Drug intelligence / Profile preview

rhodium (II) citrate

Development stage
Preclinical
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Intratumoral, Intravenous (investigational/preclinical)
01

Overview

Rhodium (II) citrate is a **metal-based anticancer agent** that belongs to the class of rhodium (II) carboxylates and has demonstrated cytotoxic and antitumor activity in vitro and in vivo, particularly against breast cancer cell lines. Its **mechanism of action** involves intercalation into DNA, impairing transcription and replication, and inducing apoptosis primarily through increased reactive oxygen species (ROS) production, as well as mitochondrial cytochrome C release and activation of intrinsic apoptotic pathways. The drug shows enhanced antitumor efficacy when formulated with nanocarriers such as maghemite (γ-Fe2O3) nanoparticles, allowing for better tumor targeting, reduced systemic toxicity, and improved therapeutic index. Intratumoral administration in preclinical models led to substantial tumor growth inhibition, reduced cell proliferation and microvascularization (as indicated by decreased Ki-67 and CD31 staining), and increased necrosis and fibrosis in tumor tissue. Rhodium (II) citrate is not an approved pharmaceutical and remains investigational, with a primary indication for breast cancer and general antitumor activity, including activity in cisplatin-resistant models[1][2][4][5].

Other names
dirhodium citrate
02

Targets

DNA

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