Poziotinib

Last updated
Poziotinib
Poziotinib.png
Legal status
Legal status
  • experimental
Identifiers
  • 1-[4-[4-(3,4-dichloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]prop-2-en-1-one
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
Formula C23H21Cl2FN4O3
Molar mass 491.34 g·mol−1
3D model (JSmol)
  • COC1=C(C=C2C(=C1)N=CN=C2NC3=C(C(=C(C=C3)Cl)Cl)F)OC4CCN(CC4)C(=O)C=C
  • 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)
  • Key:LPFWVDIFUFFKJU-UHFFFAOYSA-N

Poziotinib (NOV120101, HM781-36B) [1] is a drug in development by Hanmi Pharmaceutical (in South Korea), Luye Pharma (China), and Spectrum Pharmaceuticals (rest of world) for various cancers. [2]

It is built on an anilino-quinazoline scaffold and inhibits the epidermal growth factor receptors EGFR, HER2/neu, and Her 4 [3] and binds covalently to its targets. [4]

It was discovered at Hanmi; in August 2014 Hanmi exclusively licensed rights in China to the Chinese company Luye Pharma and in February 2015 Hanmi licensed rights in the rest of the world outside of South Korea to Spectrum. [2]

As of 2016 Spectrum had started a Phase II trial of poziotinib a second-line treatment for breast cancer. [2]

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References

  1. "Poziotinib". AdisInsight. Retrieved 25 March 2017.
  2. 1 2 3 Kim M (4 July 2016). "Hanmi Pharmaceutical to Step Up R&D Investment to Further Develop Core Technologies". BusinessKorea.
  3. Roskoski R (September 2014). "ErbB/HER protein-tyrosine kinases: Structures and small molecule inhibitors". Pharmacological Research. 87: 42–59. doi:10.1016/j.phrs.2014.06.001. PMID   24928736.
  4. "Poziotinib". NCI Drug Dictionary. National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services. Retrieved 25 March 2017.