Drug Detail

Information about ENMD-2076

Generic Name
Brand Name (US)
Drug Type
Tyrosine Kinase Inhibitor
Approval Status
Phase 2
Overall Strategy
KIT Protein Based + Oncogenic Signal Path Based
Block KIT + Block related tumor signal paths
Drug Category
KIT/PDGFRA inhibitor+ VEGF inhibitor (TKI)

Although this drug appears to inhibit KIT, there are no indications that it is being developed for GIST. Possible indications include ovarian cancer, multiple myeloma and leukemia.
Notes from the EntreMed website:
ENMD-2076 is a novel orally-active, Aurora A/angiogenic kinase inhibitor with potent activity against Aurora A and multiple tyrosine kinases linked to cancer and inflammatory diseases. ENMD-2076 is relatively selective for the Aurora A isoform in comparison to Aurora B. Aurora kinases are key regulators of the process of mitosis, or cell division, and are often over-expressed in human cancers.

ENMD-2076 exerts its effects through multiple mechanisms of action, including antiproliferative activity and the inhibition of angiogenesis. ENMD-2076 has demonstrated significant, dose-dependent preclinical activity as a single agent, including tumor regression, in multiple xenograft models (e.g. breast, colon, leukemia), as well as activity towards ex vivo-treated human leukemia patient cells.

ENMD-2076 is currently in Phase 1 clinical studies in solid tumors and multiple myeloma. The initiation of additional trials are anticipated, including studies in both solid and hematological malignancies, and the presentation of additional clinical data for ENMD-2076 by mid-2009.