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GnRH-III[4Lys(Dau=Aoa),8Lys(Dau=Aoa)]
- Development stage
- Preclinical
- Lead developer
- Eötvös Loránd University
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
GnRH-III[4Lys(Dau=Aoa),8Lys(Dau=Aoa)] is a research-stage peptide-drug conjugate (PDC) designed for targeted cancer therapy. It utilizes a modified version of the sea lamprey gonadotropin-releasing hormone-III (GnRH-III) as a targeting vector to deliver the anthracycline antibiotic daunorubicin specifically to cancer cells overexpressing GnRH receptors (GnRH-R). The conjugate features two daunorubicin molecules attached via oxime linkages (using aminooxyacetyl, Aoa, linkers) to lysine residues substituted at positions 4 and 8 of the peptide backbone. This dual-payload design is intended to increase cytotoxic potency compared to mono-substituted GnRH-III conjugates. Preclinical studies have demonstrated significant antitumor and antimetastatic activity in various models, including colorectal, breast, and melanoma cancers, with reduced systemic toxicity compared to free daunorubicin. The compound is primarily studied in academic settings, notably by research groups at Eötvös Loránd University.
- Other names
- GnRH-III(Dau-Aoa)2GnRH-III-bis-daunorubicin conjugateGnRH-III[4Lys(Dau=Aoa),8Lys(Dau=Aoa)] bioconjugate
02
Targets
TOP2A (DNA topoisomerase II)GnRHR (Gonadotropin-releasing hormone receptor)DNA
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