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gonadotropin-releasing hormone III + daunorubicin
- Development stage
- Preclinical
- Lead developer
- Eötvös Loránd University
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
- Administration
- Intravenous
01
Overview
Gonadotropin-releasing hormone III + daunorubicin is a peptide-drug conjugate (PDC) designed for targeted cancer therapy. It utilizes a native isoform of human gonadotropin-releasing hormone isolated from sea lamprey (GnRH-III) as a targeting moiety. This peptide specifically binds to gonadotropin-releasing hormone receptors (GnRH-R) that are overexpressed on various cancer cells, including those of breast, ovarian, endometrial, prostate, and colorectal cancers. The cytotoxic payload, daunorubicin (an anthracycline), is covalently attached to the peptide vector, typically via an oxime bond at the Lys8 position. This linkage ensures stability in circulation while allowing for the release of the drug upon internalization into the tumor cell. The conjugate aims to deliver high local concentrations of chemotherapy directly to malignant tissues, thereby increasing efficacy and reducing systemic side effects compared to free daunorubicin.
- Other names
- GnRH-III-daunorubicin[Dau=Aoa8]-GnRH-IIIGnRH-III-oxime-daunorubicin
02
Targets
TOP2A (DNA topoisomerase II)GnRHR (Gonadotropin-releasing hormone receptor)DNA
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