Out-licensing

Elucidation of Novel Pharmaceutical Compound Classes with Anti-Tumour Properties

Introduction/Background

In all modern industrial societies increasing incidences of most classes of solid malignant tumours are observed. Despite this fact, traditional tumour therapy has changed little over the past years: standard preparations derived from only a small number of first-generation cytotoxic agents are still administered even today. Due to their frequently unfavourable therapeutic index, ie, their lack of cell specificity, these are leading to severe impairments in healthy tissue, too, or they induce troublesome side effects and thus prove inefficient in the treatment of recurrent cancer diseases. Moreover, for many of these agents patent protection will expire soon while an adequate pipeline of follow-up products with innovative mechanisms of action and ease of administration is still lacking. Recently several natural compounds with promising anti-tumour effects have been isolated from tunicates, sponges, as well as marine microorganisms of which some have already found their way into advanced clinical trials. Their use in adjuvant therapy or in synergistic action with molecular-targeted therapies gives reason to the hope to actually cure the disease in the future rather than simply prolongate life expectancy.

Aims/Hypothesis

We are investigating novel anti-tumour compounds.

Research

The physiological role of natural products with isoquinoline or naphthalene skeletal frameworks served as a model for the three synthesized compound classes A-C, for which for the first time a pronounced growth inhibition of various tumour cell lines was now found. Low-molecular-weight natural compounds (C) or their structural analogues (A,B) are expectedly to show a good drug likeness. Distinct in vitro activities have been observed for the lead structures with uniformly broad activity profiles. There is an almost immeasurable cytotoxicity of the lead structures and many derivatives toward healthy mammalian cells and minimal sub-acute toxicity in animal experiments.

Conclusion

Novel pharmaceutical compound classes have been identified with anti-tumour properties.

Relevance/Opportunity

These novel agents can be developed a therapy of tumour diseases, particularly of the lymphatic tissue, as well as inflammatory diseases. A German patent has been granted and additional German and international patent applications are pending. Development partnerships with out-licensing option are being sought. Please enquire quoting reference no. UMZ063.

Preclinical