brigatinib

Ligand id: 7741

Name: brigatinib

IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: brigatinib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 2
Rotatable bonds 8
Topological polar surface area 92.43
Molecular weight 528.22
XLogP 4.72
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Brigatinib (AP26113) received Breakthrough Therapy designation from the U.S. FDA for the treatment of patients with ALK-rearranged metastatic NSCLC whose tumours are resistant to crizotinib. This was converted via accelerated approval for these patients in April 2017. Phase 3 trial NCT02737501 compared brigatinib and crizotinib 'head-to-head'. Click here to view the list of all AP26113 trials currently registered with ClinicalTrials.gov.
Mechanism Of Action and Pharmacodynamic Effects
ALK was first identified as a chromosomal rearrangement in anaplastic large-cell lymphoma (ALCL), and has since been shown to be a driver of some non-small cell lung cancers (NSCLCs) and neuroblastomas, in addition to ALCL. ALK is not normally expressed in normal adult tissues, making it a promising molecular target for oncology.