공시 • Jul 02
Artelo Biosciences Announces Positive First-In-Human Data for ART26.12, a Novel Non-Opioid Treatment Candidate for Persistent Pain
Artelo Biosciences, Inc. 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-relatedAEs 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. 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 angesic 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 As part of the U.S Food and Drug Administration's Overdose Prevention Framework, the Agency has issued draft guidance aimed at encouraging the development of non-opioid analgesics for pain.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, & pharmacokinetics of ART26., a novel, peripherally acting, non-opioid, non-steroidal analgesic. The initial clinical development planned is for chemotherapy-induced peripheral neuropathy (CIPN). FABPs are a family of intracellular proteins that chaperone lipids important to normal cellular function. FABP is overexpressed and associated with abnormal lipid signaling in several pathologies. In addition to ART26.12 in CIPN, Artelo's extensive library of small molecule inhibitors of FABPs has shown therapeutic promise for the treatment of certain cancers, neuropathic and nociceptive pain, anxiety disorders, and psoriasis. ART26.12 has been included in Helping to End Addiction Long-term®? (HEAL) Initiative's Initiative's Initiative's Initiative's Phase 1 single Ascending Dose study in the SAD study. The SAD study enrolled49 subjects. The SAD study enrolled 51 subjects. The key findings include; Excellent Safety Results: All adverse event (AEs) were mild and transient, transient, and self- resolving. No drug-related AEs were observed in the blinded datasets, and self-resolving, and no drug-related candidate in the field of pain Management. ART26.12 is observed in the blinded dataset.