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.
 |
| 2nd generation PRMT5 inhibitor |
| BG PRMT5i |
In 2019 and 2023, Beigene filed patents for PRMT5 inhibitors, providing several examples.
| Patents |
[Update] In September 2024, Beigene registered a phase 1 trial (NCT06589596) of BGB-58067 monotherapy in solid tumors patients. The potential of combining PRMT5 inhibitor with IO therapy (anti-PD-1, etc.) may be explored.
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.
Comments