Crestone, Inc. is a drug discovery and development company focused on developing novel treatments for serious bacterial infections. The company currently has two programs that address areas of significant and growing unmet medical need, both with novel mechanism of action agents.

1. Novel antibiotic for Clostridium difficile infections. CRS3123 (formerly known as REP3123) is in development for the treatment of C. difficile infection (CDI). This disease occurs when toxin-producing bacteria colonize the gastrointestinal tract, and is associated with significant morbidity and mortality. Due to the development of hyper-virulent drug-resistant strains, incidence has more than doubled in the last decade. Preclinical testing of CRS3123 shows superior performance over existing therapies, which have significant shortcomings. Phase 1 clinical studies for CRS3123 are currently being conducted with the NIAID Division of Microbiology and Infectious Disease (DMID).

 

2. Novel oral agents for Gram-positive infections. Crestone is optimizing a novel class of DNA replication inhibitors with Gram-positive antibacterial activity. This promising chemical series is currently in advanced lead optimization, funded by an SBIR grant from NIAID and by a Bioscience Discovery Evaluation Grant from the State of Colorado. These molecules selectively inhibit an essential component of the replicative DNA polymerase complex and are potent, orally available, and effective against all clinically-relevant Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), penicillin-resistant Streptococcus pneumoniae (PRSP) and Bacillus anthracis. We anticipate development of a drug similar to Zyvox in spectrum, but with key advantages such as bactericidal activity and improved safety.