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TG Therapeutics Says TGR-1202 Appears Well Tolerated, Grade 3 Events Have Been Limited

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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 55^th 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 signals.

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.

Pharmacokinetics

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 (t[½]) exceeding 24 hours which supports once daily (QD) oral administration of TGR-1202.   

Clinical Activity

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.

Posted-In: News FDA

 

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