ralimetinib + tamoxifen

**Ralimetinib + tamoxifen** is an investigational **combination therapy** consisting of ralimetinib (LY2228820 dimesylate) and tamoxifen. Ralimetinib is a **small-molecule inhibitor** of p38 MAPK (mitogen-activated protein kinase), a kinase involved in cell response to stress, cytokine production, and mechanisms of cancer cell survival. Tamoxifen is a selective estrogen receptor modulator, acting as an antagonist of estrogen receptors in breast tissue to inhibit hormone-driven tumor growth. This combination has been studied in clinical trials for **hormone receptor-positive metastatic breast cancer** refractory to aromatase inhibitors. Ralimetinib targets the p38 MAPK pathway to enhance anti-tumor activity and potentially overcome resistance to endocrine therapy, while tamoxifen suppresses estrogen-mediated tumor proliferation[1][5]. The recommended phase II dose in studies is 300 mg ralimetinib every 12 hours plus tamoxifen. No patients achieved complete or partial response, but some achieved stable disease for several months[5].

Other names

ralimetinib + tamoxifenLY2228820 + tamoxifen