TY - JOUR
T1 - Acute myeloid leukemia resistant to venetoclax-based therapy
T2 - What does the future hold?
AU - Dhakal, Prajwal
AU - Bates, Melissa
AU - Tomasson, Michael H.
AU - Sutamtewagul, Grerk
AU - Dupuy, Adam
AU - Bhatt, Vijaya Raj
N1 - Publisher Copyright:
© 2022 Elsevier Ltd
PY - 2023/5
Y1 - 2023/5
N2 - Venetoclax is a highly selective B-cell lymphoma-2 (BCL-2) inhibitor, which, combined with a DNA hypomethylating agent or low dose cytarabine, results in high rates of initial responses in patients with acute myeloid leukemia (AML). However, the disease relapses in most patients. Mechanisms of resistance to venetoclax-based therapy include TP53 gene mutations or inactivation of p53 protein, activating kinase mutations such as FLT3 and RAS, and upregulation of other BCL-2 family apoptotic proteins. Current clinical trials are exploring strategies such as doublet or triplet regimens incorporating a p53 activator, an anti-CD47 antibody, or other novel agents that target genes and proteins responsible for resistance to venetoclax. Further studies should focus on identifying predictive biomarkers of response to venetoclax-based therapy and incorporating immunotherapeutic approaches such as checkpoint inhibitors, bispecific antibodies, antibody-drug conjugates, and CAR T-cell therapy to improve outcomes for patients with AML.
AB - Venetoclax is a highly selective B-cell lymphoma-2 (BCL-2) inhibitor, which, combined with a DNA hypomethylating agent or low dose cytarabine, results in high rates of initial responses in patients with acute myeloid leukemia (AML). However, the disease relapses in most patients. Mechanisms of resistance to venetoclax-based therapy include TP53 gene mutations or inactivation of p53 protein, activating kinase mutations such as FLT3 and RAS, and upregulation of other BCL-2 family apoptotic proteins. Current clinical trials are exploring strategies such as doublet or triplet regimens incorporating a p53 activator, an anti-CD47 antibody, or other novel agents that target genes and proteins responsible for resistance to venetoclax. Further studies should focus on identifying predictive biomarkers of response to venetoclax-based therapy and incorporating immunotherapeutic approaches such as checkpoint inhibitors, bispecific antibodies, antibody-drug conjugates, and CAR T-cell therapy to improve outcomes for patients with AML.
KW - Acute myeloid leukemia
KW - Apoptosis
KW - FLT3
KW - Mutations
KW - TP53
KW - Venetoclax, resistance
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U2 - 10.1016/j.blre.2022.101036
DO - 10.1016/j.blre.2022.101036
M3 - Review article
C2 - 36549969
AN - SCOPUS:85144490871
SN - 0268-960X
VL - 59
JO - Blood Reviews
JF - Blood Reviews
M1 - 101036
ER -