Table 4.
Small-molecule compounds inhibiting CSC progression through activating Hippo pathway
| Name | Target | Mechanism | Type of cancer | Phase | NCT number (starting time)/publication date | Assessment |
|---|---|---|---|---|---|---|
| Verteporfin | YAP/TAZ | Reduces the expression of CSC markers and suppresses CSC proliferation | Gastric and esophageal cancer | Preclinical | August 1, 2014 | Without visible toxicity in the mice [99] |
| gastric cancer | Preclinical | Apr 15, 2020 | ||||
| Evodiamine | LATS1/2 | Inhibits the proliferation of colon CSCs | Colon cancer | Preclinical | December 10, 2019 | Induces low toxicity and still needs much experiments to prove [100] |
| Fluvastatin | YAP | Reduces the expression of CD44 and the characteristics of malignant mesothelioma stem cells | Malignant mesothelioma | Preclinical | January 28, 2017 | Without any genotoxic, and relatively safe in patients [101, 102] |
| Atorvastatin | TAZ | Decreases MDA-MB 231 cells stemness-related features (such as the decrease of CD44+/CD24- subpopulation of cells) | Breast cancer | Phase II | NCT02416427(April 15, 2015) | Muscle loss [103] |
| CA3 | YAP/TEAD | Suppresses tumor microsphere, formation and reduces the proportion of ALDH1+ cells | Esophageal adenocarcinoma | Preclinical | February, 2018 | Without apparent toxicity in mice according to the current studies [104] |
| CPZ | YAP | Inhibits tumor microsphere-formation and stem marker expression | Breast cancer | Preclinical | April 1, 2019 | Induces fatal hepatic failure [105] |