Table 2.
Potential YAP Inhibitors Tested in Active TNBC Clinical Trials.
| Inhibitor | Clinical Trial Number | Mechanism | References |
|---|---|---|---|
| Zoledronic Acid | NCT02595138 | Bisphosphonate which inhibits bone resorption and also inhibits farnesyl diphosphate synthase | [89] |
| Erlotinib | NCT02071862 | Epidermal growth factor receptor (EGFR) Inhibitor which can sequester YAP in the cytoplasm | [90] |
| Trametinib | NCT01964924 | MEK1/2 Inhibitor leading to decreased YAP protein levels and transcriptional activity. | [91] |
| Indomethacin | NCT02950259 | Nonsteroidal anti-inflammatory drug that inhibits prostaglandins and is associated with YAP1 stimulation. | [92] |
| Selumetinib (AZD6244) | NCT02583542 | MEK1/2 inhibitor which reduces YAP protein levels | [92] |
| Ipatasertib | NCT02162719 | ATP-competitive, selective AKT inhibitor which can reverse EMT conferred by YAP overexpression | [93] |
| Alisertib (MLN8237) | NCT02187991 | Aurora kinase A inhibitor which was capable of suppressing YAP protein levels | [94] |
Note: The Clinicaltrials.gov database was used to assess active, interventional clinical trials for TNBC treatment within phase 1, 2, 3, or 4 of development. Following inhibitor identification, literature was consulted to determine any YAP modulating effects [72].