Drug intelligence / Profile preview

Tat-ELP-DOXO

Development stage
Unknown
Lead developer
University of Mississippi Medical Center
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Tat-ELP-DOXO is a research-stage biopolymer-drug conjugate consisting of three components: the HIV Tat cell-penetrating peptide (CPP), which facilitates intracellular delivery by promoting uptake across cell membranes; an Elastin-like polypeptide (ELP), a thermally responsive biopolymer derived from mammalian elastin that passively accumulates in solid tumors and aggregates under hyperthermic conditions; and doxorubicin (DOXO), conjugated via an acid-sensitive (6-maleimidocaproyl)hydrazone linker to a terminal cysteine on the ELP. The active chemotherapeutic payload is doxorubicin, which intercalates into DNA and inhibits topoisomerase II. Tat-ELP-DOXO is designed to improve tumor-targeted delivery of doxorubicin using mild hyperthermia, thereby reducing systemic toxicity. It has been studied in preclinical models of breast cancer.

Other names
Tat-ELP-doxorubicin
02

Targets

TOP2A (DNA topoisomerase II)DNA

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