Anticancer Agents Based on Cyclopentenones

Background

Current anti-cancer therapeutics suffer from the problems of low cytotoxic activity for cancer cells, specific cytotoxic activity for specific cancer types, drug resistance after some period as, for example, following therapy with cis-platin, and/or lack of ability to prevent cancers addicted to continuous high level protein synthesis.

Technology Overview

Researchers have synthesized 2 chemical compounds that address these therapeutic bottlenecks. The invention relates to 2 novel cyclopentenone derivatives with potent anti-cancer activity. The compounds markedly inhibit the proliferation and induce the killing of cancer cell lines in culture and in animal models. Cells that are resistant to the chemotherapeutic agent cis-platin do not confer cross-resistance to the cyclopentenone derivatives, suggesting that they could provide new therapeutic options in platinum-resistant tumors, addressing a major clinical problem. Another aspect of the invention is the synergetic effects of these compounds with proteasomal inhibitors which may be particularly relevant to the clinical management of ovarian cancer and multiple myeloma where these inhibitors are used. Figure 1. Figure 2.

Stage of Development

The invention is in TRL-4. The technology has been validated in lab with the next steps being:

• Toxicity studies in mouse models
• Phase I clinical studies

Benefits

• Broad spectrum cytotoxic activity against different cancer types Potential for the treatment of platinum- resistant tumors: cis-platin-resistant cancer cells do not display cross-resistance to the new compounds
• Potential for targeting tumors possessing “translation addiction” by inducing ribosomal stress pathways
• Potential enhancement of proteasomal inhibitor therapy due to synergism with bortezomib in tumor cell killing

Applications

Pharmaceutical Companies

Opportunity

This opportunity is in collaboration with the University of Crete, Greece.

Patents

• EP Application