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TG Therapeutics, Inc. Announces Presentation of Encouraging Clinical Activity of TGR-1202 in an Ongoing Multi-center Phase I Clinical Study All evaluable CLL patients treated with once daily TGR-1202 at 800 mg exhibited

Key Takeaway: TG Therapeutics, Inc. Announces Presentation of Encouraging Clinical Activity of TGR-1202 in an Ongoing Multi-center Phase I Clinical Study NEW YORK, Dec 9, 2013 - TG Therapeutics, Inc. (Nasdaq: TGTX), an innovative, clinical-stage biopharmaceutical company today announced cl

Full Press Release Details

TG Therapeutics, Inc. Announces Presentation
of Encouraging Clinical Activity of TGR-1202 in an
Ongoing Multi-center Phase I Clinical Study
NEW YORK, Dec 9, 2013 - TG Therapeutics, Inc. (Nasdaq:
TGTX), an innovative, clinical-stage biopharmaceutical company today announced clinical results from an ongoing first-in-human
Phase I single agent study of TGR-1202, the Company's oral PI3K-Delta inhibitor being developed for the treatment of select
hematologic malignancies. Data from the Phase I dose-escalation study are being presented today at a poster session during the
55th American Society of Hematology Meeting (ASH) in New Orleans, LA.
The multi-center Phase I study is being conducted in the United
States in patients with relapsed and refractory Chronic Lymphocytic Leukemia (CLL), non-Hodgkin's Lymphoma (NHL) and other
select hematologic malignancies with no limit on prior therapies. Once daily oral administration of TGR-1202 is being evaluated
in a 3+3 dose escalation design with the primary study objectives being to determine the safety and tolerability, pharmacokinetic
profile, and maximum tolerated dose (MTD) of TGR-1202 with secondary objectives of assessing pharmacodynamics and preliminary efficacy
Today's poster presentation includes data from 22 patients
with relapsed and refractory hematologic malignancies treated with TGR-1202 at doses ranging from 50 mg to 1200 mg QD. Evaluable
patients included CLL (10), indolent NHL (5), Hodgkin's Lymphoma (3) and one patient each with Mantle Cell Lymphoma, Germinal
Center Diffuse Large B-cell Lymphoma (DLBCL) and Hairy Cell Leukemia.
Key data presented from the study include:
Safety and Tolerability
TGR-1202 appears to be well-tolerated with no dose-related trends
in adverse events observed. Grade 3 events have been limited and no patient has discontinued study drug due to an adverse event.
Notably, of the 22 patients evaluable for safety, no hepatotoxicity or Grade 3 or greater GI side effects were observed. No MTD
has been achieved and dose escalation is ongoing, now dosing patients at 1800 mg QD.
Pharmacokinetic evaluation for TGR-1202 displays linear kinetics
through 1200 mg QD. TGR-1202 was found to be rapidly absorbed (Tmax of approximately 2 hours) with an estimated effective steady
state half-life (t½) exceeding 24 hours which supports once daily (QD) oral administration of TGR-1202.
Nineteen patients were evaluable for efficacy, which included
all patients up through the 800 mg QD cohort. Patients in the 1200mg QD cohort were too early to evaluate.
Nodal responses were observed at the 800 mg cohort. In this
cohort, 100% of the evaluable CLL patients demonstrated significant nodal reductions of which 3 of 4 patients achieved a nodal
partial response (>50% reduction) at the first response assessment. In addition to the activity observed in CLL, a heavily pre-treated
patient (6 prior lines of therapy) with refractory Germinal Cell DLBCL, an aggressive form of NHL, achieved a 40% reduction in
tumor burden at first response assessment on a dose of 400 mg QD of TGR-1202 and continues on study (5+ months).
As of December 1, 55% of patients remained on study, with on-study
durations ranging from 1 month for the recent 1200 mg cohort patients to 9+ months. Patients in previous cohorts are allowed to
dose-escalate once a higher dose level has been cleared for safety evaluation, as such, all patients on study are currently being
treated at 800 mg QD or higher.
Enrollment into the study continues, with an expansion cohort
recently opened at 800 mg QD as dose escalation continues.
Dr. Michael Savona, the Principal Investigator for the study
and Director of Leukemia Research at the Sarah Cannon Research Institute in Nashville, TN stated "TGR-1202 has an excellent
safety profile and linear pharmacokinetics in our Phase I study. The liver toxicity seen with similar B-cell receptor antagonists
has thus far been absent. Likewise, we are excited to see considerable activity at doses above 400mg, and continue to escalate."
Michael S. Weiss, the Company's Executive Chairman and
Interim CEO commented on the data, "We are very encouraged by these initial results which suggest that TGR-1202 is well-tolerated
with evidence of meaningful activity in a relapsed/refractory patient population, despite not yet having established our MTD. While
expanding enrollment at the 800 mg dose level, we look forward to continuing dose-escalation in this trial to fully characterize
the pharmacokinetic profile of TGR-1202 as well as the dose exposure/ response relationship with the goal of identifying an optimal
The poster, entitled "A Phase I Dose Escalation Study
of TGR-1202, a Novel PI3K-delta Inhibitor for Patients with Relapsed or Refractory Hematologic Malignancies," is being presented
on Monday, December 9, 2013 from 6:00 - 8:00PM CT in Hall G at the Ernest N. Morial Convention Center, New
Orleans, LA, a copy of which is available at www.tgtherapeutics.com/pipeline/publications.cfm.
ABOUT TG THERAPEUTICS, INC.
TG Therapeutics is an innovative, clinical-stage biopharmaceutical
company focused on the acquisition, development and commercialization of medically important pharmaceutical products for the treatment
of cancer and other underserved therapeutic needs. Currently, the company is developing two therapies targeting hematological malignancies.
TG-1101 (ublituximab) is a novel, glycol-engineered 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, jointly
with Rhizen Pharmaceuticals S A. The delta isoform of PI3K is strongly expressed in cells of hematopoietic origin and is believed
to be important in the proliferation and survival of B-lymphocytes. Both TG-1101 and TGR-1202 are in clinical development for patients
with hematologic malignancies. TG Therapeutics is headquartered in New York City.
Cautionary Statement
Some of the statements included in this press release, particularly
those anticipating future clinical trials and business prospects for TG-1101 and TGR-1202 may be forward-looking statements that
involve a number of risks and uncertainties. For those statements, we claim the protection of the safe harbor for forward-looking
statements contained in the Private Securities Litigation Reform Act of 1995. Among the factors that could cause our actual
results to differ materially are the following: our ability to successfully and cost-effectively complete pre-clinical and clinical
trials for TG-1101 and TGR-1202; the risk that early pre-clinical and clinical results that supported our decision to move forward
with TG-1101 and TGR-1202 will not be reproduced in additional patients or in future studies; the risk that TGR-1202 will not produce
satisfactory safety and efficacy results to warrant further development following completion of the current phase 1 study; the
risk that the data (both safety and efficacy) from future clinical trials will not coincide with the data produced from prior pre-clinical
and clinical trials; our ability to achieve the milestones we project over the next year; our ability to manage our cash in line
with our projections, and other risk factors identified from time to time in our reports filed with the Securities and Exchange
Commission. Any forward-looking statements set forth in this press release speak only as of the date of this press release. We
do not undertake to update any of these forward-looking statements to reflect events or circumstances that occur after the date
hereof. This press release and prior releases are available at www.tgtherapeutics.com. The information found on our
website is not incorporated by reference into this press release and is included for reference purposes only.
CONTACT: Jenna Bosco
Director- Investor Relations
TG Therapeutics, Inc.
Telephone: 212.554.4484
Email: ir@tgtxinc.com
Last updated: Dec 9, 2013