RP-1664

RP-1664 is an orally bioavailable, selective small molecule inhibitor of polo-like kinase 4 (PLK4), developed by Repare Therapeutics as a potential antineoplastic agent for the treatment of advanced solid tumors. By selectively inhibiting PLK4, a protein involved in mitosis and cell division, RP-1664 disrupts mitosis and induces apoptosis in cancer cells. Preclinical data suggest that it may be particularly effective in tumors with TRIM37 amplification or overexpression due to synthetic lethality. The drug is currently being evaluated in Phase 1 clinical trials to assess its safety, pharmacokinetics, pharmacodynamics, and preliminary anti-tumor activity in patients with advanced solid tumors. It is administered orally as hard capsules and development focuses on cancers with specific genetic alterations (TRIM37 amplification/overexpression) that may confer increased sensitivity to PLK4 inhibition.

Other names

PLK4 inhibitor RP-1664PLK-4 inhibitor RP-1664PLK 4 inhibitor RP-1664RP-1664 sulfateRP1664 sulfateRP 1664 sulfate