Artelo Biosciences, Inc. a clinical-stage pharmaceutical company focused on modulating lipid-signaling pathways to develop treatments for people living with cancer, pain, dermatological or neurological conditions, today announced favorable results from its first-in-human study evaluating ART26.12, a novel inhibitor of Fatty Acid Binding Protein 5 (FABP5). The results affirm the promising safety and pharmacokinetic (PK) profile previously observed in preclinical studies.

Inhibiting FABP5 represents a unique mechanism of action with ART26.12 standing out as a first-in-class candidate in the field of pain management. The Phase 1 Single Ascending Dose (SAD) study was designed to assess the safety, tolerability, and pharmacokinetics of ART26.12 in healthy volunteers. The SAD study enrolled 49 subjects.

The key findings include:

• Excellent Safety Results: All adverse events (AEs) were mild, transient, and self-resolving. No drug-related AEs were observed in the blinded dataset, and no tolerability issues or safety signals were detected across multiple assessments (vital signs, ECGs, clinical laboratory tests, physical examinations, and visual analogue mood scales).
• Predictable PK: Full dose-exposure profiles were successfully explored. Plasma analysis confirmed dose-dependent, linear absorption across the evaluated range.
• Therapeutic Window: A wide safety margin was observed between estimated therapeutic plasma concentrations and the highest exposure levels achieved, supporting potential titration for maximum efficacy in future studies.
  
  

Andrew Yates, Ph.D., Senior Vice President and Chief Scientific Officer at Artelo, commented, “We are greatly encouraged with the results of the SAD study with our lead FABP5 inhibitor and we are particularly pleased to observe that the safety and PK profile that had been generated from ART26.12’s non-clinical studies translated well to the human experience.”

ART26.12 is the first orally administered, selective, and peripherally restricted FABP5 inhibitor to enter human clinical evaluation. By targeting FABP5, ART26.12 modulates endogenous lipid signaling molecules that exert analgesic effects through established pathways, including TRPV1, PPAR alpha, and cannabinoid receptors, with additional mechanisms such as Nav1.8 under investigation.

The chronic pain therapeutics market exceeded $97 billion globally in 2023 and is expected to surpass $159 billion by 2030¹, driven by the increasing prevalence of conditions such as neuropathic pain, arthritis, and fibromyalgia. Despite the scale of the market, innovation remains sparse—particularly for non-opioid therapies. As part of the U.S Food and Drug Administration’s Overdose Prevention Framework, the Agency has issued draft guidance aimed at encouraging the development of non-opioid analgesics for pain. ART26.12 is positioned to fill this gap with an innovative mechanism of action and favorable safety profile. A Multiple Ascending Dose study to further evaluate the safety, tolerability, and pharmacokinetics of ART26.12 with repeated dosing over time is expected to commence in the fourth quarter this year.