Full Press Release Details
Therapeutics, Inc. Announces Preclinical Data Presentations for
TGR-1202 at the 58th American Society of
Hematology Annual Meeting
Preclinical work may offer rationale for the differentiated
activity and safety effects of TGR-1202
DIEGO, CA (December 5, 2016) - TG Therapeutics, Inc. (NASDAQ:TGTX),
announced the presentation yesterday of two preclinical data sets,
one oral presentation and one poster presentation, for TGR-1202,
the Company's once-daily PI3K delta inhibitor, at the
American Society of Hematology (ASH) annual meeting in San Diego,
S. Weiss, the Company's Executive Chairman and Interim Chief
Executive Officer, stated, "We want to thank the teams at Columbia
and Moffitt for their extensive laboratory work on TGR-1202 to
better understand the mechanism of action and impact on the immune
system. The preclinical data they have generated helps to better
explain and perhaps offer a rationale for the differentiated safety
profile seen with TGR-1202 as compared to earlier generation PI3K
delta inhibitors. We believe these preclinical findings along with
the robust safety and efficacy data we have observed in the clinic,
support our belief that TGR-1202 is a differentiated best in class
PI3K delta inhibitor. We look forward to continuing our research
collaborations with Columbia and Moffitt and to presenting updated
safety and efficacy data for TGR-1202 to further confirm its unique
presentation today has really begun to shed some long-needed light
on the important differences among the PI3K delta inhibitors. His
work has identified that a novel kinase important in the PI3K
pathway, CK-1epsilon, is uniquely inhibited by TGR-1202, which may
explain the drug's effects on c-Myc. These chemical
differences may also help to explain the important immunologic
differences in the safety profiles of these agents, stated
Dr. Owen A. O'Connor, Professor
of Medicine and Experimental Therapeutics, Director Lymphoid
Malignancies at Columbia Presbyterian Medical
following summarizes the oral presentation and poster presentation
which occurred yesterday:
Silencing c-Myc Translation as a Therapeutic Strategy through
Targeting PI3K Delta and CK1 Epsilon in Hematological Malignancies
(Abstract Number 291)
oral presentation includes data from the manuscript titled,
Silencing c-Myc Translation as a Therapeutic Strategy
through Targeting PI3K Delta and CK1 Epsilon in Hematological
Malignancies, which was recently published in Blood, the Journal of the American
Society of Hematology. The presentation was delivered by Changchung
Deng, MD, PhD of Columbia Presbyterian Medical Center and included
the following highlights:
carfilzomib, but not combinations of other drugs in the same
classes, synergistically inhibit c-Myc translation and c-Myc
dependent gene transcription, by potently inhibiting
phosphorylation of 4E-BP1;
carfilzomib synergistically induce apoptosis in lymphoma cells
through targeting c-Myc, whereas the other combinations did
idelalisib or duvelisib, was found to uniquely inhibit casein kinase-1 (CK1) epsilon;
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.
Presentation: Modulation of T Cell Compartment in a
Preclinical CLL Murine Model By a Selective PI3K Delta Inhibitor,
TGR-1202 (Abstract Number 3236)
poster presentation included preclinical data describing the
differential regulation of human T-cells by TGR-1202 in a
preclinical CLL murine model. Highlights from this poster
duvelisib oral administration demonstrated
comparable efficacy by reducing CLL burden over time in leukemic
duvelisib both targeted the T cell population in vivo, however:
maintained the number of Tregs and Th17 cells and expression of
functional markers on Tregs compared to duvelisib treatment
in vivo and ex vivo; and
in greater disruption of Treg/Th17 ratio compared to TGR-1202
in vivo, which may have
implications for occurrence of autoimmune-like organ
PRESENTATION DETAILS:
Copies of the above referenced presentations are
available on the Company's website at www.tgtherapeutics.com,
located on the Publications page.
TG THERAPEUTICS INVESTOR & ANALYST EVENT DETAILS:
TG Therapeutics will also host an investor and
analyst reception on Monday, December 5th,
2016 beginning at 8:00pm PT. The event will take place at the
Marriott Gaslamp, in San Diego, California, in the Presidio AB
will be webcast live and will be available on the Events page,
located within the Investors & Media section of the
Company's website at
www.tgtherapeutics.com, as well as
archived for future review. This event will also be broadcast via
conference call. In order to access the conference line,
please call 1-877-407-8029 (U.S.), 1-201-689-8029 (outside the
U.S.), and reference Conference Title: TG Therapeutics 2016
Investor & Analyst Event.
TG THERAPEUTICS, INC.
Therapeutics is a biopharmaceutical company focused on the
acquisition, development and commercialization of novel treatments
for B-cell malignancies and autoimmune diseases. Currently, the
company is developing two therapies targeting hematological
malignancies and autoimmune diseases. TG-1101 (ublituximab) is a
novel, glycoengineered monoclonal antibody that targets a specific
and unique epitope on the CD20 antigen found on mature
B-lymphocytes. TG Therapeutics is also developing TGR-1202, an
orally available PI3K delta inhibitor. The delta isoform of PI3K is
strongly expressed in cells of hematopoietic origin and is believed