olmutinib

Ligand id: 9196

Name: olmutinib

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 110.86
Molecular weight 486.18
XLogP 4.56
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Olmutinib has been approved in South Korea (May 2016) [2] for the treatment of patients with locally advanced or metastatic EGFR T790M mutation-positive non-small cell lung cancer (NSCLC), who had been previously treated with an EGFR tyrosine kinase inhibitor (based on results from trial NCT01588145 [6]). Additional Phase 2 clinical trials in T790M-positive non-small cell lung cancer are ongoing- see NCT02485652 [5] and NCT02444819 for example. Olmutinib has been granted breakthrough therapy designation in NSCLC by the US FDA (December 2015). In Sept 2016 Boehringer Ingelheim announced that olmutinib develpment would be returned to Hanmi but it's unclear if this will affect US approval.
Mechanism Of Action and Pharmacodynamic Effects
Olmutinib inhibits T790M mutant EGFR and EGFR activating mutants whilst sparing wild-type receptor activity, thereby showing selectivity towards cancer cells harbouring these receptor tyrosine kinase mutations.