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Novel Selective HDAC6 Inhibitor Under Study in Multiple Myeloma

By: Melissa E. Fryman, MS
Posted: Wednesday, April 24, 2019

Nexturastat A, a selective histone deacetylase (HDAC) 6 inhibitor, may prove to be an effective treatment for patients with multiple myeloma. In an in vitro study using human multiple myeloma cell lines, Kailin Xu, MD, and colleagues, of the Xuzhou Medical University, Jiangsu, China, found that nexturastat A halted cell division and spurred apoptosis. Furthermore, nexturastat A seemed to overcome resistance to bortezomib. Their results were published in Bioscience Reports.

In this study, two human multiple myeloma cell lines, RPMI-8226 and U266, were treated with nexturastat A and then analyzed in a series of experiments. CCK8 viability assay and flow cytometry showed that nexturastat A reduced viability and induced cell-cycle arrest in both cell types. Furthermore, as evidenced by staining with cell-death markers, nexturastat A seemed to induce apoptosis in both cell lines, presumably through transcriptional activation of the p21 promoter. These effects were time- and dose-dependent.

Separately, using RPMI-8226/BTZ100, a human multiple myeloma cell line that harbors resistance to bortezomib, the researchers found that the addition of nexturastat A inhibited cell growth and may also induce apoptosis. Thus, they concluded that nexturastat A may overcome bortezomib resistance in human multiple myeloma cells, also in a dose-dependent manner. Lastly, in mice injected with RPMI-8226 cells that were treated with nexturastat A, reduction in both tumor weight and size was seen.

“These interesting findings provide the rationale for the future advancement of this novel HDAC6 inhibitor as a potential therapeutic antimyeloma agent,” the authors concluded.

Disclosure: The study authors reported no conflicts of interest.

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