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Summary of TGF-β inhibitors as novel therapeutic targets

DrugMechanism of actionDevelopment stageMalignancy typeReferenced summary of results
AP12009Antisense oligodeoxynucleotide specific for the mRNA of human TGF-β2Phase I/IIGlioblastoma/anaplastic astrocytomaSuperior efficacy and safety for AP12009 over chemotherapy and positive risk-benefit assessment71
CAT192 (lerdelimumab)Monoclonal antibody to TGF-β1PreclinicalHuman lung epithelial cells (A549)An approximate median inhibitory concentration (IC50) value of 3 mg/mL72
GC1008Monoclonal antibody to TGF-β1Phase IAdvanced renal cell carcinoma or malignant melanomaSafe and well tolerated73
AP11014Antisense oligodeoxynucleotide specific for the mRNA of human TGF-β1PreclinicalLung, colon, and prostate cancer cell linesDecreased TGF-β secretion73
ID11Monoclonal antibody to TGF-βPreclinicalBreast cancer cell linesSuppressed breast cancer metastases to lungs74