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SNU-2535

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Histamine H1 receptor

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Bacterial penicillin-binding protein

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ALECTINIB

LIJ4CT1Z3Y

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Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

ALK tyrosine kinase receptor

Conditions:

Anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group. Alectinib is spe...

cifically used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Inhibition of ALK prevents phosphorylation and subsequent downstream activation of STAT3 and AKT resulting in reduced tumour cell viability. Approved under accelerated approval in 2015, alectinib is indicated for use in patients who have progressed on or were not tolerant of crizotinib, which is associated with the development of resistance. Alectinib is marketed as Alecensa.

Alectinib Hydrochloride

P9YY73LO6J

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Status:

US Approved Rx (2015)

First approved in 2015

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

ALK tyrosine kinase receptor

Conditions:

Anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group. Alectinib is spe...

cifically used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Inhibition of ALK prevents phosphorylation and subsequent downstream activation of STAT3 and AKT resulting in reduced tumour cell viability. Approved under accelerated approval in 2015, alectinib is indicated for use in patients who have progressed on or were not tolerant of crizotinib, which is associated with the development of resistance. Alectinib is marketed as Alecensa.

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