In this article, we will discuss Olaratumab (Mechanism of Action). So, let’s get started.
Mechanism of Action
Olaratumab is a human IgG1 antibody that binds platelet-derived growth factor receptor alpha (PDGFR-α).
PDGFR-α is a receptor tyrosine kinase expressed on cells of mesenchymal origin. Signaling through this receptor plays a
role in cell growth, chemotaxis, and mesenchymal stem cell differentiation. The receptor has also been detected on some
tumor and stromal cells, including sarcomas, where signaling can contribute to cancer cell proliferation, metastasis, and maintenance of the tumor microenvironment. The interaction between olaratumab and PDGFR-α prevents binding of the receptor by the PDGF-AA and -BB ligands as well as PDGF-AA, -BB, and -CC-induced receptor activation and downstream PDGFR-α pathway signaling. Olaratumab exhibits in vitro and in vivo anti-tumor activity against selected sarcoma cell lines and disrupted the PDGFR-α signaling pathway in in vivo tumor implant models.
Olaratumab exposure-response relationships and the time course of the pharmacodynamics response are unknown.