Investigational Drug Details
| Drug ID: | D379 |
| Drug Name: | Tropifexor |
| Synonyms: | LJN452 |
| Type: | Chemical drug |
| DrugBank ID: | DB16343 |
| DrugBank Description: | Tropifexor is under investigation in clinical trial NCT02516605 (A Multi-part, Double Blind Study to Assess Safety, Tolerability and Efficacy of Tropifexor (LJN452) in PBC Patients). |
| PubChem ID: | 121418176 |
| CasNo: | 1383816-29-2 |
| Repositioning for NAFLD: | No |
| SMILES: | O(Cc1c(noc1C1CC1)c1c(OC(F)(F)F)cccc1)[C@@H]1C[C@H]2N([C@@H](C1)CC2)c1nc2c(s1)cc(cc2F)C(=O)O |
| Structure: |
|
| InChiKey: | VYLOOGHLKSNNEK-PIIMJCKOSA-N |
| Molecular Weight: | 603.594 |
| DrugBank Targets: | Bile acid receptor agonist&binder |
| DrugBank MoA: | -- |
| DrugBank Pharmacology: | -- |
| DrugBank Indication: | -- |
| Targets: | FXR agonist |
| Therapeutic Category: | Enhance lipid metabolism |
| Clinical Trial Progress: | Phase 2 terminated (NCT04147195: Sponsor Decision) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0037 | NCT04147195 | Phase 2 | Recruiting | No Results Available | June 4, 2020 | February 28, 2022 | Details |
| L0083 | NCT03681457 | Phase 1 | Completed | No Results Available | September 24, 2018 | December 14, 2020 | Details |
| L0229 | NCT03517540 | Phase 2 | Completed | Has Results | September 11, 2018 | January 24, 2022 | Details |
| L0238 | NCT02855164 | Phase 2 | Terminated | Has Results | August 1, 2016 | September 5, 2021 | Details |
| L0456 | NCT04065841 | Phase 2 | Recruiting | No Results Available | 19/08/2019 | 21 February 2022 | Details |
| L0522 | JPRN-JapicCTI-173735 | Phase 2 | Not Recruiting | Has Results | 17/10/2017 | 18 October 2021 | Details |
| L0585 | EUCTR2015-005215-33-SK | Phase 2 | Not Recruiting | No Results Available | 10/05/2016 | 11 May 2020 | Details |
| L0773 | CTRI/2019/01/017014 | Phase 2 | Recruiting | No Results Available | 09/01/2019 | 24 November 2021 | Details |
| L0999 | EUCTR2019-002324-32-BE | Phase 2 | -- | -- | 2019/12/13 | -- | 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 | |
|---|---|---|---|---|
| A03718 | 33894097 | Liver Int | A nonbile acid farnesoid X receptor agonist tropifexor potently inhibits cholestatic liver injury and fibrosis by modulating the gut-liver axis. | Details |
| A03845 | 33849361 | Expert Opin Drug Discov | The identification of farnesoid X receptor modulators as treatment options for nonalcoholic fatty liver disease. | Details |
| A07297 | 32552182 | Expert Opin Investig Drugs | Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH). | Details |
| A08711 | 32015483 | Sci Rep | Obeticholic acid and INT-767 modulate collagen deposition in a NASH in vitro model. | Details |
| A08915 | 31940200 | J Med Chem | Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. | Details |
| A09473 | 31731005 | Contemp Clin Trials | A randomized, double-blind, multicenter, phase 2b study to evaluate the safety and efficacy of a combination of tropifexor and cenicriviroc in patients with nonalcoholic steatohepatitis and liver fibrosis: Study design of the TANDEM trial. | Details |
| A10776 | 31197565 | Handb Exp Pharmacol | Nonsteroidal FXR Ligands: Current Status and Clinical Applications. | Details |
| A14976 | 29148806 | J Med Chem | Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH). | Details |
| A31019 | 31388629 | Hepatol Commun | Tropifexor-Mediated Abrogation of Steatohepatitis and Fibrosis Is Associated With the Antioxidative Gene Expression Profile in Rodents. | Details |
| A42377 | 34738233 | J Clin Pharmacol | Pharmacokinetics of Tropifexor, a Potent Farnesoid X Receptor Agonist, in Participants With Varying Degrees of Hepatic Impairment. | Details |
| A42623 | 33985820 | J Hepatol | FXR agonists for NASH: How are they different and what difference do they make? | Details |
| A47670 | 33952610 | Drug Metab Dispos | Evaluation of the Absorption, Metabolism, and Excretion of a Single Oral 1-mg Dose of Tropifexor in Healthy Male Subjects and the Concentration Dependence of Tropifexor Metabolism. | Details |
| A51404 | 35779659 | J Hepatol | Digital pathology with artificial intelligence analyses provides greater insights into treatment-induced fibrosis regression in NASH. | Details |