Drug intelligence / Profile preview

alectinib

Development stage
Approved
Lead developer
Chugai Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Alectinib is an orally administered small molecule tyrosine kinase inhibitor used primarily for the treatment of non-small cell lung cancer (NSCLC) that is positive for anaplastic lymphoma kinase (ALK) gene rearrangements. It selectively inhibits the activity of ALK tyrosine kinase, including mutant forms associated with resistance to earlier ALK inhibitors such as crizotinib. By blocking ALK phosphorylation and downstream signaling pathways (including STAT3 and AKT), alectinib reduces tumor cell proliferation and survival. Alectinib also inhibits RET protein but with less potency than ALK. The drug demonstrates good penetration into the central nervous system, making it effective against brain metastases in NSCLC patients. Developed by Chugai Pharmaceutical (a member of the Roche group), alectinib was first approved in Japan in 2014 and subsequently received approvals worldwide for both metastatic and adjuvant settings in ALK-positive NSCLC.

Brand names
Alecensa
Other names
alectinibCH5424802CH-5424802CH 5424802Alecensa
02

Targets

RET (Rearranged during transfection receptor tyrosine kinase)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)

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