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RTIOXA-47 (also known as ROXA-47) is a novel, metabolically stable small molecule dual orexin receptor agonist developed by RTI International in collaboration with the University of Minnesota. It targets both orexin receptor type 1 (OX1R) and orexin receptor type 2 (OX2R) with low nanomolar potency. In preclinical rodent models, peripheral administration of RTIOXA-47 has been shown to enhance spontaneous physical activity, increase energy expenditure, and reduce body weight and fat mass, suggesting therapeutic potential for the treatment of obesity. Additionally, RTIOXA-47 improves cognitive function (such as memory and active avoidance) and sleep-wake quality (increasing wakefulness and reducing sleep fragmentation), with its cognitive and physical activity benefits primarily mediated via OX1R activation.
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