On April 18, 2016 TG Therapeutics, Inc. (Nasdaq:TGTX) reported the presentation of preclinical data describing the differential regulation of human T-cells by TGR-1202 in a poster presentation at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2016, which is being held April 16 – 20, 2016 at the Ernest N. Morial Convention Center in New Orleans, Louisiana (Press release, TG Therapeutics, APR 18, 2016, View Source [SID:1234510981]).
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As part of an ongoing research collaboration with the H. Lee Moffitt Cancer Center and Research Institute in Tampa, FL, data was generated comparing TGR-1202 with the PI3K-delta inhibitors idelalisib and duvelisib in in-vitro models assessing the impact on T-cell subsets. Key conclusions from the poster are as follows:
TGR-1202 exhibits dose dependent cytotoxicity against human T cells beginning 25uM, comparable to the PI3K-delta inhibitors idelalisib and duvelisib,
TGR-1202 allows relative conservation of TH2 cytokine expression and GATA-3 mRNA compared to other PI3K-delta inhibitors idelalisib and duvelisib
Regulatory T cell (Treg) population number and function is reduced overall after treatment with all three agents but to a lesser degree in TGR-1202 treated samples
TGR-1202 does not robustly reduce the expression of PD-1 and CTLA-4 on Tregs, suggesting that a suppressive phenotype is maintained to a greater extent compared to idelalisib and duvelisib.
Michael S. Weiss, the Company’s Executive Chairman and Interim Chief Executive Officer, stated, "Many of the adverse events associated with existing PI3K-delta inhibitors such as colitis and hepatic toxicity, and most recently with opportunistic infections, are thought to be related to T-cell immune mediated mechanisms. This pre-clinical data now begins to elucidate key differences in the impact of these inhibitors on human T-cell subsets, which may explain the differentiated safety profile observed with TGR-1202 to date in the clinic. These data represent the first step in improving our understanding and we look forward to continuing our research collaboration with the team at Moffitt."
PRESENTATION DETAILS
A copy of the poster is available on the Company’s website at www.tgtherapeutics.com, located on the Publications Page, within the Pipeline section.