Beigene has submitted the IND application for the PRMT5 (Protein arginine methyltransferase 5) inhibitor BGB-58067 in China. This aligns with the plan to enter the clinic in Q4 2024.
BGB-58067
BGB-58067 is a second-generation MTA-cooperative PRMT5 inhibitor with brain-penetrating and good intracranial efficacy. MTAP-deletion lung cancer and GI cancers are the target diseases for the PRMT5 inhibitor.
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| 2nd generation PRMT5 inhibitor |
| BG PRMT5i |
In 2019 and 2023, Beigene filed patents for PRMT5 inhibitors, providing several examples.
| Patents |
PRMT5 Inhibitors in China
Currently, no PRMT5 inhibitors are under investigation in the clinical stage. SIM0272, discovered by Simcere, was terminated from the phase 1 trial as an R&D strategy adjustment.GTA182
GTA182 is also an MTA-cooperative, brain-penetrant, second-generation PRMT5 inhibitor discovered by GT Apeiron. It also demonstrates > 100-fold selectivity for MTAP deleted cells compared with MTAP wild-type cells. The core structure of the compounds in its patent is similar to that of Beigene's.
Apeiron filed the IND application for GT182 in July 2024.
| GT182 |
ABSK131 and ABSK132 are also MTA-cooperative PRMT5 inhibitors discovered by Abbsiko Therapeutics. The two products, which may be designed like the two different core structures in BeiGene's two patents, are still in the preclinical stage.
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