BL-1021

BL-1021 is an orally available small molecule drug developed for the treatment of neuropathic pain. It was designed to mimic the activities of anti-neuropathic antidepressant drugs but with fewer common adverse effects, such as sedation and cardiac toxicity. Preclinical studies demonstrated efficacy in animal models of neuropathic pain, showing a favorable safety profile and improved efficacy compared to other anti-pain medications. Mechanistically, BL-1021 acts as a blocker of voltage-gated sodium channels Nav1.6 (Sodium channel protein type VIII alpha subunit), Nav1.7 (Sodium channel protein type IX alpha subunit), and Nav1.8 (Sodium channel protein type X alpha subunit). The drug reached Phase 1 clinical trials but development was discontinued.