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DALANTERCEPT ALK-1 ligand trap Prop INN; USAN Angiogenesis inhibitor Treatment of solid tumors

DRUGS OF THE FUTURE(2015)

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Abstract
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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Key words
Dalantercept,ALK-1 inhibitor,Fusion protein,ACE-041,Ligand trap,Endometrial carcinoma,Ovarian cancer,Head and neck cancer,Renal cell carcinoma,Hepatocellular carcinoma
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