acalabrutinib

E888598

Acalabrutinib is a second-generation, highly selective Bruton tyrosine kinase inhibitor used primarily in the treatment of certain B-cell malignancies such as mantle cell lymphoma and chronic lymphocytic leukemia.

All labels observed (1)

Label Occurrences
acalabrutinib canonical 3

How this entity was disambiguated

Statements (53)

Predicate Object
instanceOf Bruton tyrosine kinase inhibitor ⓘ
protein kinase inhibitor ⓘ
second-generation BTK inhibitor ⓘ
small molecule drug ⓘ
approvedBy European Medicines Agency ⓘ
U.S. Food and Drug Administration ⓘ
ATCCode L01EL02 ⓘ
bindingSite Cys481 of BTK ⓘ
linked to: BTK
bioavailability oral, moderate ⓘ
blackBoxWarning none ⓘ
commonAdverseEffect diarrhea ⓘ
fatigue ⓘ
headache ⓘ
myalgia ⓘ
upper respiratory tract infection ⓘ
contraindication known hypersensitivity to acalabrutinib ⓘ
developedBy Acerta Pharma ⓘ
AstraZeneca ⓘ
dosageForm oral capsule ⓘ
oral tablet ⓘ
drugInteraction strong CYP3A inducers ⓘ
strong CYP3A inhibitors ⓘ
eliminationHalfLife approximately 1 hour ⓘ
FDAApprovalDate 2017-10-31 ⓘ
FDADesignation orphan drug for mantle cell lymphoma ⓘ
hasActiveMetabolite ACP-5862 ⓘ
hasCASNumber 1420477-60-6 ⓘ
hasHigherSelectivityThan ibrutinib ⓘ
hasINN acalabrutinib ⓘ
hasMolecularFormula C26H23N7O2 ⓘ
hasMolecularWeight 465.51 g/mol ⓘ
hasSelectivityFor BTK over other kinases ⓘ
hasTradeName Calquence ⓘ
linked to: Imbruvica
hasUSAN acalabrutinib ⓘ
indication chronic lymphocytic leukemia ⓘ
mantle cell lymphoma ⓘ
previously untreated chronic lymphocytic leukemia ⓘ
relapsed or refractory mantle cell lymphoma ⓘ
small lymphocytic lymphoma ⓘ
isSecondGenerationComparedTo ibrutinib ⓘ
linked to: Imbruvica
legalStatusInEuropeanUnion prescription only ⓘ
legalStatusInUnitedStates prescription only ⓘ
mechanismOfAction irreversible covalent inhibition of Bruton tyrosine kinase ⓘ
metabolism hepatic ⓘ
pregnancyCategory may cause fetal harm (based on mechanism and animal data) ⓘ
primaryMetabolizingEnzyme CYP3A4 ⓘ
proteinBinding high ⓘ
routeOfAdministration oral ⓘ
seriousAdverseEffect atrial fibrillation ⓘ
cytopenias ⓘ
hemorrhage ⓘ
infections ⓘ
targets Bruton tyrosine kinase ⓘ

How these facts were elicited

Referenced by (3)

Full triples — surface form annotated when it differs from this entity's canonical label.

BTK → inhibitedBy → acalabrutinib ⓘ
acalabrutinib → hasINN → acalabrutinib ⓘ