omacetaxine mepesuccinate

Ligand id: 7454

Name: omacetaxine mepesuccinate

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 2
Rotatable bonds 11
Topological polar surface area 123.99
Molecular weight 545.26
XLogP 2.03
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
This drug was designated as an orphan drug for rare diseases by the European Medicines Agency (EMA) in 2004, for treatment of chronic myeloid leukemia (CML). In 2012, the US FDA granted full approval for the same indication, in patients who have shown resistance and/or intolerance to two or more tyrosine kinase inhibitors.
Mechanism Of Action and Pharmacodynamic Effects
Omacetaxine inhibits protein translation. It is hypothesised that the drug binds to the A site of the 60S ribosomal subunit, preventing entry of charged tRNAs, thereby preventing elongation of nascent proteins [2-3]. The cells undergo cell cycle arrest [4] and apoptose [1].
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