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Major Progress | Significant Research Advancement Achieved in MoMed Biotech's Independently Developed Oral Estrogen Hybrid Degrader Molecule Drug

2023.10.16

MoMed Biotech's latest experiment results show that the PROTAC molecule designed and developed by the R&D team can significantly reduce the level of ERα protein in MCF-7 cells of human breast cancer. The best degradation agent, DC50, has a value of 0.67 nM, which is the same as the degradation level achieved by the ARV-471 developed by Arvinas (entering clinical phase II, DC50=1.8 nM).Background:Breast cancer is the most common malignant tumor that occurs in breast epithelial tissue, with the highest mortality rate among female malignancies. According to the global cancer data released by the International Agency for Research on Cancer (IARC) of the World Health Organization in 2020, about 2.26 million women were diagnosed with breast cancer (about 685,000 died from breast cancer), surpassing the number of lung cancer diagnoses for the first time at 2.21 million, becoming the "largest cancer in the world"; The 2023 cancer data report of the top medical journal Clinical Oncology (CA) in the world shows that breast cancer still ranks first in the high incidence rate of cancer in women. In China, the heavy burden caused by breast cancer is not inferior, and with the amplifying effect of population aging, it may further increase without sustained effective intervention. In breast cancer tumor tissues, various targets related to the occurrence and development of breast cancer can be observed. Many drugs have been applied clinically for these targets. However, most of these drugs belong to small molecule inhibitors. With long-term use of drugs, many patients will develop drug resistance. Therefore, overcoming drug resistance and developing more effective drugs have become urgent problems to be solved in current breast cancer treatment. Proteolysis targeting chimera (PROTAC) technology is a new type of targeted protein degradation technology, which has shown good application prospects in drug development field. Drugs such as Bavdegalutamide, ARV-471, and NX-2127, which have entered the clinical stage, have confirmed the activity and future application potential of PROTAC in cancer treatment. Targeting the relevant targets in breast cancer by using PROTAC technology for degradation is expected to become one of the feasible strategies in breast cancer treatment.Experimental results:Estrogen receptor (ER) is a steroid hormone receptor and belongs to a large nuclear receptor family. In addition, estrogen receptors are also estrogen-regulated transcription factors that play a key role in the occurrence and proliferation of breast cancer. It is estimated that nearly 80% of breast cancer expresses estrogen receptors. Recently, MoMed Biotech's self-developed oral chimeric degradation agent molecule development project team announced good news regarding the estrogen-targeting molecule they designed. The latest experimental results show that the molecule designed by the R&D team can significantly reduce the level of ERα protein in MCF-7 cells of human breast cancer. The best degradation agent, DC50, has a value of 0.67 nM. This is the same level achieved by the ARV-471 developed by Arvinas (entering clinical phase II, DC50=1.8 nM).

https://qiniu.mfdemo.cn/momed/微信截图_20231016141808.webp

MoMed Biotech will continue to further optimize the existing degradation agents and conduct animal experiments to verify their effectiveness and safety in the future.

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