Antiviral Drugs
Peptidic Drugs
Other Substances
Spin-offs
Antiviral Drugs Peptidic Drugs Other Substances Spin-offs

Other Substances

In the 1950s and early 1960s, the investigation of plant (Compositae family) metabolites made the Department one of the world centers in the area of natural product chemistry with many priorities in the identification and structure determination of natural products. The discovery in chamomile of an anti-inflammatory sesquiterpene, chamazulene, initiated the original synthesis of its derivative, guaiazulene I (1,4-dimethyl-7-isopropylazulene) and finally resulted in the preparation of DERMAZULEN, a commercial ointment with anti-allergic, anti-inflammatory, antipyretic, and antiseptic properties, still available today.

An investigation of insect hormones and hormone analogues, and the search for the potential of their use as an alternative means of insect pest control was another area in which the DNP obtained international recognition. A large array of juvenile hormone analogues (juvenoids) synthesized in the institute has been investigated for their effect on the physiology, development, reproduction and behavior of insects. This extensive research had led to the development of several new technologies that were field-tested and some have been patented and applied. Most notably, a technique based on the juvenoid methoprene against the pharaoh’s ant (Monomorium pharaonis) was designed. A widely-used commercial preparation LAFAREX®, which locally exterminated this troublesome pest, was an outcome of this research.

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Separation of Lu-177 for medical application

Lutetium-177 (Lu-177) is an important therapeutic radionuclide used to treat cancer. Targeted drugs deliver Lu-177 to tumors where it emits beta particles that destroy the cancer cells. Many types of solid tumors can be treated in this way, and there are numerous drugs in clinical trials that use Lu-177. However, preparing the radioactive Lu-177 for thousands of patients is a significant challenge. It must be perfectly separated from neutron-irradiated ytterbium-176, which is chemically similar. The purity required for medical use is high, and it must be achieved quickly to prevent losses due to radioactive decay. This makes the large-scale separation of Lu-177 extremely difficult.

Dr. Miloslav Polášek, Head of IOCB Prague’s Coordination Chemistry Research Group, has developed a unique technology that is much faster than the current methods for the separation of Lu-177 from Yb-176. The technology is based on molecules called chelators that wrap around the atoms of lutetium or ytterbium. The molecules were specially designed to recognize and amplify the small differences between these two elements. This technique achieves efficient separation in only 10 minutes using a conventional HPLC system, compared to many hours required by other separation technologies.

 

Schematic depiction of the separation method principle. (Credit: Tomáš David).

 

In May 2019, the Institute of Organic Chemistry and Biochemistry of the CAS (IOCB Prague) signed an agreement providing SHINE Technologies, LLC (SHINE) with a global and exclusive license to this novel separation technology.

In January 2020, SHINE, GE Healthcare and IOCB Prague announced the production of the first Lu-177 doses. The prepared purity and amount demonstrated the suitability of the technology for large-scale Lu-177 production. Most importantly, the lot passed GE Healthcare’s quality control testing, including internationally recognized radionuclide purity standards.

The success story continued in November 2020, when SHINE made the first commercial sales of Lu-177 prepared using the licensed separation technology. SHINE is currently completing a large-scale production facility in Janesville, Wisconsin, with a capacity to make 300,000 doses of Lu-177 per year. We can expect that the demand for Lu-177 will grow rapidly, as more clinical studies demonstrate the therapeutic power of Lu-177.

SHINE and IOCB Prague maintain a strong relationship and collaborative spirit outside of their purely commercial activities. In September 2021, they signed a collaboration agreement to foster further basic research of medical radionuclides by Dr. Polášek’s team at IOCB Prague.

SHINE Technologies

SHINE is a fusion technology company working to become the world’s leading provider of radioisotopes for nuclear medicine in the near term. Since 2019, SHINE has enhanced its ability to fill critical needs in the rapidly growing therapeutic isotope market. Its therapeutics division is currently commercializing the production of Lu-177, a therapeutic isotope, which then needs to be combined with a disease-specific target molecule to treat cancer.

More about Miloslav Polášek Group: https://polasek.group.uochb.cz/en

More about SHINE Technologies: https://www.shinefusion.com/

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