The transforming growth factor-beta (TGF-β) signaling pathway has been reported to be dysregulated in the pathogenesis of several malignancies including gynecologic cancers. This provides a proof of concept of its potential value as a therapeutic target and prognostic biomarker in cervical cancer. Here we provide an overview on the biological role and clinical impact of TGF-β inhibitors either as a single agent or as a combinatorial therapy in gynecological cancers, concentrating on phase I to phase II/III clinical trials. Aberrant TGF-β signaling may lead to carcinogenesis. Inhibition of TGF-β represents an interesting area of focus for the treatment of gynecological cancer. There are several TGF-β inhibitors which are potential anticancer agents and are undergoing clinical trials in cancer, including galunisertib, dalantercept, and vigil. There is a growing body of data showing the potential therapeutic impact of targeting the TGF-β pathway in different cancer types, although further studies are still warranted to explore the value of this strategy and finding the most appropriate patients who could most benefit from therapy.
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