name: | Umbralisib |
ATC code: | L01EX25 | route: | oral |
n-compartments | 2 |
Umbralisib is an oral, selective phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitor with additional inhibition of casein kinase 1 epsilon (CK1ε). It is used for the treatment of certain B-cell malignancies, including marginal zone lymphoma and follicular lymphoma. It was approved by the FDA but was voluntarily withdrawn from the market in 2022 due to safety concerns.
Pharmacokinetic parameters as observed in adult cancer patients receiving oral umbralisib as a single agent.
Burris, HA, et al., & O'Connor, OA (2018). 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. The Lancet. Oncology 19(4) 486–496. DOI:10.1016/S1470-2045(18)30082-2 PUBMED:https://pubmed.ncbi.nlm.nih.gov/29475723