Umbralisib
Umbralisib is an experimental oral PI3K delta inhibitor (previously known as RP5264 and TGR 1202).[1]
It also inhibits CK1 epsilon.[2]
It has had clinical studies for Chronic lymphocytic leukemia (CLL).[3][4]
Three year data (including Follicular lymphoma and DLBCL) was announced June 2016.[5]
It is in combination trials for various leukemias and lymphomas, e.g., Mantle cell lymphoma (MCL).[6][7] and other lymphomas.[8]
References
- ↑ Clinical trial number NCT01767766 for "Evaluate the Safety and Efficacy of TGR 1202 in Patients With Relapsed or Refractory Hematologic Malignancies" at ClinicalTrials.gov
- ↑ Umbralisib Shows Early Promise in CLL and Lymphoma Feb 2018
- ↑ Novel BTK, PI3K Inhibitors on Horizon for Relapsed CLL. March 2016
- ↑ Therapy Focus - TG Could Benefit From Zydelig Setback. March 2016
- ↑ TG Therapeutics Inc.: TG Therapeutics, Inc. Announces First Patient Enrolled in the Registration-Directed UNITY-DLBCL Phase 2b Trial. June 2016
- ↑ Clinical trial number NCT02268851 for "A Phase I/Ib Safety and Efficacy Study of the PI3K-delta Inhibitor TGR-1202 and Ibrutinib in Patients With CLL or MCL" at ClinicalTrials.gov
- ↑ Follow-Up Data for Combination of TGR-1202 (umbralisib) plus Ibrutinib in Patients with Relapsed or Refractory CLL and MCL. 2017
- ↑ Clinical trial number NCT02793583 for "Study to Assess the Efficacy and Safety of Ublituximab + TGR-1202 With or Without Bendamustine and TGR-1202 Alone in Patients With Previously Treated Non-Hodgkins Lymphoma (UNITY-NHL)" at ClinicalTrials.gov
Further reading
- Barrientos, Jacqueline C (2018). "Can umbralisib bring PI3Kδ out of the shadows?". The Lancet Oncology. doi:10.1016/S1470-2045(18)30154-2. PMID 29475725.
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