prexasertib + ralimetinib

**Prexasertib + ralimetinib** is an investigational combination therapy that pairs prexasertib, a checkpoint kinase 1 (CHK1) inhibitor, with ralimetinib, a p38 mitogen-activated protein kinase (MAPK) inhibitor. Prexasertib inhibits CHK1, leading to impaired DNA damage response and promotion of cancer cell death, especially in the presence of replicative stress or DNA damage. Ralimetinib targets p38 MAPK—a signaling molecule involved in cell stress response, inflammation, and possibly tumor progression. This drug combination was designed to test synergistic antitumor effects, particularly in patients with advanced or metastatic cancers, including those with certain KRAS and/or BRAF mutations. In a phase 1 trial, the combination was not able to establish a recommended phase 2 dose due to toxicities[1][5][7]. Both drugs are investigational agents developed by Eli Lilly.

Other names

prexasertib + ralimetinib