Crestone, Inc. Secures NIH Funding for Development Through Phase 1 of Novel Antibiotic Candidate CRS0540, A Novel Inhibitor of DNA Replication in Gram-positive Pathogens

BOULDER, Colo.--()--Crestone, Inc. today announced a contract award from the National Institutes of Health for the advancement of its antibiotic candidate CRS0540 to treat infections caused by drug-resistant Gram-positive bacteria.

The lead compound CRS0540 has demonstrated efficacy in several mouse models of infection including MRSA soft tissue and blood stream infections, pneumococcal lung infection, and even an inhalational anthrax challenge model.

Under this four-year contract from NIH, Crestone’s drug candidate CRS0540 will be manufactured under GMP conditions, formulated for oral and intravenous administration, tested in IND-enabling safety pharmacology and GLP toxicity studies, and evaluated for safety in a first-in-human Phase 1 clinical trial. Potential indications are skin and skin structure and respiratory infections.

“Antibiotics with a novel mode of action and a good safety profile are sorely needed to augment the armamentarium of drugs to treat infections with resistant pathogens, and CRS0540 dosed orally has already demonstrated efficacy in various animal models of infection,” said Urs Ochsner, PhD, co-Founder and Vice President of R&D and CEO at Crestone. “Medicinal chemistry efforts over several years to improve potency and to optimize the pharmacological properties of these DNA replication inhibitors have led to CRS0540, a very promising candidate to move into clinical development,” said Joshua Day, PhD, Director of Chemistry at Crestone, who will be the Principal Investigator.

Funding for these studies will be provided entirely by NIH’s National Institute of Allergy and Infectious Diseases (NIAID) under Contract No. 75N93020C00020 for a total of up to $18.2 million including the base period and subsequent option periods.

About CRS0540

CRS0540 is a mechanistically novel oral/IV antibacterial drug candidate that is intended for treatment of infections caused by antibiotic-resistant pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), macrolide-resistant Streptococcus pyogenes (Group A strep) and vancomycin-resistant enterococci (VRE), as well as treatment of food-borne illness caused by Listeria monocytogenes. CRS0540 derives from a series of thiadiazole urea compounds that exhibit potent inhibition of PolC, the catalytic subunit of the replicative DNA polymerase in Gram-positive bacteria. As a novel mechanism of action agent, CRS0540 has shown activity against all clinically relevant antibiotic-resistant Gram-positive pathogens.

About Crestone, Inc.

Boulder, Colorado-based Crestone, Inc. is a clinical stage biopharmaceutical company focused on inventing and developing novel mechanism of action small molecule drugs for serious bacterial infections. The active pipeline includes antibacterial agents to treat Clostridioides difficile infection (CDI), resistant Gram-positive infections such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE), chronic infections such as nontuberculous mycobacterial (NTM) disease, and Helicobacter pylori infections.

Release Summary

Crestone, Inc. Secures NIH Funding for Development of Antibiotic Candidate CRS0540, a Novel Inhibitor of Bacterial DNA Replication