Chemical formula: C₂₆H₂₃N₇O₂ Molecular mass: 465.517 g/mol PubChem compound: 71226662
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.
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 |
|---|---|---|
| L01EL02 | L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01E Protein kinase inhibitors → L01EL Bruton's tyrosine kinase (BTK) inhibitors | |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
| Title | Information Source | Document Type | |
|---|---|---|---|
| CALQUENCE Capsule | FDA, National Drug Code (US) | MPI, US: SPL/PLR | |
| CALQUENCE Hard capsule | European Medicines Agency (EU) | MPI, EU: SmPC | |
| CALQUENCE Film-coated tablet | European Medicines Agency (EU) | MPI, EU: SmPC |
Acalabrutinib is an active ingredient of these brands:
United States (US)Australia (AU)Austria (AT)Brazil (BR)Canada (CA)Croatia (HR)Ecuador (EC)Estonia (EE)Finland (FI)France (FR)Hong Kong (HK)Ireland (IE)Israel (IL)Japan (JP)Lithuania (LT)Netherlands (NL)New Zealand (NZ)Poland (PL)Romania (RO)Singapore (SG)South Africa (ZA)Spain (ES)Turkey (TR)United Kingdom (UK)Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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