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arylboronate doxorubicin prodrug

Development stage
Preclinical
Modality
Small Molecules
Administration
Intratumoral
01

Overview

Arylboronate doxorubicin prodrugs are a class of reactive oxygen species (ROS)-responsive therapeutic agents designed to improve the tumor selectivity of the anthracycline antibiotic doxorubicin. These prodrugs consist of doxorubicin conjugated to an arylboronate moiety, which serves as a trigger. In the presence of elevated ROS levels (such as hydrogen peroxide) typically found in the tumor microenvironment, the arylboronate group undergoes oxidative cleavage and subsequent self-immolative degradation, releasing the active doxorubicin. This mechanism aims to concentrate the cytotoxic effect within malignant tissues while sparing healthy cells from systemic toxicity. Preclinical research, including studies on MiaPaCa-2 pancreatic cancer models, has demonstrated the feasibility of this approach for inducing tumor regression and achieving intratumoral drug concentrations comparable to direct injection.

Other names
arylboronate-based ROS-responsive prodrug of doxorubicinbenzeneboronate doxorubicin prodrugROS-responsive doxorubicin prodrug
02

Targets

DNATOP2A (DNA topoisomerase II)TOP2B (DNA topoisomerase II beta)

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