Alecensa

Alectinib

Clinical data
Pronunciation	ə-LEK-ti-nib
Trade names	Alecensa
AHFS/Drugs.com	Multum Consumer Information
Routes of administration	By mouth (capsules)
ATC code	L01XE36 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	37% (under fed conditions)
Protein binding	>99%
Metabolism	CYP3A4
Metabolites	M4 (active)
Biological half-life	33 hours (alectinib), 31 hours (M4)
Excretion	Feces (98%)
Identifiers
IUPAC name 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	1256580-46-7
PubChem CID	49806720
DrugBank	DB11363
ChemSpider	26326738
KEGG	D10542
ChEBI	CHEBI:90936
Chemical and physical data
Formula	C30H34N4O2
Molar mass	482.62 g/mol
3D model (Jmol)	Interactive image
SMILES CCc1cc2c(cc1N3CCC(CC3)N4CCOCC4)C(c5c(c6ccc(cc6[nH]5)C#N)C2=O)(C)C
InChI 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

Alectinib (INN, marketed as Alecensa) is an oral drug that blocks the activity of anaplastic lymphoma kinase (ALK) and is used to treat non-small-cell lung cancer (NSCLC). It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group.

Approved in Japan in July 2014 for the treatment of ALK fusion-gene positive, unresectable, advanced or recurrent non-small cell lung cancer.

Alecensa was approved by the US FDA in December 2015 to treat patients with advanced ALK-positive NSCLC whose disease worsened after, or who could not tolerate, treatment with crizotinib (Xalkori).

In a Japanese trial, after approximately 2 years, 19.6% of patients had achieved a complete response, and the 2-year progression-free survival rate is 76%.

In Feb 2016 the J-ALEX phase III study comparing alectinib with crizotinib was terminated early because an interim analysis showed that progression-free survival was longer with alectinib.