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onvansertib
- Development stage
- Phase 2
- Lead developer
- Cardiff Oncology
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Onvansertib is an orally bioavailable, small molecule inhibitor of polo-like kinase 1 (PLK1), a serine/threonine kinase that plays a crucial role in the regulation of mitosis and DNA damage repair. By competitively inhibiting ATP binding to PLK1, onvansertib disrupts mitosis, induces G2/M cell-cycle arrest, and promotes apoptosis in tumor cells overexpressing PLK1. This mechanism targets cancer cell proliferation and enhances the efficacy of standard chemotherapies by impairing DNA repair pathways. Onvansertib is being developed primarily for oncology indications including acute myeloid leukemia (AML), colorectal cancer (especially KRAS-mutant metastatic CRC), pancreatic cancer, prostate cancer, small cell lung cancer, triple negative breast cancer, chronic myelomonocytic leukemia, medulloblastoma, and ovarian cancer. The drug was originally discovered by Nerviano Medical Sciences and is currently being developed by Cardiff Oncology[1][5][6].
- Other names
- onvansertib-fumarateonvansertib free base
02
Targets
PLK1 (Polo like kinase 1)
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