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Phase I study of domatinostat (4SC‐202), a class I histone deacetylase inhibitor in patients with advanced hematological malignancies
Domatinostat (4SC‐202) is a selective class I histone deacetylase inhibitor (HDACi). This phase I study investigated safety, tolerability, pharmacokinetics (PK), pharmacodynamics, and antitumorExpand
First-in-human study of 4SC-205 (AEGIS), a novel oral inhibitor of Eg5 kinesin spindle protein.
2564 Background: 4SC-205 is a potent small molecule inhibitor of the kinesin spindle protein Eg5 with broad anti-tumour activity in vitro and in vivo. Currently, 4SC-205 is the only oral availableExpand
First-in-human study of 4SC-202, a novel oral HDAC inhibitor in advanced hematologic malignancies (TOPAS study).
8559 Background: 4SC-202 is a specific inhibitor of protein deacetylases HDAC1, 2 and 3 and lysine specific demethylase LSD1 (KDM1A). Enzymatic inhibition leads to transcriptional repression of WntExpand
Overcoming the proliferation rate paradox: Clinical evaluation of a continuous dosing scheme of the novel oral Eg5 inhibitor 4SC-205.
2528 Background: Mitotic proteins, like Eg5, are exclusively expressed during mitosis. Targeted therapy directed against such proteins prevents side-effects like peripheral neuropathies. However,Expand
A Novel Microtubule Inhibitor 4SC-207 with Anti-Proliferative Activity in Taxane-Resistant Cells
Microtubule inhibitors are invaluable tools in cancer chemotherapy: taxanes and vinca alkaloids have been successfully used in the clinic over the past thirty years against a broad range of tumors.Expand
PO-012 Pre-clinical insight into how platelet count affects the activity of HDACi resminostat in combination with the multi-kinase inhibitor sorafenib in HCC
Introduction In a recent phase I/II clinical trial in hepatocellular carcinoma (HCC), (NCT02400788), the combination of HDAC-inhibitor resminostat (YHI1001) with a multi-kinase inhibitor sorafenibExpand
Resminostat plus sorafenib in hepatocellular carcinoma (HCC) as apotential new treatment approach in platelet-driven solid tumors.
e14571Background: A phase I/II clinical trial in advanced hepatocellular carcinoma (HCC) conducted by Yakult Honsha (NCT02400788) indicated the combination of the HDAC inhibitor resminostat and sor...
The effect of 4SC-207, a novel antimitotic agent, on multidrug-resistant cell lines.
e14090 Background: 4SC-207 is a novel small molecule with strong anti-mitotic activity. In this study the potency on in vitro cell proliferation, including chemotherapeutically resistantExpand