– Based on healthy subject bioequivalence studies, improvements in absorption are projected to increase exposure levels by approximately 3-4 fold
NEW YORK, NY, USA I May 8, 2014 I TG Therapeutics, Inc. (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.
SOURCE: TG Therapeutics
Post Views: 168
– Based on healthy subject bioequivalence studies, improvements in absorption are projected to increase exposure levels by approximately 3-4 fold
NEW YORK, NY, USA I May 8, 2014 I TG Therapeutics, Inc. (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.
SOURCE: TG Therapeutics
Post Views: 168
