Synonyms: BI 6727 | BI-6727
Compound class:
Synthetic organic
Comment: Volasertib is an ATP-competitive, investigational inhibitor of polo-like kinase 1 (PLK1). It is the second in a novel class of drugs called dihydropteridinone derivatives [3]. This compound is represented on PubChem by CID 10461508. This CID varies slightly in its chiral specification from our ligand entry. Our structure was drawn from the image submitted to the WHO for the INN (note that the long chemical name provided for the INN registration is not sufficient to resolve absolute stereochemistry as depicted in the accompanying image). Some bioactivity may be linked to the trihydrochloride salt form.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
In 2013, the US FDA granted volasertib breakthrough therapy designation for the treatment of patients with acute myeloid leukemia (AML), in response to positive results from a Phase 2 clinical trial (NCT00804856) in which the drug demonstrated substantial improvement on a clinically significant endpoint (in this case objective response) over available cytarabine therapy. The drug has now progressed to Phase 2I (NCT01721876) in combination with cytarabine for AML patients aged >65 years who have not received prior treatment and who are ineligible for intensive therapy. Phase 2 clinical trials are underway to assess volasertib as a treatment for additional conditions such as ovarian cancer, urothelial cancer and advanced non-small-cell lung cancer. |
Mechanism Of Action and Pharmacodynamic Effects |
PLK1 is ubiquitously present in the nuclei of dividing cells, where it controls several stages of the cell cycle and cell division [1-2]. Inhibition of PLK1 blocks cell division. |