On February 21, 2018 TG Therapeutics, Inc. (NASDAQ:TGTX) reported the publication of the results from the Phase 1 first-in-human study of umbralisib (TGR-1202), the Company’s novel once-daily PI3K delta inhibitor, in The Lancet Oncology (Press release, TG Therapeutics, FEB 21, 2018, View Source [SID1234524106]). The paper includes safety and efficacy information from 90 patients with relapsed or refractory b-cell malignancies, including patients with Chronic Lymphocytic Leukemia (CLL) and various forms of lymphoma treated with single agent umbralisib. In this study, umbralisib was well tolerated with a favorable safety profile distinct from prior generation PI3K delta inhibitors. Grade 3/4 immune mediated AEs commonly associated with other PI3K delta inhibitors were limited, with transaminitis occurring in 3 patients ( < 3%), and pneumonia and colitis in 2 patients each ( < 2% for each). Notably, both events of colitis occurred at doses exceeding the current Phase 3 dose. Umbralisib was also clinically active with 85% of relapsed or refractory CLL patients achieving an objective response (50% per IWCLL criteria; 35% a partial response with lymphocytosis) and 53% of patients with relapsed or refractory Follicular Lymphoma (FL) achieving an objective response, including 2 patients with a Complete Response (CR).
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These data, in addition to the unique structural attributes and enhanced selectivity profile of umbralisib, are described further in the manuscript entitled, "Umbralisib, a novel PI3K and casein kinase-1 epsilon inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study," which was published yesterday in The Lancet Oncology. The online version of the article can be accessed at http://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(18)30082-2/fulltext.
Dr. Howard A. Burris, the Chief Medical Officer and Executive Director of the Drug Development Program at the Sarah Cannon Research Institute in Nashville, TN, and lead author stated, "We are pleased to have treated the first patient ever with umbralisib over 5 years ago and believe it has an important place in the treatment landscape for patients with hematologic malignancies. Several patients from this Phase 1 study are still on study today, approaching 5 years of continuous daily therapy, speaking to both the safety and efficacy profile of this unique agent."
Dr. Owen A. O’Connor, Professor of Medicine and Experimental Therapeutics, Director Lymphoid Malignancies at Columbia Presbyterian Medical Center, stated, "Pre-clinically umbralisib has a very unique profile, selectively inhibiting both PI3K delta and CK1 epsilon, as previously described in our Blood paper. The clinical results in this paper support our thesis that the differentiated preclinical profile explains the differences seen in the clinic between umbralisib and the other PI3K delta inhibitors."
"We want to thank Dr. Burris, Dr. O’Connor and all the investigators who participated in this first-in-human Phase 1 trial for umbralisib, which has set the stage for our ongoing pivotal UNITY-CLL and UNITY-NHL trials. With over 1,000 patients treated with umbralisib to date, we and the investigators believe umbralisib is a differentiated, active and more selective PI3K delta inhibitor that exhibits a favorable safety profile as compared to prior generation molecules," stated Michael S. Weiss, the Company’s Executive Chairman and Chief Executive Officer.