- Based on healthy subject bioequivalence studies, improvements in absorption are projected to increase exposure levels by approximately 3-4 fold
NEW YORK, May 8, 2014 (GLOBE NEWSWIRE) -- TG Therapeutics, Inc. (Nasdaq:TGTX), an innovative, clinical-stage biopharmaceutical company, today announced that a micronized (reduced particle size) formulation for the Company's novel, once-daily PI3K-delta inhibitor, TGR-1202, has demonstrated improved pharmacokinetics with approximately double the TGR-1202 exposure (AUC) in a healthy subject bioequivalence study. A second food-effect study in healthy subjects which evaluated the relative oral bioavailability and pharmacokinetics of TGR-1202 in a fed and fasted-state also demonstrated an approximate doubling in absorption with fed-state dosing. Together, the Company believes that these modifications may result in an approximately 3-4 fold increase in exposure over that seen in the ongoing Phase 1 study. Results from these studies will be included in a presentation of updated data from the ongoing Phase 1 study of TGR-1202 in patients with relapsed and refractory hematologic malignancies at the American Society of Clinical Oncology Meeting (ASCO) later this month.
Preliminary data from the ongoing Phase 1 study of TGR-1202, which was presented at the 2013 American Society of Hematology (ASH) Annual Meeting, demonstrated promising clinical activity with a favorable safety profile, notably lacking the hepatotoxicity observed with similar PI3K-delta inhibitors. In this study, TGR-1202 has been dosed as high as 1800 mg QD in a fasting state and as high as 1200 mg QD in a fed-state, with no maximum tolerated dose (MTD) achieved to date and no concerning safety trends identified. Dose-escalation has resumed in this ongoing Phase I study with micronized TGR-1202 dosed at 200 mg QD in a fed-state.
"We are excited to introduce this improved formulation of TGR-1202 into our ongoing Phase 1 study at significantly lower doses, starting at 200 mg QD, and expect to see exposure levels comparable to those seen at much higher doses of the original formulation," stated Michael S. Weiss, the Company's Executive Chairman and Interim Chief Executive Officer. Mr. Weiss continued, "2014 is off to an exciting start and we look forward to providing clinical updates for TG-1101 and TGR-1202, both as single agents and in combination at a number of upcoming conferences, including ASCO and EHA."
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, 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 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, the timing of commencing, completing or reporting such trials, the business prospects for TG-1101 and TGR-1202, and the potential benefits that might be achieved with the micronized formulation and fed-state dosing 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 the enhanced absorption seen in the healthy human volunteer bioequivalence studies will not be seen in whole or in part when the modified formulation and fed-state dosing are studied in patients with B-cell malignancies; the risk that TGR-1202 will not produce satisfactory safety and efficacy results to warrant further development following the 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; the risk that trials will take longer to enroll than expected; 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.
TGTX - G