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].
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2D Structure
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Physico-chemical Properties
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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
SMILES / InChI / InChIKey
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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)
InChI Key LPFWVDIFUFFKJU-UHFFFAOYSA-N
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.
[4]
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