Acalabrutinib

Active ingredient description

Acalabrutinib is a small-molecule inhibitor of BTK (Bruton’s tyrosine kinase). Acalabrutinib and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. In nonclinical studies, acalabrutinib inhibited BTK-mediated activation of downstream signaling proteins CD86 and CD69 and inhibited malignant B-cell proliferation and tumor growth in mouse xenograft models.

Medicine classification

This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:

ATC code
Group title
Classification
L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01E Protein kinase inhibitors → L01EL Bruton's tyrosine kinase (BTK) inhibitors
Discover more medicines within L01EL02

Medicines

Acalabrutinib is the active ingredient of these drugs:

Drug
Countries

Australia Austria Brazil Canada Ecuador

Product monographs

Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):

Title
Type
Country
Structured Product Labeling (SPL/PLR)
US

Structural formula

Graphic representation of the active ingredient's molecular structure

Molecular mass: 465.517 g/mol

External identifiers

CAS Substance: 1420477-60-6
DrugBank Drug: DB11703
KEGG Drug: D10893
RxNorm Ingredient: 1986808
SNOMED-CT Concept: 763037006
Acalabrutinib (substance)
UNII Identifier: I42748ELQW
ACALABRUTINIB