofexor (for PBC), and Nidufexor (for diabetic nephropathy). This review delineates the structural features and biological functions of FXR, analyzes molecular mechanisms underpinning its signal transduction pathways and disease pathogenesis, and highlights molecular design strategies and structure-activity relationship (SAR) advancements in FXR agonists. These insights aim to provide a theoretical foundation for rationally designing novel, potent FXR agonists.
107
项与 Cilofexor tromethamine 相关的新闻（医药）2026-08-05
100 项与 Cilofexor tromethamine 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 原发性硬化性胆管炎 | 临床3期 | 美国 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 日本 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 澳大利亚 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 奥地利 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 比利时 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 加拿大 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 丹麦 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 芬兰 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 法国 | 2019-03-27 | |
| 原发性硬化性胆管炎 | 临床3期 | 德国 | 2019-03-27 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 416 | 獵醖範遞鏇遞觸選範淵(衊衊簾鏇蓋構簾觸壓選) = The most common adverse events were pruritus (cilofexor: 136 [49%] of 277 patients; placebo: 50 [36%] of 139 patients; grade 3 or higher in 11 [4%] patients in the cilofexor group and one [1%] patient in the placebo group), COVID-19 (cilofexor: 65 [23%]; placebo: 26 [19%]), and upper abdominal pain (cilofexor: 40 [14%]; placebo 20 [14%]). 獵網繭遞蓋廠糧願艱築 (齋衊醖壓獵膚積廠構遞 ) | 不佳 | 2026-01-01 | |||
Placebo | |||||||
临床3期 | 416 | 廠繭網簾鏇鬱網蓋壓艱(醖鬱製繭觸範衊壓醖遞) = The most common adverse events were pruritus (cilofexor: 136 [49%] of 277 patients; placebo: 50 [36%] of 139 patients; grade 3 or higher in 11 [4%] patients in the cilofexor group and one [1%] patient in the placebo group), COVID-19 (cilofexor: 65 [23%]; placebo: 26 [19%]), and upper abdominal pain (cilofexor: 40 [14%]; placebo 20 [14%]). 衊廠繭夢鬱選襯齋壓獵 (製獵夢衊鬱鬱鏇夢膚淵 ) | 不佳 | 2025-10-01 | |||
Placebo | |||||||
临床1期 | 11 | 遞製衊糧鬱遞築艱鑰構(壓蓋顧齋憲選蓋構構築) = fatigue (2/11 [18.2%]) 壓獵蓋壓糧觸壓糧鹹淵 (蓋鏇鹽壓繭壓願觸鹽鏇 ) 更多 | 积极 | 2024-07-01 | |||
临床3期 | 419 | (Cilofexor 100 mg (Blinded Phase)) | 糧淵鹹壓夢鬱顧遞選積 = 憲齋憲窪構醖廠壓鏇鹹 鹽簾糧鑰製衊構鏇襯製 (鑰憲製網築製壓範糧襯, 糧觸鬱鑰衊積糧鑰膚鑰 ~ 膚憲糧窪憲窪艱顧壓淵) 更多 | - | 2023-11-29 | ||
Placebo (Placebo (Blinded Phase)) | 糧淵鹹壓夢鬱顧遞選積 = 憲夢範齋範願獵夢廠願 鹽簾糧鑰製衊構鏇襯製 (鑰憲製網築製壓範糧襯, 鹽構憲範鏇鏇夢糧淵壓 ~ 餘鹽觸醖鏇鬱範網鹽鑰) 更多 | ||||||
临床1期 | 11 | 夢顧壓簾獵襯廠積積構 = 醖衊鑰壓簾窪壓遞觸襯 憲夢窪蓋構遞齋艱餘鹹 (膚鹹鹹鏇鹹齋夢糧獵膚, 選構憲構築積遞網夢艱 ~ 鏇觸遞願繭繭壓顧淵獵) 更多 | - | 2023-07-27 | |||
临床3期 | 11 | 鑰範構夢餘膚範遞鏇積(構襯範網廠鏇顧鏇鹽遞) = 夢艱夢遞艱壓醖壓齋簾 願網夢鹹簾鑰廠觸鹽齋 (憲壓獵鏇蓋廠遞糧鹽繭 ) 更多 | 积极 | 2022-06-23 | |||
临床2期 | 108 | 壓餘願簾夢壓襯憲構壓(衊鑰衊鏇製構製膚窪淵) = Treatments were well tolerated - the incidence of adverse events was similar across groups (73-90%) and most events were gastrointestinal in nature. 鑰襯網築齋淵鹽遞範繭 (製膚艱膚艱觸糧糧網齋 ) 更多 | 积极 | 2022-04-16 | |||
临床2期 | 66 | 築築醖觸選積顧製衊範(製廠顧膚願鏇製壓鏇衊) = most treatment-emergent adverse events were Grade 1 to 2 severity 積製簾蓋遞齋繭壓網襯 (壓窪憲醖積憲齋簾願壓 ) 更多 | 积极 | 2022-01-06 | |||
临床2期 | 109 | (Semaglutide) | 鬱製構齋觸憲憲醖衊淵 = 壓觸憲鏇齋齋鹽遞鑰獵 壓憲繭憲鏇窪衊醖蓋築 (範構願觸窪壓積蓋鑰壓, 積觸膚範窪鹽憲齋艱鹹 ~ 蓋選襯築膚製獵積醖築) 更多 | - | 2021-07-15 | ||
(Semaglutide + Firsocostat 20 mg) | 鬱製構齋觸憲憲醖衊淵 = 淵顧鑰壓鏇積襯艱繭鏇 壓憲繭憲鏇窪衊醖蓋築 (範構願觸窪壓積蓋鑰壓, 積簾蓋願鏇顧遞觸鬱簾 ~ 艱齋願製範選廠膚窪鑰) 更多 | ||||||
临床2期 | 12 | 積範鹽夢夢構範構艱餘(顧範膚願鏇積襯繭製願) = There were no serious adverse events but short intervals of cardiac arrhythmia recorded in 2 patients led to termination of the study. 築憲鹽餘簾範範構鹽憲 (繭鬱壓齋淵簾積鏇鏇築 ) | 积极 | 2021-05-01 |
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