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PRMT5 inhibitor (MTA-cooperative)
- Development stage
- Preclinical
- Lead developer
- Ryvu Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
PRMT5 inhibitor (MTA-cooperative), also known as RVU305, is an oral, brain-penetrant, methylthioadenosine (MTA)-cooperative inhibitor of protein arginine methyltransferase 5 (PRMT5) being developed by Ryvu Therapeutics. It is designed to target cancers with homozygous deletion of the methylthioadenosine phosphorylase (MTAP) gene, which is codeleted with CDKN2A in approximately 10-15% of human tumors. In MTAP-deleted cells, the accumulation of MTA leads to partial inhibition of PRMT5, creating a synthetic lethal vulnerability. RVU305 selectively binds and stabilizes the PRMT5-MTA complex, inhibiting PRMT5-dependent symmetric arginine dimethylation (SDMA) and tumor growth while sparing normal MTAP wild-type cells. It is currently in IND/CTA-enabling preclinical development for MTAP-deleted solid tumors, including glioblastoma.
- Other names
- MTA-cooperative PRMT5 inhibitor
02
Targets
PRMT5 (Protein arginine N-methyltransferase 5)
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