alectinib

Ligand id: 7739

Name: alectinib

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View more information in the IUPHAR Pharmacology Education Project: alectinib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 1
Rotatable bonds 3
Topological polar surface area 72.36
Molecular weight 482.27
XLogP 4.08
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
This compound was initially approved in Japan as a treatment for ALK-rearranged non-small cell lung cancer (NSCLC). In the US, the FDA's breakthrough therapy designation was translated to full marketing approval in December 2015, for patients with ALK-positive, metastatic, crizotinib-refractory NSCLC.
Click here to link to the list of alecitinib trials registered with ClinicalTrials.gov.
Mechanism Of Action and Pharmacodynamic Effects
Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers, following gene alterations such as chromosomal translocation, amplification, or point mutation [6-7]. Targeted inhibition of mutated ALK can reduce tumour burden in patients whose tumours carry these specific gene alterations.