Drug intelligence / Profile preview

D-F07

Development stage
Preclinical
Lead developer
The Wistar Institute
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

D-F07 is a tricyclic chromenone-based small molecule inhibitor of the Inositol-Requiring Enzyme 1 (IRE-1) RNase activity. It is designed as a prodrug containing a 1,3-dioxane aldehyde-masking group to improve stability and cellular uptake. By inhibiting IRE-1, D-F07 prevents the unconventional splicing of XBP-1 mRNA into its active form, XBP-1s, a transcription factor essential for the survival and proliferation of B-cell malignancies such as multiple myeloma, chronic lymphocytic leukemia, and mantle cell lymphoma. Research indicates that D-F07 can be combined with PI3K/AKT pathway inhibitors to enhance cytotoxicity and has been further modified with reactive oxygen species (ROS)-sensitive groups for tumor-targeted delivery.

02

Targets

ERN1 (Inositol-requiring enzyme 1 alpha)

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