poziotinib   Click here for help

GtoPdb Ligand ID: 7903

Synonyms: HM781-36B | NOV120101
Compound class: Synthetic organic
Comment: Poziotinib is an orally bioavailable, clinically active, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with antineoplastic activity [1-2]. It is a potent inhibitor of the most common EGFR and HER2 exon 20 insertion mutants that are predominantly activating in nature, and resistant to exisitng reversible and irreversible EGFR tyrosine kinase inhibitors [3-4].
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 7
Topological polar surface area 76.58
Molecular weight 490.1
XLogP 4.47
No. Lipinski's rules broken 0
Click here for help
Canonical SMILES C=CC(=O)N1CCC(CC1)Oc1cc2c(ncnc2cc1OC)Nc1ccc(c(c1F)Cl)Cl
Isomeric SMILES C=CC(=O)N1CCC(CC1)Oc1cc2c(ncnc2cc1OC)Nc1ccc(c(c1F)Cl)Cl
InChI InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29)
No information available.
Summary of Clinical Use Click here for help
Poziotinib has advanced to Phase 2 clinical trial either alone or in combination for several types of advanced solid malignancies. Click here to link to ClinicalTrials.gov's full list of poziotinib trials.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03066206 Poziotinib in EGFR Exon 20 Mutant Advanced NSCLC Phase 2 Interventional M.D. Anderson Cancer Center Preliminary results from a small cohort of 11 patients with NSCLC and EGFR exon 20 insertion mutations, indicated a response rate of 64%. This appears impressive, but it's important to note this trial is not yet complete, and median PFS and OS have yet to be reported. 3