Template:Second-generation BTKi table: Difference between revisions

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|+ '''Novel BTK Inhibitors for CCL Treatment'''
|+ '''Second-generation Bruton’s Tyrosine Kinase Inhibitors (BTKi) for CCL Treatment'''
|-
|-bgcolor="CEDFF2"
! width=120px|BTK inhibitor
! width=110px|BTK inhibitor
! width=120px|BTK binding mechanism
! width=150px|BTK binding mechanism
! width=120px|Selectivity for BTK
! width=80px|Selectivity for BTK
! width=200px|Relevant non-BTK targets
! width=320px|Relevant non-BTK targets
! width=120px|Phase of clinical development
! width=90px|Clinical Phase
|-
|-
| Acalabrutinib  
| Acalabrutinib  
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| N/A
| N/A
| II/III
| II/III
|-
|-bgcolor="F5FAFF"
| Zanubrutinib  
| Zanubrutinib  
| Covalent, irreversible  
| Covalent, irreversible  
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| N/A
| N/A
| I/II
| I/II
|-
|-bgcolor="F5FAFF"
| Vecabrutinib
| Vecabrutinib
| Non-covalent, reversible
| Non-covalent, reversible
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| N/A
| N/A
| I  
| I  
|-
|-bgcolor="F5FAFF"
| ARQ-531
| ARQ-531
| Non-covalent, reversible
| Non-covalent, reversible
| Low   
| Low   
| Lck/Yes novel tyrosine kinase (LYN), mitogen-activated protein kinase kinase 1 (MEK1)
| Lck/Yes novel tyrosine kinase (LYN),<br>mitogen-activated protein kinase kinase 1 (MEK1)
| I
| I
|-
|-
| colspan=5|Table data {{#pmid:31028669|PMID31028669}}
| colspan=5|Table data {{#pmid:31028669|PMID31028669}}
|}
|}

Latest revision as of 14:11, 30 April 2019

Second-generation Bruton’s Tyrosine Kinase Inhibitors (BTKi) for CCL Treatment
BTK inhibitor BTK binding mechanism Selectivity for BTK Relevant non-BTK targets Clinical Phase
Acalabrutinib Covalent, irreversible High N/A II/III
Zanubrutinib Covalent, irreversible Moderate N/A II/III
Tirabrutinib Covalent, irreversible High N/A I/II
Vecabrutinib Non-covalent, reversible Moderate interleukin-2-inducible (ITK) I/II
LOXO-305 Non-covalent, reversible High N/A I
ARQ-531 Non-covalent, reversible Low Lck/Yes novel tyrosine kinase (LYN),
mitogen-activated protein kinase kinase 1 (MEK1)
I
Table data [1]
  1. Bond DA & Woyach JA. (2019). Targeting BTK in CLL: Beyond Ibrutinib. Curr Hematol Malig Rep , , . PMID: 31028669 DOI.