Drug intelligence / Profile preview

DK049

Development stage
Preclinical
Lead developer
LadRx
Modality
Small Molecules
Administration
Intravenous
01

Overview

DK049 is an albumin-binding prodrug conjugate developed by CytRx using its proprietary LADR (Linker-Activated Drug Release) technology, designed for oncology applications. It features a two-stage linker that leverages pH sensitivity and enzymatic activation to control the release of its **gemcitabine** cytotoxic payload selectively at tumor sites, enabling prolonged tumor exposure while minimizing release in healthy tissues. Preclinical data from human tumor xenograft models demonstrated superior efficacy in **pancreatic cancer**, **non-small cell lung cancer**, and **ovarian cancer**, with tumors shrinking significantly (e.g., 13-fold smaller in ovarian models using 85% less drug than comparators) at non-toxic doses, and potential to evade drug resistance mechanisms.[1][3][12]

02

Targets

DNA

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