On July 8, 2020 TG Therapeutics, Inc. (NASDAQ: TGTX) reported the publication of preclinical data describing the unique immunomodulatory effects of umbralisib, the Company’s investigational oral once-daily dual inhibitor of PI3K-delta and CK1-epsilon, in Blood Advances, a Journal of the American Society of Hematology (ASH) (Free ASH Whitepaper) (Press release, TG Therapeutics, JUL 8, 2020, View Source [SID1234561749]).
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Michael S. Weiss, the Company’s Executive Chairman and Chief Executive Officer stated "We want to thank Dr. Javier Pinilla-Ibarz, and the team at the H. Lee Moffitt Cancer Center & Research Institute for their important preclinical work examining the unique effect of umbralisib on T cells compared to other PI3K inhibitors. We have been encouraged by the safety profile reported in umbralisib clinical trials, and this preclinical data helps us to better understand the potential mechanistic rationale for the differentiated safety profile observed to date."
Dr. Javier Pinilla-Ibarz, Lymphoma Section Head, Director of Immunotherapy, Malignant Hematology Division at the H. Lee Moffitt Cancer Center in Tampa, Florida, and the senior author on the publication stated, "We have long been intrigued by the unique properties umbralisib has exhibited as a PI3K inhibitor. It is evident from the non-clinical work published today and from the clinical data seen thus far, that umbralisib is a novel molecule with differentiated effects on the T cell repertoire. We are pleased to contribute to elucidating the mechanisms of umbralisib and look forward to continuing our research."
The manuscript included preclinical data describing the effects of idelalisib, duvelisib and umbralisib on regulatory T cells (Tregs) on normal human T cells, T cells from CLL patients and T cells in an Eμ-TCL1 adoptive transfer mouse CLL model. While all three inhibitors exhibited anti-tumor efficacy in the Eμ-TCL1 CLL model, idelalisib or duvelisib-treated mice displayed increased immune-mediated toxicities, impaired function and reduced numbers of Tregs, whereas Treg number and function was more sustained in umbralisib-treated, CLL bearing mice. In addition, the manuscript also explored the effects of inhibition of CK1-epsilon on improvements in CLL Treg number and function and suggested the differentiated safety profile of umbralisib may be due to its role as a dual PI3K-delta/CK1-epsilon inhibitor.
These data are described further in the manuscript entitled, "The dual PI3K delta/CK1 epsilon inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells," which was published online in the First Edition section of Blood Advances, the Journal of the American Society of Hematology (ASH) (Free ASH Whitepaper). The online version of the article can be accessed at View Source