Drug intelligence / Profile preview

Pt-Mal-LHRH

Development stage
Preclinical
Lead developer
Eastern Kentucky University
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intraperitoneal
01

Overview

Pt-Mal-LHRH is a novel targeted platinum-based chemotherapeutic conjugate developed by researchers at Eastern Kentucky University. It is designed to selectively target reproductive cancer cells, such as triple-negative breast cancer (TNBC) and ovarian cancer, that overexpress the luteinizing hormone-releasing hormone (LHRH) receptor (also known as the gonadotropin-releasing hormone receptor, GnRHR). The compound is synthesized by linking activated cisplatin to the LHRH peptide via a malonate linker, which chelates platinum in a manner similar to carboplatin. By binding to the LHRH receptor, Pt-Mal-LHRH facilitates receptor-mediated endocytosis, leading to significantly increased intracellular platinum accumulation, enhanced cytotoxicity, and reduced systemic side effects compared to conventional untargeted platinum drugs like carboplatin and cisplatin.

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)DNA

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