RQ-00202730

RQ-00202730 (also known as AAT-730 or OCT4130401) is a potent and highly selective small molecule agonist of the cannabinoid receptor 2 (CB2), originally developed by RaQualia Pharma and its spin-off AskAt, and later licensed to Oxford Cannabinoid Technologies (OCT). The compound is a benzimidazole derivative designed to treat chronic pain conditions, with a lead focus on chemotherapy-induced peripheral neuropathy (CIPN). It demonstrates an EC50 of 19 nM at the CB2 receptor and exhibits more than 1,300-fold selectivity over the CB1 receptor, which minimizes the risk of central nervous system side effects typically associated with CB1 activation. By activating CB2 receptors, the drug modulates nociceptive and inflammatory signaling. RQ-00202730 entered a Phase 1 first-in-human clinical trial in the United Kingdom in July 2023.