Drug intelligence / Profile preview

W54011

Development stage
Preclinical
Lead developer
Mitsubishi Tanabe
Modality
Small Molecules
Administration
Oral
01

Overview

W54011 is a potent, selective, and orally active small molecule antagonist of the **C5a receptor (C5aR1/CD88)**. Originally developed by **Mitsubishi Tanabe Pharma**, it functions by competitively inhibiting the binding of the complement fragment C5a to its receptor, thereby blocking downstream signaling pathways involved in inflammation and tumor progression. In the context of oncology, W54011 has been shown to inhibit the growth, invasion, and stemness of glioblastoma cells by reversing epithelial-mesenchymal transition (EMT) and inducing apoptosis. While it is primarily utilized as a high-affinity pharmacological tool in preclinical research to investigate complement-mediated pathologies, its efficacy in animal models of glioblastoma and other inflammatory conditions highlights its potential therapeutic relevance.

02

Targets

C5AR1 (Complement C5a receptor 1)

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