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Drugs Fut 2015, 40(10): 633
ISSN 0377-8282
Copyright 2015 Clarivate Analytics
CCC: 0377-8282
DOI: 10.1358/dof.2015.040.10.2386993
 
 
Dalantercept. ALK-1 ligand trap, Angiogenesis inhibitor, treatment of solid tumors
Hector-Greene, M.E., Blobe, G.C.
 
 
The TGF-beta superfamily receptor activin receptor-like kinase 1 (ALK-1) has essential roles in regulating angiogenesis during development and homeostasis, as well as pathophysiological tumor angiogenesis. Dalantercept is a soluble chimeric protein composed of the ALK-1 extracellular domain fused to the human Fc domain. Dalantercept acts as a ligand trap to prevent the activation of endogenous ALK-1 by bone morphogenetic proteins 9/10. In preclinical models, dalantercept inhibits tumor growth and enhances the efficacy of cytotoxic chemotherapy. In early clinical development, dalantercept as a single agent has had a promising disease control rate. Dalantercept has a favorable safety profile, with fluid retention and edema being the most common side effects. Current studies are investigating the role of dalantercept with cytotoxic chemotherapy and other targeted therapies.


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