KT-3000

KT-3000 is a novel class of bi-functional small-molecule drug candidates developed by Rakovina Therapeutics. The compounds in the KT-3000 series are designed to act as dual inhibitors of poly(ADP-ribose) polymerase (PARP) and histone deacetylase (HDAC), combining both mechanisms into a single molecule. This dual action aims to provide synergistic anti-cancer effects, particularly for tumors that are resistant to standard therapies, including those that have become refractory to FDA-approved PARP inhibitors. Preclinical data demonstrate that lead candidates from the KT-3000 series exhibit potent inhibition of both PARP and HDAC at low nanomolar concentrations, resulting in significantly higher DNA damage and cancer cell death compared to single-agent or combination treatments with existing PARP or HDAC inhibitors. The primary focus has been on Ewing sarcoma and other soft tissue tumors, but there is potential for broader application in cancers such as breast and ovarian cancer with acquired resistance to current treatments[1][2][3][4][6][8].

Other names

KT-3000 seriesKT3000 seriesKT 3000 serieskt-3283kt3283kt 3283