On June 15, 2018 TG Therapeutics, Inc. (NASDAQ: TGTX), reported the presentation of an integrated analysis of long term safety data of umbralisib (TGR-1202), the Company’s PI3K delta inhibitor, either dosed as a single agent and in combination, in patients with relapsed or refractory lymphoid malignancies, as well as the first preclinical data presentation of TG-1701, the Company’s orally available and covalently-bound BTK inhibitor (Press release, TG Therapeutics, JUN 15, 2018, View Source [SID1234527350]). Data from these trials are being presented today during the 23rd Congress of the European Hematology Association (EHA) (Free EHA Whitepaper).

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Michael S. Weiss, the Company’s Executive Chairman and Chief Executive Officer, stated, "We are extremely pleased to present updated data from our integrated safety analyses of umbralisib. There is a generally held belief that severe toxicities are more common following 6 months of exposure on a PI3K delta inhibitor. While this has held true for first generation delta inhibitors, we are pleased to present data from 177 patients on daily umbralisib for more than 6 months, ranging upwards of 5+ years, and believe the long-term follow-up data demonstrates that umbralisib has a differentiated safety profile, uniquely distinct from prior generation PI3K delta inhibitors." Mr. Weiss continued, "The differentiated safety profile of umbralisib is critical as we think about potential triple and quad combination strategies, especially in combination with our novel, proprietary BTK inhibitor, TG-1701, for which we also presented some exciting pre-clinical data. The kinase profile of TG-1701 looks quite competitive with the most specific BTK inhibitors and more selective than ibrutinib. We look forward to seeing more data on TG-1701 and expect to open a TG sponsored Phase 1/2 trial later this year."

Highlights from today’s presentations include the following:

Poster Presentation: Long term integrated safety analysis of umbralisib (TGR-1202), a PI3K delta/CK1-epsilon inhibitor with a differentiated safety profile in patients with relapsed/refractory lymphoid malignancies

This presentation builds on a prior integrated analysis of 347 patients with relapsed or refractory lymphoid malignancies presented last year. The presentation includes data that were pooled from 4 completed or ongoing Phase 1 or 2 studies containing umbralisib, focusing on 177 patients who have been on daily umbralisib for a minimum of 6 months. Patients were heavily pretreated, with 45% of patients having seen 3 or more prior lines of therapy.

Highlights from this poster include:

● Umbralisib continues to exhibit a differentiated safety profile compared to prior generation PI3K delta inhibitors

● 177 patients have been treated with daily umbralisib for 6+ months, with a median duration of exposure of 1.3 years, and 33% patients on drug 2+ years and the longest patients on daily umbralisib for over 5 years

o Serious adverse events occurring in >1% of patients were limited to pneumonia (3%), diarrhea (2%), and cellulitis (2%)

o Only 2% of patients discontinued as a result of diarrhea/colitis after being on umbralisib for more than 6 months
oDiscontinuations due to other adverse events (AEs) of interest for prior generation PI3K inhibitors were also rare

Poster Presentation: TG-1701 is a novel, orally available, and covalently-bound BTK inhibitor

● TG-1701, a novel, specific and covalent BTK inhibitor, is more selective than ibrutinib toward a set of kinases

● BTK occupancy assays in vitro and in vivo suggest that 100% occupancy can be reached using low doses of TG-1701 in human dose escalation clinical trial

● In pre-clinical experiments, TG-1701 inhibited the phosphorylation of BTK and other kinases downstream of the BCR pathway.

● In cellular and animal models of b-cell malignancies, TG-1701 demonstrated similar antitumor efficacy to ibrutinib and acalabrutinib