darovasertib + siremadlin

Darovasertib (formerly LXS196 or IDE196) is a potent, oral small molecule inhibitor of protein kinase C (PKC), designed to target cancers with GNAQ and GNA11 mutations. It inhibits both novel and classical PKC isoforms, disrupting the PKC signaling pathway that drives proliferation in uveal melanoma cells. Siremadlin (HDM201) is a highly potent and selective small molecule inhibitor of the p53-MDM2 interaction; by blocking MDM2, it prevents degradation of p53 and thereby reactivates this tumor suppressor pathway. The combination of darovasertib and siremadlin is being investigated for synergistic anti-tumor activity in metastatic uveal melanoma—particularly in patients whose tumors harbor GNAQ/GNA11 mutations—by simultaneously inhibiting oncogenic PKC signaling and restoring p53 function[3][4][5][7].

Other names

darovasertib + HDM201LXS196 + HDM201