Stabilized Etnangien derivative – antibiotic drug candidate from myxobacteria
Reference Number TO 02-00236
Challenge
Today, antibiotics are more than ever in the focus of scientists. In light of an increasing antibiotic resistance of bacteria there is an unquestioned need for new antibiotics with novel active principles. Natural compounds are often used in drug development followed by chemical derivatisation to optimise its pharmacodynamic, pharmacokinetic and importantly safety characteristics.
Since myxobacteria are demonstrably a rich and successful source for natural compounds, several of these molecules are considered as potential drug candidates facing manifold indications including infection. A very prominent example for successful drug development in this context is epothilone, (isolated at the former GBF now HZI, Helmholtz Centre for Infection Research), that was recently brought to the market by BMS for treatment of breast cancer.
Technology
The technology discloses etnangien, isolated from myxobacteria as well as chemically stabilized derivatives thereof allowing for the first time the development of a new and potent antibiotic based on this promising natural compound. Etnangien is active against gram-positive bacteria like mycobacteria including rifampicin-resistant strains. It acts as a general nucleic acid polymerase inhibitor (DNA, RNA, RT), the preferred target being RNA-polymerase. Further disclosed is the respective genecluster responsible for etnangien biosynthesis allowing for heterologous production of etnangien in a chosen production strain and finally enabling optimised fermentation conditions.
Commercial Opportunity
Etnangien and its stabilized derivatives are a promising basis for antibiotic drug development. Offered are
- a license covering etnangien, stabilised derivatives and the
respective genecluster for therapeutic development,
- co-operation for further development.
Patent Situation
Granted German patent for etnangien (DE 19630980), EP patent applications filed in 2007 for derivatives and genecluster.
Further Reading
Irschik et al., J. Nat. Prod. 2007, 70, 1060-1063
