. Author manuscript; available in PMC: 2009 Jun 8.

Published in final edited form as: Breast Cancer Res Treat. 2008 Oct 9;115(3):453–495. doi: 10.1007/s10549-008-0184-1

Table 1.

TGFβ pathway antagonists in clinical development

Agent	Class	Type	Molecular target(s)	Clinical trials	Clinical indication	Ref.
AP 12009	Ligand trap	Antisense oligonucleotide	TGFβ2	Phase II	Pancreas Colorectal Melanoma	[196, 198, 199]
Belagenpumatucel-L	Ligand trap	TGF-β2 antisense-modified tumor cell vaccine	TGFβ2	Phase II	Non-small cell lung cancer	[248, 249]
CAT-152 (lerdelimumab)	Ligand trap	Humanized monoclonal antibody (IgG4)	TGFβ2	Phase III	Glaucoma	[250, 251]
CAT-192 (metelimumab)	Ligand trap	Humanized monoclonal antibody (IgG4)	TGFβ1	Phase I-II	Systemic sclerosis	[252]
GC1008	Ligand trap	Human monoclonal antibody (IgG4)	TGFβ1, -2, -3	Phase I-II	Melanoma	[231]
LY2157299	Receptor serine-threonine kinase inhibitor	Small molecule	TβR-I/Alk5 (TGFβ) Alk4, Alk7 (Activin)	Phase I	Grade III-IV malignant glioma	[232]