Drug intelligence / Profile preview

SYH2039

Development stage
Phase 1
Lead developer
BeiGene
Modality
Small Molecules
Administration
Oral
01

Overview

SYH2039 is a novel, orally administered small molecule inhibitor of methionine adenosyltransferase 2A (MAT2A), developed for the treatment of solid tumors harboring MTAP (methylthioadenosine phosphorylase) deletion mutations. MTAP deletion occurs in approximately 15% of all cancers, including glioblastoma, pancreatic cancer, and non-small cell lung cancer. The loss of MTAP disrupts methionine metabolism in tumor cells, creating a unique vulnerability that MAT2A inhibitors like SYH2039 can exploit by selectively blocking methionine production and starving cancer cells while sparing normal tissue. The drug is being developed by CSPC ZhongQi Pharmaceutical Technology and has been globally licensed to BeiGene (soon to be BeOne Medicines). It is currently in phase 1 clinical trials for advanced or metastatic solid tumors with plans for combination therapy with PRMT5 inhibitors[1][2][3][4][5][6][7][8].

02

Targets

MAT2A (Methionine adenosyltransferase 2A)

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