The presentations include results from the Phase 1 clinical study of ART26.12 as well as new biomarker analyses designed to identify indicators of target engagement and pharmacological activity in healthy volunteers.

During the first of two presentations, Professor Saoirse E. O'Sullivan, Vice President of Translational Science at Artelo Biosciences, shared results from the first-in-human study with a selective FABP5 inhibitor titled: A Phase 1 Study to Assess the Safety and Pharmacokinetics of ART26.12. The Phase 1 study evaluated single ascending oral doses of ART26.12 in healthy volunteers which demonstrated that ART26.12 was generally well-tolerated across all evaluated dose levels and exhibited predictable, linear pharmacokinetics.

Key findings included:

  • Favorable safety and tolerability profile across all cohorts
  • Linear, dose-dependent pharmacokinetics
  • Dose-proportional systemic exposure
  • ART26.12 plasma concentrations exceeding projected therapeutic levels based on preclinical efficacy studies
  • Wide margin between anticipated therapeutic exposures and maximum tolerated doses
     

Also today, Myles Osborn, Lead Medicinal Chemist at Artelo Biosciences, delivered new data in a presentation titled: Unbiased Identification of Putative Clinical Biomarkers of Target Engagement with the Selective Fatty Acid Binding Protein 5 Inhibitor ART26.12.

Researchers interrogated proteomic and lipidomic databases from preclinical studies with ART26.12 with plasma samples collected from healthy volunteers who participated in the single ascending dose Phase 1 study of ART26.12 to identify potential biomarkers. Aided by artificial intelligence and machine learning algorithms, the analysis identified treatment-related changes across multiple biological pathways, including lipid metabolism, inflammation, extracellular matrix regulation, phospholipid signaling, and triglyceride metabolism. The findings represent an important step toward establishing pharmacodynamic biomarkers that could support future clinical development and provide insight into biological target engagement.