Drug intelligence / Profile preview

CA-4S2

Development stage
Preclinical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Likely Intravenous
01

Overview

CA-4S2 is a novel hybrid prodrug designed for cancer therapy, specifically advanced hepatocellular carcinoma. It is a **responsive reactive oxygen species (ROS)-augmented prodrug**, meaning it is formulated to be activated in the tumor microenvironment with high ROS, leading to enhanced and selective cytotoxicity to cancer cells while sparing normal tissues. In preclinical models, CA-4S2 incorporated into an engineered scaffold with copper ions (CA-4S2@ES-Cu) demonstrated significantly superior tumor-suppressing efficacy compared to the standard therapy sorafenib, achieving nearly threefold higher antitumor activity. The structure of CA-4S2 is based on a combretastatin A-4 analog, suggesting it interferes with microtubule function, disrupting tumor vasculature and inhibiting cancer cell proliferation[3].

Other names
CA-4S2CA4S2CA 4S2
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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