Results 1 to 10 of about 25,648 (169)

Progress in understanding the mechanisms of resistance to BCL-2 inhibitors

open access: yesExperimental 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

Semimechanistic Modeling to Guide Venetoclax Coadministration with Ritonavir and Digoxin

open access: yesClinical 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

The HDAC and PI3K dual inhibitor CUDC-907 synergistically enhances the antileukemic activity of venetoclax in preclinical models of acute myeloid leukemia

open access: yesHaematologica, 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

Interaction of Antifungal Drugs with CYP3A- and OATP1B-Mediated Venetoclax Elimination

open access: yesPharmaceutics, 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

Inhibition of p38 MAPK or immunoproteasome overcomes resistance of chronic lymphocytic leukemia cells to Bcl-2 antagonist venetoclax

open access: yesCell 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

On the Stability and Degradation Pathways of Venetoclax under Stress Conditions

open access: yesPharmaceutics, 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

Targeting BCL-2 regulated apoptosis in cancer [PDF]

open access: yes, 2018
The ability of a cell to undergo mitochondrial apoptosis is governed by pro- and anti-apoptotic members of the BCL-2 protein family. The equilibrium of pro- versus anti-apoptotic BCL-2 proteins ensures appropriate regulation of programmed cell death ...
Campbell, Kirsteen J.   +1 more
core   +1 more source

Retrospective, real‐life study of venetoclax plus azacitidine or low‐dose cytarabine in French patients with acute myeloid leukemia ineligible for intensive chemotherapy

open access: yesCancer 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

Another treatment option for relapsed or refractory chronic lymphocytic leukaemia. [PDF]

open access: yes, 2017
We hereby report the clinical and biologic features of 33 of 4680 (0.7%) patients with chronic lymphocytic leukemia (CLL), managed at 10 Italian centers, who developed Hodgkin lymphoma (HL), a rare variant of Richter syndrome.
Mauro, Francesca Romana
core   +1 more source

Pharmacological inhibition of BCL-2 with the FDA-approved drug venetoclax impairs longitudinal bone growth

open access: yesScientific Reports, 2023
Treatment-related skeletal complications are common in childhood cancer patients and survivors. Venetoclax is a BCL-2 inhibitor that has shown efficacy in hematological malignancies in adults and is being investigated in pediatric cancer clinical trials ...
Lilly Velentza   +5 more
doaj   +1 more source

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