Clinical Trials

Tropifexor (LJN452) has been evaluated in several Phase 1 and Phase 2 clinical trials sponsored by Novartis Pharmaceuticals to address various hepatic and metabolic disorders. These investigations assessed safety and efficacy across conditions including non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease, primary biliary cholangitis, primary bile acid diarrhea, and general liver disease. The overall clinical program encompasses both completed safety and crossover studies as well as terminated Phase 2 evaluations.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04065841 TERMINATED
Non Alcoholic Steatohepatitis (NASH)
Novartis Pharmaceuticals
 2019-12-30 PHASE2
NCT04147195 TERMINATED
Non-alcoholic Fatty Liver Disease; Nonalcoholic Steatohepatitis
Novartis Pharmaceuticals
 2020-06-04 PHASE2
NCT04408937 COMPLETED
Liver Disease
Novartis Pharmaceuticals
 2020-05-29 PHASE1
NCT03517540 COMPLETED
Non-alcoholic Steatohepatitis (NASH)
Novartis Pharmaceuticals
 2018-09-11 PHASE2
NCT04408937 Completed
Liver Disease
Novartis Pharmaceuticals|Novartis
 2020-05-29 Phase 1
NCT02855164 TERMINATED
Non-alcoholic Steatohepatitis (NASH)
Novartis Pharmaceuticals
 2016-08-01 PHASE2
NCT03681457 COMPLETED
Non-alcoholic Fatty Liver Disease
Novartis Pharmaceuticals
 2018-09-24 PHASE1
NCT02516605 COMPLETED
Primary Biliary Cholangitis
Novartis Pharmaceuticals
 2015-09-09 PHASE2
NCT02713243 COMPLETED
Primary Bile Acid Diarrhea
Novartis Pharmaceuticals
 2016-01-16 PHASE2
NCT02855164 Terminated
Non-alcoholic Steatohepatitis (NASH)
Novartis Pharmaceuticals|Novartis
 2016-08-01 Phase 2
NCT02713243 Completed
Primary Bile Acid Diarrhea
Novartis Pharmaceuticals|Novartis
 2016-01-16 Phase 2

(data from https://clinicaltrials.gov, updated on 2025-01-28)

Check the Tropifexor (LJN452) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Tropifexor acts as a highly potent agonist that selectively binds to the farnesoid X receptor (FXR), thereby activating downstream transcriptional regulation of bile acid synthesis, lipid transport, and metabolic homeostasis. This receptor activation suppresses hepatic bile acid production and reduces triglyceride accumulation, providing therapeutic benefit in liver disorders such as non-alcoholic steatohepatitis and primary biliary cholangitis.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.