Artelo Biosciences (NASDAQ: ARTL) has announced positive results from its first-in-human study evaluating its novel non-opioid candidate, ART26.12, for the treatment of persistent pain.
ART26.12 is the first orally active fatty acid binding protein 5 (FABP5) inhibitor evaluated in humans. By targeting FABP5, ART26.12 modulates endogenous lipid signalling molecules that exert analgesic effects through established pathways, including TRPV1, PPAR alpha, and cannabinoid receptors, with additional mechanisms such as Nav1.8 under investigation.
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.
According to Artelo, 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.
In a statement, Andrew Yates, Ph.D., SVP and CSO 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.”
The first-in-class approach addresses a significant unmet need in the chronic pain therapeutics market, which surpassed $97 billion globally in 2023 and is projected to exceed $159 billion by 2030, driven by the rising prevalence of conditions such as neuropathic pain, arthritis, and fibromyalgia. Despite the market’s size, innovation remains limited—especially in non-opioid therapies.
As part of its Overdose Prevention Framework, the FDA has issued draft guidance aimed at encouraging the development of non-opioid analgesics. ART26.12 is well positioned to help fill this gap, offering an innovative mechanism of action and a favorable safety profile. A Multiple Ascending Dose study to further evaluate the safety, tolerability, and PK of ART26.12 with repeated dosing over time is expected to begin in Q4 this year.
