Derivatives of the small molecule anticancer drug, AMPI-109


Triple-negative breast cancer (TNBC) does not express the estrogen, progesterone or HER2 receptors and accounts for 10-20% of all breast cancer cases. TNBC lacks exploitable targets and tends to be higher grade than other breast cancers, making it difficult to develop effective treatments. PRL-3 is an oncogenic phosphatase that is overexpressed in many types of cancer. In particular, PRL-3 is overexpressed in greater than 50% of basal breast cancers and associated with poor survival in breast cancer patients. Dr. Jim Lambert has characterized an orally available small molecule, VDX-111, which targets PRL-3. Inhibition of PRL-3 using VDX-111 yields antiproliferative and apoptotic effects in multiple TNBC lines. Additionally, xenograft models show reduction in TNBC tumor volumes. VDX-111 shows great promise as potent therapeutic for TNBC and is currently being optimized.

For Information, Contact:
Jeff Walenta
University of Colorado
James Lambert
Michael Wempe
M. Scott Lucia
Rahul Ray
Disease Areas:
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