Gastrointestinal (GI) tract infections and imbalance of gut microbiota are associated with some common and serious diseases, including peptic ulcer and gastric cancer associated with H. pylori infection (HPI), pseudomembranous colitis associated with C. difficile infection (CDI), hepatic encephalopathy (HE) associated with cirrhosis and bacteria in the GI tract, irritable bowel syndrome – diarrhea (IBS-D) and Crohn’s Disease (CD). Long term of therapy is required for the management of HE, IBS-D and some other diseases associated with GI tract infections. Safety and tolerability of the treatment are essential. GI tract-specific antibiotic rifaximin (Xifaxan) is an important therapy in this area. Rifaximin is a locally acting drug with a low systemic exposure. It possesses excellent safety and tolerability profile and has been used widely in the treatment of HE and IBS-D.
TNP-2092 oral capsule is a multi-targeting, GI tract-specific antibiotic. Like rifaximin, TNP-2092 is a locally acting drug with low systemic exposure. In completed Phase I clinical trials, TNP-2092 oral capsule demonstrated excellent safety and tolerability. Rifaximin is a RNA polymerase inhibitor and possesses a high frequency for development of resistance. Clinical studies indicated that rifaximin develop resistance rapidly during clinical trials. Different from rifaximin, TNP-2092 is a multi-targeting molecule by exerting its bactericidal effect through targeting RNA polymerase, DNA gyrase and topoisomerase IV. It possesses better antibacterial activity and lower potential for development resistance as compare to rifaximin. TNP-2092 has the potential to improve the treatment of HE, IBS-D and other diseases associated GI tract infections and become an important member of the $5 billion-dollar GI tract-specific antibiotic market.