Claritas Announces Completion of IND-Enabling In Vitro Genotoxicity Studies with R-107 - Seite 2

The in vitro micronucleus test detects genotoxic damage and provides a preferred alternative to the previously used chromosome aberration test for detection of aneugenic (whole chromosome) or clastogenic (chromosome breakage) damage, using micronuclei formation as a biological marker. Treatments of human lymphocyte cultured cells covering a broad range of concentrations of R-107, separated by narrow intervals, were performed in this study at Covance. R-107 did not induce micronuclei in cultured human peripheral blood lymphocytes following all treatments tested, with the maximum concentration analyzed approximately equivalent to 1 millimolar (recommended as a suitable maximum concentration for the in vitro micronucleus assay in accordance with current regulatory guidelines). It was therefore determined that R-107 is considered unable to induce chromosome breaks (clastogenicity) and/or whole chromosome loss (aneugenicity) in this test system.

The data in both the Ames Assay and the in vitro micronucleus test confirm that R-107 does not have any carcinogenic ability, which positively contributes to its safety profile and moves the drug closer to initiation of human clinical testing in a Phase I study.

R-107 is a Nitric Oxide-Releasing Molecule
R-107 is a liquid, nitric oxide-releasing molecular prodrug that can be administered by injection, in contrast to nitric oxide gas therapy which requires a special type of delivery device and complex administration by trained respiratory therapists. When administered by injection, R-107 is slowly hydrolyzed by the blood, thereby releasing its active payload, R-100, which in turn steadily and slowly releases nitric oxide. This depot-like action of R-107 results in a sustained delivery of nitric oxide to tissues throughout the body, allowing for a smooth delivery of the active drug over 24 hours following a single dose of R-107.

Professor Salvatore Cuzzocrea, a member of Claritas’ board of directors and President of the University of Messina and former President of the European Shock Society is working with Salzman Group and Claritas, and has read and approved of the scientific disclosure in this news release. Professor Cuzzocrea has deep expertise regarding the medical use of nitric oxide and nitric oxide donors, and has published more than 600 papers on nitric oxide. He has conducted research and experiments with nitric oxide and nitric oxide donors since 1994, and worked closely as an advisor with the Salzman Group team that designed and invented R-107.