Drug intelligence / Profile preview

ralimetinib

Development stage
Phase 2
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Ralimetinib is an orally administered small molecule developed primarily as a selective, ATP-competitive inhibitor of the α and β isoforms of p38 mitogen-activated protein kinase (MAPK), with nanomolar potency. It was originally designed to target p38 MAPK, which regulates cytokine production in the tumor microenvironment and supports cancer cell survival under stress. However, recent research indicates that ralimetinib also inhibits epidermal growth factor receptor (EGFR) kinase activity, and its anticancer effects are likely driven by EGFR inhibition rather than p38α inhibition. Ralimetinib has been investigated in clinical trials for various cancers including ovarian cancer (phase II), glioblastoma (phase I/II), metastatic breast cancer, fallopian tube cancer, and advanced solid tumors. The drug was developed by Eli Lilly[1][2][3][4][5][6][7].

Other names
ralimetinib mesylateLY2228820 FREE BASELY-2228820 FREE BASELY 2228820 FREE BASE
02

Targets

MAPK11 (p38 beta mitogen-activated protein kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)MAPK14 (p38 mitogen-activated protein kinase alpha)CYP3A4 (Cytochrome P450 3A4)

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