Acalabrutinib

Acalabrutinib
Clinical data
Trade namesCalquence
Other namesACP-196
AHFS/Drugs.comMonograph
MedlinePlusa618004
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Identifiers
  • 4-{8-Amino-3-[(2S)-1-(2-butynoyl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl}-N-(2-pyridinyl)benzamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
ECHA InfoCard100.247.121 Edit this at Wikidata
Chemical and physical data
FormulaC26H23N7O2
Molar mass465.517 g·mol−1
3D model (JSmol)
  • CC#CC(=O)N1CCC[C@H]1c2nc(c3n2ccnc3N)c4ccc(cc4)C(=O)Nc5ccccn5
  • InChI=1S/C26H23N7O2/c1-2-6-21(34)32-15-5-7-19(32)25-31-22(23-24(27)29-14-16-33(23)25)17-9-11-18(12-10-17)26(35)30-20-8-3-4-13-28-20/h3-4,8-14,16,19H,5,7,15H2,1H3,(H2,27,29)(H,28,30,35)/t19-/m0/s1
  • Key:WDENQIQQYWYTPO-IBGZPJMESA-N

Acalabrutinib, sold under the brand name Calquence, is a medication used to treat various types of non-Hodgkin lymphoma, including mantle cell lymphoma (MCL) and chronic lymphocytic leukemia/small lymphocytic Lymphoma (CLL/SLL).[7] It may be used both in relapsed as well as in treatment-naive settings.[8]

Common side effects include headaches, feeling tired, low red blood cells, low platelets, and low white blood cells.[7] It is a second generation Bruton's tyrosine kinase inhibitor.[9][10] Acalabrutinib blocks an enzyme called Bruton's tyrosine kinase, which helps B cells to survive and grow.[5] By blocking this enzyme, acalabrutinib is expected to slow down the build-up of cancerous B cells in CLL, thereby delaying progression of the cancer.[5]

Acalabrutinib was approved for medical use in the United States in 2017,[7] and in the European Union in November 2020.[5]

  1. ^ "Acalabrutinib (Calquence) Use During Pregnancy". Drugs.com. 23 October 2019. Retrieved 28 March 2020.
  2. ^ "Calquence". Therapeutic Goods Administration. 13 December 2019. Retrieved 31 August 2024.
  3. ^ "Summary Basis of Decision (SBD) for Calquence". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  4. ^ "Calquence- acalabrutinib capsule, gelatin coated". DailyMed. 22 November 2019. Retrieved 11 November 2020.
  5. ^ a b c d "Calquence EPAR". European Medicines Agency. 20 July 2020. Retrieved 11 November 2020. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. ^ "Calquence Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  7. ^ a b c "Acalabrutinib Monograph for Professionals". Drugs.com. Retrieved 16 March 2019.
  8. ^ "FDA approves new treatment for adults with mantle cell lymphoma". U.S. Food and Drug Administration (FDA) (Press release). 31 October 2017. Retrieved 28 March 2020.
  9. ^ Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, et al. (January 2016). "Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia". The New England Journal of Medicine. 374 (4): 323–332. doi:10.1056/NEJMoa1509981. PMC 4862586. PMID 26641137.
  10. ^ Wu J, Zhang M, Liu D (March 2016). "Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor". Journal of Hematology & Oncology. 9: 21. doi:10.1186/s13045-016-0250-9. PMC 4784459. PMID 26957112.