New antimitotic Rhizoxin derivatives

Challenge
Cancer diseases are the second frequent causes of death in Europe and the USA. From a total of 58 million deaths worldwide in 2005, cancer accounts for 7.6 million (or 13%) of all deaths according to the World Health Organisation (WHO). Due to the significant adverse effects of the common used anti-cancer drugs there is an ongoing demand for new efficient substances with minor adverse effects. 

Technology
This invention discloses four new Rhizoxin derivatives isolated from the newly discovered endosymbiotic bacteria species Burkholderia rhizoxina. These substances, which are belonging to the class of macrocyclic polyketides are characterized by strong antiproliferative, cytotoxic and antifungal effects The polyketide Rhizoxin binds very efficiently to ß-tubulin and inhibits the polymerisation of the tubulin molecules, which is a prerequisite for the forming of the mitotic apparatus and the cell division. Due to its mitostatic effects Rhizoxin was already used in clinical studies as therapeutic agent against cancer. Rhizoxin itself is not efficient enough as treatment against cancer but the new isolated derivatives are showing distinct higher effects and are therefore quite promising new candidates.

Commercial Opportunity
In-licensing or cooperation for further development of a pharmaceutical or diagnostic composition.

Developmental Status
Analysis conducted in monolayer assays of several different cancer cell lines, including resistant cancer cell lines.

Patent Situation
Priority filed in 2005. European Patent granted (EP1940848), US, JP, CA, AU applications pending. 

Further Reading

Scherlach et al. 2006. Antimitotic Rhizoxin Derivatives from a Cultured Bacterial Endosymbiont of the Rice Pathogenic Fungus Rhizopus microsporus. J. Am. Chem. Soc. 2006, 128, 11529-11536

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Kontakt:

Sabina Heim, Ph.D.
Technology Manager
Ascenion GmbH

T: +49 (0)531-6181-2090
F: +49 (0)531-6181-2098
heim(at)ascenion.de