ELTE researchers have developed a new Hungarian anti-cancer active agent candidate with outstanding activity that can be used in low doses, in the framework of the Synthesis+ excellence program.
Colleagues of Eötvös Lóránd University have developed two fluorine- and one chlorine-substituted derivatives under the code name TBP-333 as a more effective anti-cancer active agent candidate than any other. They uphold that tumors are among the leading causes of death worldwide. Since the 1990s, the number of cancer deaths has skyrocketed, with the total number of cancer deaths in the EU Member States and the UK having approached 1.5 million in 2022.
Treating cancer is a major challenge. Traditional chemotherapy treatments use drugs that kill most tumor cells but also cause significant damage to healthy cells, with many side effects.
Other serious problems include the recurrence of metastatic tumors and the frequent development of resistance to chemotherapeutic agents.
Therefore, in recent years, a prominent role has been given to so-called targeted oncological therapies, in which the active agent used is used to induce uncontrolled division of cancer cells that are malfunctioning in cell cycle regulation. These treatments target specific molecular targets within cells, such as proteins.
The direct objective of the Synthesis+ excellence program is to develop and expand the synthetic capacity of ELTE. The indirect goal of the program is to strengthen, coordinate and enhance the synergies between colleagues, workshops, and communities related to synthetic works, so that the university can be more effective in research and development, and focus on some areas of innovation.
ELTE Faculty of Science. Photo via Facebook/ELTE Természettudományi kar
The ELTE Faculty of Science is also conducting research on the development of anti-cancer active agents with the support of the Synthesis+ excellence program. The Department of Organic Chemistry has so far produced more than 140 new compounds, including the TBP-333 derivative,
whose two fluorine and one chlorine atom have been specially substituted, is proving to be the most potent potential anti-cancer active agent candidate to date.
Comparative tests have shown the new Hungarian active agent to be significantly more potent than ONC-212, considered by US developers to be the most promising candidate (soon to enter human clinical trials involving pancreatic cancer and leukemia patients).
As described, against PANC-1 pancreatic carcinoma cells that are highly resistant to chemotherapy treatments, TBP-333 is much less toxic to the body, thus reducing the expected adverse side effects and anti-tumor activity by several orders of magnitude compared to ONC-212, being about 4,000 times more potent.
The TBP-333 compound has also been proven internationally, and the Toronto research team working with Hungarian researchers, has tested and proven its efficacy. Extensive biological research, among other things, is now needed before the candidate can progress to clinical use.