Table 1.

Oncology clinical trials with compounds targeting the TGF-β pathway

DrugClinicaltrials.gov identifiersDiseaseMechanism of action
Antisense oligonucleotides (ASO)
AP12009 Antisense PharmaNCT00431561 (phase III)High-grade gliomaASO to TGF-β2 mRNA
NCT00844064 (phase I)Melanoma, pancreatic, and colorectal cancers
AP11014 Antisense PharmaPreclinical (42)NSCLC, prostate, and colorectal cancersASO to TGF-β1 mRNA
Belagenpumatucel-L (Lucanix) NovaRx CorpNCT00676507 (phase III)Advanced–stage NSCLCMixture of 4 allogenic NSCLC cell lines engineered to express ASO to TGF-β2 mRNA
Anti–TGF-β antibodies and ligand traps
NCT00356460 (phase I)Renal cell carcinoma, malignant melanoma, mesotheliomaHuman pan–TGF-β monocloncal neutralizing antibody
GC1008* GenzymeNCT01401062 (phase I)Metastatic breast cancer with radiotherapy
*Oncology trials recently suspendedNCT01472731 (phase I)Malignant glioma
Fc:TβRIIPreclinical (47–49)Mesothelioma, liver, breast, and pancreatic cancersSoluble TβRII fused to Fc domain of murine IgG1
TGF-β receptor kinase inhibitors
LY2157299 Eli Lilly and CompanyNCT01246986 (phase I)Hepatocellular carcinomaTargets the ATP-binding site of TβRI kinase
NCT01220271 (phase I/II)Malignant glioma with radiochemotherapy
NCT01373164 (phase I/II)Pancreatic cancer with gemcitabine
SC-208 SciosPreclinical (50)Malignant glioma
SB-431542 GlaxoSmithKlinePreclinical (51)Malignant glioma
LY2109761 Eli Lilly and CompanyPreclinical (53–56)Colon, pancreatic, and breast cancerDual TβRI/TβRII kinase inhibitor