Poziotinib

Poziotinib is an investigational drug not approved by the FDA.

Poziotinib is an investigational, orally administered, irreversible tyrosine kinase inhibitor targeting EGFR and HER2 with exon 20 insertion mutations.

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Poziotinib is designed to be small and flexible. EGFR and HER2 are part of a larger family of receptors. The epidermal growth factor receptor (EGFR) family of proteins comprise the structurally related receptors EGFR, HER2, HER3, and HER4. Members with kinase domains, like EGFR, are activated upon ligand binding and dimerization - either with another EGFR, or with other members such as HER2.

Poziotinib is an investigational drug not approved by the FDA.

A variety of mutations in EGFR result in their constant activation, and are associated with certain cancers. Among the known activating mutations in EGFR and HER2, <br />exon 20 insertions add additional amino acids to the protein sequence causing a conformational change, heavily restricting access to the drug binding pocket of the kinase active site. Preclinical studies suggest that poziotinib can access the restricted binding pocket caused by these exon 20 insertion mutations and may help inhibit its kinase activity.

In pre-clinical models of cancer, poziotinib was shown to inhibit kinase activity of EGFR and HER2 with exon 20 insertion mutations, inhibiting proliferation, leading to cancer cell death.

More About Poziotinib

Development Indications

Non Small Cell Lung Cancer
SPI-POZ-202 (Phase 2): EGFR and HER2 Exon 20 Insertion Mutations Locally Advanced or Metastatic NSCLC

Breast Cancer
SPI-POZ-201 (Phase 2): HER2+ Metastatic Breast Cancer
SPI-POZ-101 (Phase 1b) Combination With T-DM1 in HER2+ Breast Cancer

Latest News on Poziotinib

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