CC10230

CC10230 is a novel, peripherally restricted small molecule agonist of the alpha-2A adrenergic receptor (ADRA2A) designed for integrated cancer therapy and supportive care. By targeting peripheral alpha-2A adrenoceptors, the compound aims to suppress tumor growth and alleviate cancer-related pain while avoiding the dose-limiting central nervous system (CNS) toxicities, such as sedation and hypothermia, typically associated with non-selective agonists like clonidine. CC10230 is engineered as a strong P-glycoprotein (P-gp) substrate, which ensures minimal penetration across the blood-brain barrier (Kp,uu,brain < 0.03). In preclinical studies, CC10230 demonstrated significant tumor growth inhibition (TGI of 62.3% in MC38 models) and robust anti-allodynic efficacy in bone cancer pain models, supporting its potential for sustained therapy without the tolerability limitations of conventional alpha-2A agonists.