Drug intelligence / Profile preview

ralimetinib + gemcitabine + carboplatin

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Ralimetinib (LY2228820) is a highly selective, oral small molecule inhibitor of p38α and p38β mitogen-activated protein kinases (MAPKs), developed for oncology indications. Its primary anticancer mechanism involves inhibition of the p38 MAPK pathway, which is crucial for tumor cell survival and regulation of pro-inflammatory cytokines, as well as angiogenesis. In addition, ralimetinib can directly inhibit EGFR kinase, although with lower potency compared to p38α. The combination of ralimetinib with gemcitabine (a nucleoside analog cytotoxic chemotherapy) and carboplatin (a platinum-based alkylating agent) has been evaluated in clinical trials for advanced cancers such as platinum-sensitive ovarian cancer, aiming to exploit synergistic mechanisms: cell signaling pathway inhibition (p38 MAPK/EGFR), DNA synthesis inhibition, and DNA crosslinking[1][2][3][4].

Other names
ralimetinib + gemcitabine + carboplatin
02

Targets

MAPK11 (p38 beta mitogen-activated protein kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)DNA

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