ACC1 inhibitors(Acetyl-CoA carboxylase 1 inhibitors), ACC2 inhibitors(Acetyl-CoA carboxylase 2 inhibitors), FXR agonists(Bile acid receptor FXR agonists)

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Therapeutic Areas

Digestive System DisordersOther Diseases

Active Indication

Compensated cirrhosisFibrosisNonalcoholic Steatohepatitis

Inactive Indication-

Originator Organization

Gilead Sciences, Inc.

Active Organization

Gilead Sciences, Inc.

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

Structure

Molecular FormulaC28H31N3O8S

InChIKeyZZWWXIBKLBMSCS-FQEVSTJZSA-N

CAS Registry1434635-54-7

View All Structures (3)

Clinical Trials associated with Cilofexor/Firsocostat

NCT04971785 / Active, not recruitingPhase 2

A Phase 2, Randomized, Double-Blind, Double-Dummy, Placebo-Controlled Study Evaluating the Safety and Efficacy of Semaglutide, and the Fixed-Dose Combination of Cilofexor and Firsocostat, Alone and in Combination, in Subjects With Compensated Cirrhosis (F4) Due to Nonalcoholic Steatohepatitis (NASH)

The goals of this clinical study are to learn more about the study drugs, semaglutide (SEMA) with the fixed-dose combination (FDC) of cilofexor/firsocostat (CILO/FIR), and understand whether they cause fibrosis improvement and Nonalcoholic Steatohepatitis (NASH) resolution in participants with cirrhosis due to NASH.

Start Date09 Aug 2021

Sponsor / Collaborator

Gilead Sciences, Inc.

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100 Clinical Results associated with Cilofexor/Firsocostat

100 Translational Medicine associated with Cilofexor/Firsocostat

100 Patents (Medical) associated with Cilofexor/Firsocostat

Literatures (Medical) associated with Cilofexor/Firsocostat

01 Sep 2007·Journal of EthnopharmacologyQ2 · MEDICINE

Hypolipidemic effects and mechanisms of Panax notoginseng on lipid profile in hyperlipidemic rats

Q2 · MEDICINE

Article

Author: B.Q. Gong ; W. Ji

Maintenance of normal lipid levels has implicated the involvement of genes induced by liver X receptor alpha (LXRalpha) and Farnesoid X receptor (FXR). This study was designed to evaluate the hypolipidemic effects of n-butanol extract (NE3) of Panax notoginseng (Burk.) F.H. Chen root on lipid homeostasis and investigate the possible mechanisms in animal experiments. In the transactivation assays, NE3 was identified as a dual FXR/LXRalpha agonist. Subsequently, Sprague-Dawley male rats on a high-fat/high-cholesterol diet were treated orally with NE3 or vehicle alone. As expected, the concentrations of serum TC, TG and LDL-C in rats treated with various concentrations of NE3 showed significant (P<0.01) and dose-dependent decrease, respectively, accompanied with a significant (P<0.01) and dose-dependent decrease in the concentration of hepatic TC and TG. Express-level analysis indicated that both LXRalpha target genes including ABCA1, ABCG5, ABCG8 and FXR target genes including ApoCII and SHP were significantly induced by NE3 (P<0.01). Interestingly, LDLR mRNA level was significantly higher by NE3 (P<0.01), accompanied with the significantly decreased expression levels of CYP7A1, ApoCIII and SREBP1c genes (P<0.01). Based on these results, it can be concluded that NE3 as a dual FXR/LXRalpha agonist largely prevented the accumulation of abnormal lipid in the hyperlipidemic rats.

100 Deals associated with Cilofexor/Firsocostat

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Compensated cirrhosis	Phase 2	ES	Gilead Sciences, Inc.	09 Aug 2021
Compensated cirrhosis	Phase 2	US	Gilead Sciences, Inc.	09 Aug 2021
Compensated cirrhosis	Phase 2	FR	Gilead Sciences, Inc.	09 Aug 2021
Compensated cirrhosis	Phase 2	PR	Gilead Sciences, Inc.	09 Aug 2021
Compensated cirrhosis	Phase 2	CA	Gilead Sciences, Inc.	09 Aug 2021
Compensated cirrhosis	Phase 2	AU	Gilead Sciences, Inc.	09 Aug 2021
Compensated cirrhosis	Phase 2	JP	Gilead Sciences, Inc.	09 Aug 2021
Nonalcoholic Steatohepatitis	Phase 2	ES	Gilead Sciences, Inc.	09 Aug 2021
Nonalcoholic Steatohepatitis	Phase 2	CA	Gilead Sciences, Inc.	09 Aug 2021
Nonalcoholic Steatohepatitis	Phase 2	JP	Gilead Sciences, Inc.	09 Aug 2021

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Cilofexor/Firsocostat

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