Rhenium compounds as anticancer agents
Summary of technology
Metal-based anticancer agents, such as cisplatin, are used as gold standard cancer therapies. While these drugs are effective in eradicating malignant cells, their selectivity is poor, meaning that significant adverse effects are experienced during treatment through damage inflicted on healthy cells. Improved selectivity and targeted cancer therapies with minimal side effects are being sought. Many drugs have been developed which contain platinum, and other metals are now being developed as anticancer agents.
Researchers at Curtin University developed a series of rhenium containing compounds that target cancerous cells and block their growth. These compounds are promising candidates for treatment of tumours with aggressive potential for metastasis (for example, pancreatic cancer).
A library of molecular candidates have been synthesized, and structure-activity relationship to modulate selectivity and therapeutic potential has been explored.
The rhenium compounds offer the following advantages:
- low toxicity demonstrated
- flexible molecules enhance therapeutic potential
- linking to cancer targeting agents to improve selectivity
- simple synthesis for cost effective production.
Associate Professor Max Massi and Dr Peter Simspon from the Department of Chemistry are synthetic chemists with expertise in the synthesis of metal-based compounds. They are supported by Professor Marco Falasca from the School of Biomedical Sciences, who has deep experience in cancer biology and therapeutics development.
Stage of development
Screening against cancer cell lines including pancreatic cancer, ovarian cancer and neuroblastoma has been completed. The data indicate an anticancer activity at a similar level compared to cisplatin.
Toxicity profile of the compounds in vivo was established in a zebrafish model, indicating less systemic toxicity compared to cisplatin.
Planned testing in industry standard animal models will commence in 2017.
Curtin is seeking drug development partners for this project. The ideal partner is capable of completing preclinical testing in conjunction with Curtin and taking a lead candidate into clinical testing.