Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor [PDF]
More and more targeted agents become available for B cell malignancies with increasing precision and potency. The first-in-class Bruton’s tyrosine kinase (BTK) inhibitor, ibrutinib, has been in clinical use for the treatment of chronic lymphocytic ...
Jingjing Wu, Mingzhi Zhang, Delong Liu
doaj +2 more sources
Acalabrutinib Versus Venetoclax Plus Obinutuzumab in Treatment-Naive Chronic Lymphocytic Leukemia: A Real-World Propensity Score-Matched Study. [PDF]
In a real‐world matched cohort study of treatment‐naïve TP53 wild‐type CLL patients, venetoclax plus obinutuzumab demonstrated significantly longer time to next treatment and improved 4‐year overall survival compared to first‐line acalabrutinib. Despite higher rates of cytopenias and infections, the venetoclax‐based regimen showed superior efficacy ...
Liao PW, Ko BS, Su YC, Chao WT, Teng CJ.
europepmc +2 more sources
Acalabrutinib in Chronic Lymphocytic Leukemia: Pharmacology and Emerging Clinical Perspectives. [PDF]
ABSTRACT Acalabrutinib, a second‐generation Bruton's tyrosine kinase inhibitor (BTKi), is characterized by enhanced specificity and selectivity for BTK with minimal off‐target effects, offering a significant evolution in the treatment of chronic lymphocytic leukemia (CLL). Its mechanism of action, a covalent binding to Cys481 within the BTK active site,
Gaidano G, Danesi R.
europepmc +2 more sources
EHA Guidelines on management of chronic lymphocytic leukemia and Richter transformation. [PDF]
Abstract Previous editions of the European guidelines for the management of chronic lymphocytic leukemia (CLL) were developed by experts in CLL under the auspices of the European Society for Medical Oncology (ESMO). These previous editions have served as a reference text for many physicians caring for patients with CLL.
Eichhorst B +13 more
europepmc +2 more sources
Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia [PDF]
Background Irreversible inhibition of Bruton\u27s tyrosine kinase (BTK) by ibrutinib represents an important therapeutic advance for the treatment of chronic lymphocytic leukemia (CLL).
Jones, J. A. +10 more
core +3 more sources
The acalabrutinib-bound BTK kinase domain.
a. Overall structure of the BTK KD/acalabrutinib complex. Key features of the kinase domain are labeled. Acalabrutinib is shown in yellow sticks and covalently attached to Cys481. Activation loop is colored red with Tyr551 shown in sticks.
Amy H. Andreotti (366314) +1 more
core +1 more source
Acalabrutinib Versus Ibrutinib in Previously Treated Chronic Lymphocytic Leukemia: Results of the First Randomized Phase III Trial [PDF]
PURPOSE: Among Bruton's tyrosine kinase inhibitors, acalabrutinib has greater selectivity than ibrutinib, which we hypothesized would improve continuous therapy tolerability.
Rothbaum, Wayne +52 more
core +1 more source
Acalabrutinib is a second generation Bruton's tyrosine kinase inhibitor and was recently approved in the treatment of chronic lymphocytic leukaemia. We undertook a systematic review and meta‐analysis of randomised controlled trials to determine the risks
Thura W. Htut +2 more
doaj +1 more source
FRAILTY ASSESSMENT AS PREDICTOR OF BLEEDING FOR PATIENTS TREATED WITH ACALABRUTINIB
Introduction: The American Society of Clinical Oncology (ASCO) promotes the routine use of a comprehensive geriatric assessment, particularly emphasizing frailty, to identify vulnerabilities not detected in the standard clinical evaluation.
TX Carneiro +7 more
doaj +1 more source
Background: Patients with relapsed/refractory (R/R) chronic lymphocytic leukemia (CLL) have limited treatment options. Ceralasertib, a selective ataxia telangiectasia and Rad-3-related protein (ATR) inhibitor, demonstrated synergistic preclinical ...
Wojciech Jurczak +13 more
doaj +1 more source

