Alectinib

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Alectinib
Alectinib skeletal.svg
Systematic (IUPAC) name
9-Ethyl-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile
Clinical data
Trade names Alecensa
AHFS/Drugs.com Multum Consumer Information
Legal status
Identifiers
CAS Number 1256580-46-7
ATC code none
PubChem CID: 49806720
DrugBank DB11363
ChemSpider 26326738
KEGG D10542
ChEBI CHEBI:90936
Chemical data
Formula C30H34N4O2
Molecular mass 482.62 g/mol
  • 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

Alectinib (marketed as Alecensa) is an oral drug that blocks the activity of anaplastic lymphoma kinase (ALK)[1][1][2] 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.

Approvals and indications

Approved in Japan in July 2014[3] for the treatment of ALK fusion-gene positive, unresectable, advanced or recurrent non-small cell lung cancer.[2]

Alecensa was approved by the US FDA in December 2015 to treat patients with advanced ALK-positive NSCLC[clarification needed] whose disease worsened after, or who could not tolerate, treatment with crizotinib (Xalkori).[1]

Clinical trials

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%.[2]

In Feb 2016 the J-ALEX phase III study comparing alectinib with crizotinib was terminated early because an interim anaysis showed that progression-free survival was longer with alectinib.[4]

References

  1. ↑ 1.0 1.1 1.2 New Oral Therapy To Treat ALK-Positive Lung Cancer. Dec 2015
  2. ↑ 2.0 2.1 2.2 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Japan becomes first country to approve Roche’s alectinib for people with a specific form of advanced lung cancer
  4. ↑ Chugai’s ALK Inhibitor “Alecensa®” Trial Stopped Early for Benefit. Feb 2016

External links


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