Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of INT-787, a Novel Farnesoid X Receptor Agonist, in Healthy Volunteers: A Phase 1 Trial.

ABSTRACT: Aberrant farnesoid X receptor (FXR) signaling is implicated in cholestatic, inflammatory, and fibrotic liver diseases. In preclinical/clinical studies, semisynthetic bile acid-derived FXR agonists markedly improved hepatic function in various conditions. INT-787, a novel hydrophilic semisynthetic bile acid FXR agonist, has demonstrated a reduction in inflammatory and fibrotic markers and regulation of bile acid/lipid metabolism. This first-in-human, randomized, placebo-controlled phase 1 study assessed the safety, tolerability, pharmacokinetics, and pharmacodynamics of INT-787 and its equipotent metabolites in healthy volunteers by evaluating single ascending doses (SAD), multiple ascending doses (MAD), and food effect. Participants (n = 130) across all study portions were similar in age,

SUBMITTER: Capozza T 

PROVIDER: S-EPMC12042697 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature