pemrametostat

Pemrametostat is an orally available, potent, selective, and reversible small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5). PRMT5 is an enzyme involved in the methylation of arginine residues on histones and other proteins, which regulates gene expression and various cellular processes. By inhibiting PRMT5, pemrametostat decreases the levels of monomethylated and dimethylated arginine residues in histones H2A, H3, and H4. This modulation can lead to altered gene expression profiles that suppress cell proliferation and promote cell death in rapidly dividing cells such as cancer cells. Pemrametostat has demonstrated antiproliferative and antineoplastic activities in preclinical models. It is under clinical investigation for hematologic malignancies including myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), acute myeloid leukemia (AML), as well as advanced solid tumors and non-Hodgkin lymphoma[1][2][3][4][6].

Other names

protein arginine methyltransferase 5 inhibitor GSK3326595