PRS-639,058 is a CB2 slec5tive drug candidate that overcomes many of the obstacles found in cannabinoid drug development – poor drugability (solubility, metabolism, low oral bioavailability) and central mediated side effects. PRS-639,058 is a small synthetic molecule with easy synthesis and low cost of goods. It is orally active in animal models of neuropathic pain and autoimmune disease, and its analgesic activity is chracterized by rapid onset of action at low doses. In vitro GLP safety toxicology studies were conducted and no signes of toxictiy were detected.
Early stage CB2-specific compounds were designed and synthesized to have a uniquely different chemical structure than PRS-639,058. These compounds are CB2 receptor specific and have negligible affinity at the CB1 receptor. Furthermore, they fulfill all the requirement of druggable candidates (Lipinski rule of five). Four candidates have been selected out of 100, based on early stage screening and filtering steps for drugable and safe cannabinoid drug candidates (cannabinoid receptor binding and functional studies, in vitro metablolism, and CB1 safety studies in rats). In addition, efficacy in animal models of inflammatory bowel disease has been demonstrated.