Alectinib

Alectinib (INN,), sold under the brand name Alecensa, is an anticancer medication that is used to treat non-small-cell lung cancer (NSCLC). It blocks the activity of anaplastic lymphoma kinase (ALK). It is taken by mouth. It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group.

Alectinib
Clinical data
Pronunciation/əˈlɛktɪnɪb/ ə-LEK-ti-nib
Trade namesAlecensa
Other namesalectinib hydrochloride (JAN JP)
AHFS/Drugs.comMonograph
MedlinePlusa616007
License data
Pregnancy
category
  • AU: D
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability37% (under fed conditions)
Protein binding>99%
MetabolismMainly CYP3A4
MetabolitesM4 (active)
Elimination half-life33 hours (alectinib), 31 hours (M4)
ExcretionFeces (98%)
Identifiers
  • 9-Ethyl-6,6-dimethyl-8-[4-(morpholin-4-yl)piperidin-1-yl]-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
ECHA InfoCard100.256.083
Chemical and physical data
FormulaC30H34N4O2
Molar mass482.628 g·mol−1
3D model (JSmol)
  • CCc1cc2c(cc1N3CCC(CC3)N4CCOCC4)C(c5c(c6ccc(cc6[nH]5)C#N)C2=O)(C)C
  • InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3 COPY
  • Key:KDGFLJKFZUIJMX-UHFFFAOYSA-N
  • Key:GYABBVHSRIHYJR-UHFFFAOYSA-N

The most common side effects include constipation, muscle pain and edema (swelling) including of the ankles and feet, the face, the eyelids and the area around the eyes.

Alectinib was approved for medical use in Japan in 2014, the United States in 2015, Canada in 2016, Australia in 2017, the European Union in 2017, and the United Kingdom in 2021.

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