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Umbralisib Shows Early Promise in CLL and Lymphoma

Jason Harris
Published: Wednesday, Feb 21, 2018

Owen A. O'Connor, MD, PhD

Owen A. O'Connor, MD, PhD
The PI3K-delta inhibitor umbralisib (TGR-1202) induced an objective response rate (ORR) of 37% in patients with relapsed/refractory lymphoma or chronic lymphocytic leukemia (CLL), according to phase I findings published in The Lancet Oncology.1

“Is it possible that the time has come for PI3Kδ signaling inhibition to come out of the shadows and become an attractive target again? The clinical activity and safety reported with umbralisib in this study is encouraging,” she wrote. “Ongoing combination trials might achieve the desirable fine balance of efficacy and safety without increased toxicities, but only time will tell whether the unique mechanism of dual inhibition of PI3Kδ and casein kinase-1ε can be used in a safe manner while preserving patients' quality of life.”


  1. Burris HA, Flinn IW, Patel MR, et al. Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study [published online February 20, 2018]. Lancet Oncol. doi: 10.1016/ S1470-2045(18)30082-2
  2. Barrientos JC. Can umbralisib bring PI3Kδ out of the shadows? [published online February 20, 2018]. Lancet Oncol. doi: 10.1016/S1470-2045(18)30154-2.

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