Investigational Drug Details
| Drug ID: | D078 |
| Drug Name: | Cilofexor |
| Synonyms: | GS-9674 |
| Type: | Chemical drug |
| DrugBank ID: | DB15168 |
| DrugBank Description: | Cilofexor is under investigation in clinical trial NCT02943447 (Safety, Tolerability, and Efficacy of Cilofexor in Adults With Primary Biliary Cholangitis Without Cirrhosis). |
| PubChem ID: | 71228883 |
| CasNo: | 1418274-28-8 |
| Repositioning for NAFLD: | No |
| SMILES: | C(Oc1cc(Cl)c(cc1)C1(O)CN(C1)c1cc(C(=O)O)ccn1)c1c(noc1C1CC1)c1c(Cl)cccc1Cl |
| Structure: |
|
| InChiKey: | KZSKGLFYQAYZCO-UHFFFAOYSA-N |
| Molecular Weight: | 586.859 |
| DrugBank Targets: | -- |
| DrugBank MoA: | -- |
| DrugBank Pharmacology: | -- |
| DrugBank Indication: | -- |
| Targets: | FXR agonist |
| Therapeutic Category: | Enhance lipid metabolism |
| Clinical Trial Progress: | Phase 2 completed (Cilofexor for 24 weeks was well-tolerated and provided significant reductions in hepatic steatosis, liver biochemistry, and serum bile acids in patients with NASH. ClinicalTrials.gov No. NCT02854605.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0130 | NCT02781584 | Phase 2 | Completed | Has Results | June 13, 2016 | March 16, 2022 | Details |
| L0196 | NCT04971785 | Phase 2 | Recruiting | No Results Available | August 9, 2021 | March 11, 2022 | Details |
| L0198 | NCT03987074 | Phase 2 | Completed | Has Results | July 29, 2019 | July 15, 2021 | Details |
| L0213 | NCT03449446 | Phase 2 | Completed | Has Results | March 21, 2018 | December 3, 2020 | Details |
| L0313 | NCT02654002 | Phase 1 | Completed | Has Results | January 20, 2016 | October 12, 2020 | Details |
| L0352 | NCT02808312 | Phase 1 | Completed | Has Results | July 13, 2016 | January 7, 2021 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S02 | Enhance lipid metabolism | triglyceride-lowering; lipid tolerance; lipid metabolism | 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor; Decreases intestinal cholesterol absorption; FXR agonist; ACC inhibitor; FAS inhibitor; DGAT2 inhibitor; SCD-1 inhibitor | Atorvastatin; Ezetimibe; Obeticholic Acid; GS-9674; GS-0976; TVB-2640; IONIS-DGAT2rx; Aramchol; | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A02701 | 34278169 | Hepatol Commun | Improvements of Fibrosis and Disease Activity Are Associated With Improvement of Patient-Reported Outcomes in Patients With Advanced Fibrosis Due to Nonalcoholic Steatohepatitis. | Details |
| A03845 | 33849361 | Expert Opin Drug Discov | The identification of farnesoid X receptor modulators as treatment options for nonalcoholic fatty liver disease. | Details |
| A04968 | 33435509 | Biomedicines | The Non-Steroidal FXR Agonist Cilofexor Improves Portal Hypertension and Reduces Hepatic Fibrosis in a Rat NASH Model. | Details |
| A05661 | 33169409 | Hepatology | Combination Therapies Including Cilofexor and Firsocostat for Bridging Fibrosis and Cirrhosis Attributable to NASH. | Details |
| A07297 | 32552182 | Expert Opin Investig Drugs | Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH). | Details |
| A08427 | 32115759 | Hepatology | Cilofexor, a Nonsteroidal FXR Agonist, in Patients With Noncirrhotic NASH: A Phase 2 Randomized Controlled Trial. | Details |
| A09983 | 31536725 | Eur J Pharmacol | Farnesoid X nuclear receptor agonists for the treatment of nonalcoholic steatohepatitis. | Details |
| A10776 | 31197565 | Handb Exp Pharmacol | Nonsteroidal FXR Ligands: Current Status and Clinical Applications. | Details |
| A28794 | 34999207 | Clin Gastroenterol Hepatol | Fenofibrate Mitigates Hypertriglyceridemia in Nonalcoholic Steatohepatitis Patients Treated With Cilofexor/Firsocostat. | Details |
| A42318 | 34886776 | Curr Vasc Pharmacol | Cilofexor for the Treatment of Nonalcoholic Steatohepatitis | Details |
| A42623 | 33985820 | J Hepatol | FXR agonists for NASH: How are they different and what difference do they make? | Details |
| A43129 | 32488894 | Hepatology | Letter to the Editor: Cilofexor in Patients With Nonalcoholic Steatohepatitis (NASH): Is It Really Effective? | Details |
| A50298 | 35439567 | J Hepatol | Safety and efficacy of combination therapy with semaglutide, cilofexor and firsocostat in patients with non-alcoholic steatohepatitis: A randomised, open-label phase II trial. | Details |
| A50622 | 35323681 | Metabolites | Emerging Role of Nuclear Receptors for the Treatment of NAFLD and NASH. | Details |
| A51114 | 35686937 | Hepatology | IL-31 Levels Correlate with Pruritus in Patients with Cholestatic and Metabolic Liver Diseases and is FXR Responsive in NASH. | Details |
| A51118 | 35668318 | Hormones (Athens) | Semaglutide, cilofexor, and firsocostat for nonalcoholic steatohepatitis: a dance that may need more than one dancer. | Details |