acalabrutinib
E888598
Bruton tyrosine kinase inhibitor
protein kinase inhibitor
second-generation BTK inhibitor
small molecule drug
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.
Statements (53)
| Predicate | Object |
|---|---|
| instanceOf |
Bruton tyrosine kinase inhibitor
ⓘ
protein kinase inhibitor ⓘ second-generation BTK inhibitor ⓘ small molecule drug ⓘ |
| approvedBy |
European Medicines Agency
NERFINISHED
ⓘ
U.S. Food and Drug Administration NERFINISHED ⓘ |
| ATCCode | L01EL02 ⓘ |
| bindingSite | Cys481 of BTK NERFINISHED ⓘ |
| bioavailability | oral, moderate ⓘ |
| blackBoxWarning | none ⓘ |
| commonAdverseEffect |
diarrhea
ⓘ
fatigue ⓘ headache ⓘ myalgia ⓘ upper respiratory tract infection ⓘ |
| contraindication | known hypersensitivity to acalabrutinib ⓘ |
| developedBy |
Acerta Pharma
NERFINISHED
ⓘ
AstraZeneca NERFINISHED ⓘ |
| 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 NERFINISHED ⓘ |
| hasCASNumber | 1420477-60-6 ⓘ |
| hasHigherSelectivityThan | ibrutinib ⓘ |
| hasINN | acalabrutinib NERFINISHED ⓘ |
| hasMolecularFormula | C26H23N7O2 ⓘ |
| hasMolecularWeight | 465.51 g/mol ⓘ |
| hasSelectivityFor | BTK over other kinases ⓘ |
| hasTradeName | Calquence NERFINISHED ⓘ |
| hasUSAN | acalabrutinib ⓘ |
| indication |
chronic lymphocytic leukemia
ⓘ
mantle cell lymphoma ⓘ previously untreated chronic lymphocytic leukemia ⓘ relapsed or refractory mantle cell lymphoma ⓘ small lymphocytic lymphoma NERFINISHED ⓘ |
| isSecondGenerationComparedTo | ibrutinib NERFINISHED ⓘ |
| 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 NERFINISHED ⓘ |
Referenced by (1)
Full triples — surface form annotated when it differs from this entity's canonical label.