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- Overview
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- Abbreviations
Target Overview
Bruton tyrosine kinase (BTK) plays a critical role in the B-cell antigen-receptor signaling pathway, which is responsible for normal B-cell development, function, and survival.1,2
BTK has been implicated in the pathogenesis of B-cell malignancies and has emerged as an important therapeutic target.1,2
Compound Overview
Acalabrutinib is a potent, highly selective inhibitor of BTK.3 Acalabrutinib is currently being evaluated in multiple Phase I, II, and III clinical trials.
Mechanism of Action
Figures adapted from Woyach JA, et al. Blood. 2012;120(6):1175-1184 and Ten Hacken E, et al. Clin Cancer Res. 2014;20(3):548-556.
References
1. Horwood NJ, Urbaniak AM, Danks L. Int Rev Immunol. 2012;31(2):87-103. 2. Akinleye A, Chen Y, Mukhi N, et al. J Hematol Oncol. 2013;6:59. 3. Woyach JA, Johnson AJ, Byrd JC. Blood. 2012;120(6):1175-1184.
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Abbreviations
AIHA
autoimmune hemolytic anemia
ALT
alanine aminotransferase
ANC
absolute neutrophil count
AST
aspartate aminotransferase
AV
acalabrutinib plus venetoclax
BCC
basal cell carcinoma
BCL2
B-cell leukemia/lymphoma 2 protein
BCL6
B-cell lymphoma 6
BCR
B-cell receptor
BID
twice daily
BLNK
B-cell linker
BM
Bone marrow
BR
bendamustine/rituximab
BTK
Bruton tyrosine kinase
BTKi
BTK inhibitor
CD19
cluster of differentiation 19
CD20
cluster of differentiation 20
CD23
cluster of differentiation 23
CD5
cluster of differentiation 5
CIRS
Cumulative Illness Rating Scale
CIRS-G
Cumulative Illness Rating Score-Geriatric
CLL
chronic lymphocytic leukemia
CNS
central nervous system
CR
complete remission
CrCL
creatinine clearance
CYP3A4
Cytochrome P450 3A4
DLBCL
diffuse large B-cell lymphoma
DoR
duration of response
ECOG PS
Eastern Cooperative Oncology Group Performance Score
EFS
event-free survival
EORTC
European Organization for Research and Treatment of Cancer
FCR
fludarabine/cyclophosphamide/rituximab
GI
gastrointestinal
HBsAg
HBV surface antigen
HBV
hepatitis B virus
HCV
hepatitis C virus
HIV
human immunodeficiency virus
IKK
I kappa B kinase
IPI
International Prognostic Index
IRC
independent review committee
ITP
idiopathic thrombocytopenic purpura
IV
intravenous
iwCLL
International Workshop on Chronic Lymphocytic Leukemia
LBCL
large B-cell lymphoma
LDT
lymphocyte doubling time
LYN
Lck/Yes-related novel protein tyrosine kinase
MCL
mantle cell lymphoma
mo
months
MRD
measurable residual disease
MYC
myelocytomatosis viral oncogene
NF-κB
nuclear factor kappa-light-chain-enhancer of activated B cells
NFAT
nuclear factor of activated T cells
NHL
non-Hodgkin lymphoma
non-GCB DLBCL
non-germinal center diffuse large B-cell lymphoma
ORR
overall or objective response rate
OS
overall survival
PB
Peripheral blood
PCR
polymerase chain reaction
PFS
progression-free survival
PKC
protein kinase C
PLC
phospholipase C
PLL
prolymphocytic leukemia
PML
progressive multifocal leukoencephalopathy
PPI
proton-pump inhibitor
PR
partial response
QLC-CLL-17
Quality of Life Questionnaire - Chronic Lymphocytic Leukemia Module-17
QLQ-C30
Quality of life Questionnaire-C30
R
randomization
R-CHOP
rituximab, cyclophosphamide, doxorubicin, vincristine and prednisolone
R/R
relapsed/refractory
SCC
squamous cell carcinoma
SLL
small lymphocytic lymphoma
SYK
spleen tyrosine kinase
TN
treatment-naïve
TP53
tumor suppressor protein 53
TTNT
time to next treatment
ULN
upper limit of normal
uMRD
undetectable measurable residual disease
V
venetoclax
VO
venetoclax/obinutuzumab
Target Overview
Bruton tyrosine kinase (BTK) plays a critical role in the B-cell antigen-receptor signaling pathway, which is responsible for normal B-cell development, function, and survival.1,2
BTK has been implicated in the pathogenesis of B-cell malignancies and has emerged as an important therapeutic target.1,2
Compound Overview
Acalabrutinib is a potent, highly selective inhibitor of BTK.3 Acalabrutinib is currently being evaluated in multiple Phase I, II, and III clinical trials.
Mechanism of Action
Figures adapted from Woyach JA, et al. Blood. 2012;120(6):1175-1184 and Ten Hacken E, et al. Clin Cancer Res. 2014;20(3):548-556.
References
1. Horwood NJ, Urbaniak AM, Danks L. Int Rev Immunol. 2012;31(2):87-103. 2. Akinleye A, Chen Y, Mukhi N, et al. J Hematol Oncol. 2013;6:59. 3. Woyach JA, Johnson AJ, Byrd JC. Blood. 2012;120(6):1175-1184.
Clinical trial information
Select trial for more information
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Selected Filter(s)
Abbreviations
AIHA
autoimmune hemolytic anemia
ALT
alanine aminotransferase
ANC
absolute neutrophil count
AST
aspartate aminotransferase
AV
acalabrutinib plus venetoclax
BCC
basal cell carcinoma
BCL2
B-cell leukemia/lymphoma 2 protein
BCL6
B-cell lymphoma 6
BCR
B-cell receptor
BID
twice daily
BLNK
B-cell linker
BM
Bone marrow
BR
bendamustine/rituximab
BTK
Bruton tyrosine kinase
BTKi
BTK inhibitor
CD19
cluster of differentiation 19
CD20
cluster of differentiation 20
CD23
cluster of differentiation 23
CD5
cluster of differentiation 5
CIRS
Cumulative Illness Rating Scale
CIRS-G
Cumulative Illness Rating Score-Geriatric
CLL
chronic lymphocytic leukemia
CNS
central nervous system
CR
complete remission
CrCL
creatinine clearance
CYP3A4
Cytochrome P450 3A4
DLBCL
diffuse large B-cell lymphoma
DoR
duration of response
ECOG PS
Eastern Cooperative Oncology Group Performance Score
EFS
event-free survival
EORTC
European Organization for Research and Treatment of Cancer
FCR
fludarabine/cyclophosphamide/rituximab
GI
gastrointestinal
HBsAg
HBV surface antigen
HBV
hepatitis B virus
HCV
hepatitis C virus
HIV
human immunodeficiency virus
IKK
I kappa B kinase
IPI
International Prognostic Index
IRC
independent review committee
ITP
idiopathic thrombocytopenic purpura
IV
intravenous
iwCLL
International Workshop on Chronic Lymphocytic Leukemia
LBCL
large B-cell lymphoma
LDT
lymphocyte doubling time
LYN
Lck/Yes-related novel protein tyrosine kinase
MCL
mantle cell lymphoma
mo
months
MRD
measurable residual disease
MYC
myelocytomatosis viral oncogene
NF-κB
nuclear factor kappa-light-chain-enhancer of activated B cells
NFAT
nuclear factor of activated T cells
NHL
non-Hodgkin lymphoma
non-GCB DLBCL
non-germinal center diffuse large B-cell lymphoma
ORR
overall or objective response rate
OS
overall survival
PB
Peripheral blood
PCR
polymerase chain reaction
PFS
progression-free survival
PKC
protein kinase C
PLC
phospholipase C
PLL
prolymphocytic leukemia
PML
progressive multifocal leukoencephalopathy
PPI
proton-pump inhibitor
PR
partial response
QLC-CLL-17
Quality of Life Questionnaire - Chronic Lymphocytic Leukemia Module-17
QLQ-C30
Quality of life Questionnaire-C30
R
randomization
R-CHOP
rituximab, cyclophosphamide, doxorubicin, vincristine and prednisolone
R/R
relapsed/refractory
SCC
squamous cell carcinoma
SLL
small lymphocytic lymphoma
SYK
spleen tyrosine kinase
TN
treatment-naïve
TP53
tumor suppressor protein 53
TTNT
time to next treatment
ULN
upper limit of normal
uMRD
undetectable measurable residual disease
V
venetoclax
VO
venetoclax/obinutuzumab