Chan Yoon Cheah, MBBS, Linear Clinical Research and Sir Charles Gairdner Hospital, Perth, Australia, shares an update on an ongoing Phase I trial investigating TG-1701, a selective BTK inhibitor as monotherapy and in combination with ublituximab and umbralisib (U2) in chronic lymphocytic leukemia (CLL), mantle cell lymphoma and Waldenström’s Macroglobulinemia. Both BTK inhibition and U2 have previously demonstrated superior efficacy over standard chemoimmunotherapy in patients with treatment-naïve or relapsed/refractory CLL. The primary objective of the study is to characterize the safety profile of TG-1701 and define a recommended Phase II dose. As of February 2021, 123 patients were treated with TG-1701. The study reported that TG-1701 was well-tolerated and the maximum tolerated dose for monotherapy was not reached at 400mg. At the data cut-off, 119 of 123 patients were evaluable for response. No complete responses (CRs) were confirmed amongst patients receiving TG-1701 monotherapy. In patients receiving TG-1701 plus U2, the objective response rate was 82.3%, with a CR rate of 23.5%. This interview took place at the virtual European Hematology Association (EHA) Congress 2021.