Results 1 to 10 of about 25,087 (209)
Na+/H+ Exchanger 1 Inhibition Overcomes Venetoclax Resistance in Acute Myeloid Leukemia [PDF]
CellsDespite advances with novel targeted agents (e.g., BCL-2 or IDH inhibitors) combined with chemotherapy for acute myeloid leukemia (AML), drug resistance persists.
Shin Young Hyun +4 more
doaj +2 more sources
Clonal dynamics towards the development of venetoclax resistance in chronic lymphocytic leukemia
Nature Communications, 2018 BCL2-inhibitor venetoclax is used to treat relapsed/refractory chronic lymphocytic leukemia (CLL). Here, the authors show the clonal dynamics towards venetoclax resistance by performing whole-exome sequencing of 8 CLL patients undergoing venetoclax ...
Olaf Merkel +2 more
exaly +2 more sources
Structures of BCL-2 in complex with venetoclax reveal the molecular basis of resistance mutations
Nature Communications, 2019 The BCL-2 mutation G101V reduces venetoclax affinity and confers drug resistance in patients with chronic lymphocytic leukaemia. Here, the authors present crystal structures and biochemical analyses of venetoclax bound to BCL-2 and the G101V mutant ...
Richard W Birkinshaw +2 more
exaly +2 more sources
Progress in understanding the mechanisms of resistance to BCL-2 inhibitors
Experimental Hematology & Oncology, 2022 Venetoclax is a new type of BH3 mimetic compound that can target the binding site in the BCL-2 protein and induce apoptosis in cancer cells by stimulating the mitochondrial apoptotic pathway.
Yilan Xu, Haige Ye
doaj +1 more source
Haematologica, 2020 Venetoclax is a promising agent in the treatment of acute myeloid leukemia, though its antileukemic activity is limited to combination therapies. Mcl-1 downregulation, Bim upregulation, and DNA damage have been identified as potential ways to enhance ...
Xinyu Li +17 more
doaj +1 more source
Semimechanistic Modeling to Guide Venetoclax Coadministration with Ritonavir and Digoxin
Clinical and Translational Science, 2020 Venetoclax is a cytochrome P450, family 3, subfamily A (CYP3A) substrate and was shown to inhibit P‐gp efflux transporters in vitro. To quantify the impact of CYP3A inhibition by ritonavir on venetoclax disposition and P‐gp inhibition by venetoclax on ...
Ali A. Alhadab +2 more
doaj +1 more source
Interaction of Antifungal Drugs with CYP3A- and OATP1B-Mediated Venetoclax Elimination
Pharmaceutics, 2022 Venetoclax, a BCL-2 inhibitor used to treat certain hematological cancers, exhibits low oral bioavailability and high interpatient pharmacokinetic variability. Venetoclax is commonly administered with prophylactic antifungal drugs that may result in drug
Eric D. Eisenmann +9 more
doaj +1 more source
On the Stability and Degradation Pathways of Venetoclax under Stress Conditions
Pharmaceutics, 2020 Venetoclax is an orally bioavailable, B-cell lymphoma-2 (BCL-2) selective inhibitor, used for the treatment of various types of blood cancers, such as chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL).
Nina Žigart +3 more
doaj +1 more source
Cell Death and Disease, 2022 Chronic lymphocytic leukemia (CLL) is a hematological neoplasm of CD19-positive mature-appearing B lymphocytes. Despite the clinical success of targeted therapies in CLL, the development of resistance diminishes their therapeutic activity.
Damjan Avsec +6 more
doaj +1 more source
Cancer Medicine, 2023 Background Recently, the combination of venetoclax plus a hypomethylating agent (HMA; azacitidine ordecitabine) or low‐dose cytarabine (LDAC) showed promise in Phase III trials in previously untreated AML.
Louise Laloi +29 more
doaj +1 more source