Drug intelligence / Profile preview

aldoxorubicin

Development stage
Phase 3
Lead developer
ImmunityBio
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Aldoxorubicin is a tumor-targeting albumin-binding prodrug of the anthracycline antibiotic doxorubicin. It consists of doxorubicin linked via an acid-sensitive hydrazone linker to a maleimide moiety, which allows selective binding to the cysteine-34 position of endogenous serum albumin after intravenous administration. This conjugation enables preferential accumulation in tumors due to the enhanced permeability and retention effect and subsequent release of active doxorubicin in the acidic environment characteristic of tumor tissues or intracellular lysosomes. Aldoxorubicin was developed as a strategy to improve efficacy and reduce cardiotoxicity compared with conventional doxorubicin, allowing higher cumulative doses with less cardiac risk. The drug has been primarily investigated for advanced soft tissue sarcomas (STS), including relapsed or refractory cases, where it demonstrated improved progression-free survival over standard therapies in clinical trials[1][2][3][4][5][8].

Other names
6-maleimidocaproyl hydrazone derivative of doxorubicinaldoxorubicin hydrochloride
02

Targets

TOP2B (DNA topoisomerase II beta)TOP2A (DNA topoisomerase II)

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