Drug intelligence / Profile preview

DP-3975

Development stage
Preclinical
Lead developer
Deciphera Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

DP-3975 is a small-molecule inhibitor of the AXL receptor tyrosine kinase (RTK), originally developed by Deciphera Pharmaceuticals. It functions by binding to the AXL kinase domain, thereby inhibiting its phosphorylation and subsequent activation of downstream signaling cascades, including the PI3K/AKT/mTOR and RAF/MAPK pathways. These pathways are critical for tumor cell survival, epithelial-to-mesenchymal transition (EMT), and resistance to chemotherapy. DP-3975 has been extensively studied in preclinical models of mesothelioma and head and neck squamous cell carcinoma (HNSCC), where it has demonstrated efficacy in reducing cell proliferation, migration, and the maintenance of cancer stem cell phenotypes. While it served as a significant lead compound in AXL research, it does not appear to have progressed into formal clinical trials under this designation.

02

Targets

AXL (AXL receptor tyrosine kinase)

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