e-Drug3D

1880

ACALABRUTINIB

INN
ACALABRUTINIB

cas 1420477-60-6

CLASS

ANTINEOPLASTIC
BRUTON TYROSINE KINASE (BTK) INHIBITOR
TREATMENT OF MANTLE CELL LYMPHOMA (MCL)
FORM A COVALENT BOND WITH A CYSTEINE RESIDUE IN THE BTK ACTIVE SITE
ACP-5862 IS THE MAJOR ACTIVE METABOLITE BUT ACTIVITY IS 50 PERCENT LESS POTENT

ROUTE (list)

ORAL

ATC code

L01EL02

PK parameters

F 25 PERCENT
Tmax 0.75 HOUR
VD 34 LITER
Cl 159 LITER / HOUR
PPB 97.5 PERCENT
t1/2 0.9 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER AT PH VALUES ABOVE 6

Target

TARGET BRUTON TYROSINE KINASE (BTK)

DrugCentral

Tyrosine-protein kinase BTK UNIPROT Q06187 BTK

Download SDF file

Benzamide, 4-[8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-

Formula:
C26H23N7O2

Calculated chemical properties:

MW 465.51
NB_atoms 35
XLogP 3.31
PSA 98.57
NB_HD 3
NB_HA 9
fsp3 0.19
Lipinski(0=no;1=yes) 1

FDA
NDA 210259 (label) INN (ACALABRUTINIB) CALQUENCE (ASTRAZENECA) APPROVAL= AP YEAR= 2017
NDA 216387 (label) INN (ACALABRUTINIB MALEATE) CALQUENCE (ASTRAZENECA) APPROVAL= AP YEAR= 2022
NDA 216775 (pdf not found) INN (ACALABRUTINIB) ACALABRUTINIB (ALEMBIC PHARMS LTD) APPROVAL= TA YEAR= 2023
NDA 216833 (pdf not found) INN (ACALABRUTINIB) ACALABRUTINIB (MSN LABORATORIES PRIVATE LTD) APPROVAL= TA YEAR= 2025