Rhenium-Based Complexes and in Vivo Testing: A Brief History

Area of Science:

• Medicinal Chemistry
• Oncology
• Inorganic Chemistry

Background:

• Metal-based anticancer drugs, exemplified by cisplatin, are established cancer treatments.
• Despite their efficacy, challenges like toxicity and resistance necessitate exploring new metal-based therapeutics.
• Current research includes gold (auranofin) and ruthenium (NAMI-A, NKP-1339, TLD-1433) drug candidates in clinical trials.

Purpose of the Study:

• To chronologically review rhenium-based drug candidates that have progressed to in vivo testing.
• To assess the current status and future outlook for rhenium-based anticancer agents.

Main Methods:

• Literature review focusing on rhenium complexes with reported in vivo antitumour activity.
• Chronological documentation of rhenium-based drug candidates undergoing in vivo evaluation.
• Analysis of preclinical data and progression towards clinical trials.

Main Results:

• Rhenium complexes have shown promise in extensive in vitro studies.
• Only nine rhenium-based complexes have demonstrated in vivo antitumour activity to date.
• Further in vivo validation is a critical prerequisite for clinical trial progression.

Conclusions:

• Rhenium-based compounds represent a developing area in metal-based anticancer drug discovery.
• The transition from in vitro to in vivo efficacy is a key hurdle for these agents.
• Continued research into rhenium complexes could yield novel anticancer therapeutics.