TG Therapeutics (TGTX) Announces Publication of TGR-1202 Preclinical Data

October 27, 2016 7:33 AM EDT

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TG Therapeutics (NASDAQ: TGTX) announced the publication of preclinical data describing the synergy of the Company’s next generation, once daily, PI3K-delta inhibitor, TGR-1202, with the proteasome inhibitor carfilzomib and the unique effects of the combination to silence c-Myc in various preclinical lymphoma and myeloma models. In addition, the manuscript also, for the first time, reports on TGR-1202’s unique complimentary mechanism of inhibiting the protein kinase casein kinase-1 (CK1) epsilon, which may contribute to the silencing of c-Myc and explain TGR-1202’s clinical activity in aggressive lymphoma, including Diffuse Large B-cell Lymphoma (DLBCL). The preclinical data are described further in the manuscript titled, “Silencing c-Myc Translation as a Therapeutic Strategy through Targeting PI3K Delta and CK1 Epsilon in Hematological Malignancies,” which was published online yesterday in the First Edition section of Blood, the Journal of the American Society of Hematology. The online version of the article can be accessed at

"We want to thank Dr. Deng, Dr. O’Connor, and the team from Columbia Presbyterian Medical Center and the Center for Lymphoid Malignancies for their exhaustive and comprehensive interrogation of TGR-1202 and the elucidation of this novel complimentary mechanism. For quite some time we have been presenting the differentiated safety profile observed with TGR-1202 and the differentiated chemical structure compared to other PI3K-delta inhibitors. This preclinical work demonstrates that TGR-1202 not only potently targets PI3K-delta but in addition uniquely targets a relatively novel kinase, CK1-epsilon, which perhaps offers another rationale for the differentiated activity and safety effects we have seen in patients. We look forward to exploring this exciting concept further in the recently launched clinical trial,” stated Michael S. Weiss, the Company's Executive Chairman and Interim Chief Executive Officer.

“The data in this paper clearly demonstrates that TGR-1202 and carfilzomib in combination is markedly synergistic and selectively silenced c-Myc compared to combinations with idelalisib and bortezomib. In addition, we were excited to identify and elucidate the previously unknown mechanism of TGR-1202 and its effect on CK1 epsilon which was not exhibited by either idelalisib or duvelisib based on a kinome profiling platform analyzed. We believe this research may help explain in part the preliminary activity demonstrated by TGR-1202 in DLBCL. Given TGR-1202’s distinct safety profile as a single agent and its uniquely demonstrated ability to be used in combination with other agents, we look forward to bringing this novel combination to the clinic in our recently announced Phase 1 study of TGR-1202 and carfilzomib in patients with lymphoma,” stated Dr. Owen A. O’Connor, Professor of Medicine and Experimental Therapeutics, Director Lymphoid Malignancies at Columbia Presbyterian Medical Center.

Based on this extensive preclinical work, the Company recently announced the launch of a Phase 1/2 study to evaluate the safety and efficacy of TGR-1202 in combination with carfilzomib, in patients with relapsed or refractory lymphoma, particularly c-Myc driven lymphomas which are aggressive in nature. This study is currently open to enrollment at the Center for Lymphoid Malignancies, Columbia Presbyterian Medical Center, New York, NY. More information on this clinical study can be found at

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