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. Author manuscript; available in PMC: 2014 May 19.
Published in final edited form as: Nat Rev Cancer. 2013 Oct 17;13(11):788–799. doi: 10.1038/nrc3603

Table 2.

Identified microenvironmental effects of TGFβ inhibitors in preclinical tumour models

Drug name Cancers tested Microenvironmental effects Refs
TGFβ ligand trap
P144 Melanoma Increased dendritic cell, natural killer cell and T cell activity 144
1D11 Lung, breast and glioblastoma
  • Increased natural killer cell infiltration and CD8+ T cell-mediated tumour cell killing

  • Decreased blood vessel area

119,145, 146
TGFβ antisense
AP12009 Pancreatic Increased immune cell-mediated cytotoxicity 123
Receptor inhibitors
GW788388 Oesophageal squamous cell carcinoma
  • Decreased fibroblast activation

  • Decreased vascular development

147
LY2109761 Hepatocellular carcinoma and glioblastoma
  • Decreased angiogenesis

  • Increased pericyte coverage

148,149
LY364947 Glioblastoma Increased vascular permeability 146
LY3022859 Breast, pancreas and colon
  • Increased natural killer cell and cytotoxic T cell-mediated tumour cell killing

  • Decreased TReg cell presence

  • Decreased MDSC infiltration

126
SB431542 Breast Increased dendritic cell maturation 98
SD-208 Breast cancer bone metastasis and glioma
  • Decreased osteoclast differentiation

  • Increased immune cell-mediated cytotoxicity

127
SX-007 Glioma Increased presence of CD3+ T cells 150
SM-16 Lung
  • Increased number of activated CD8+ T cells

  • Increased presence of CD4+ T cells

151

MDSC, myeloid-derived suppressor cells; TGFβ, transforming growth factor-β; TReg, regulatory T.