Table 1 Examples of drugs used in ER-positive breast cancer treatment
From: Targeting protein quality control pathways in breast cancer
| Drug name | Notes | Developmental stage | References |
|---|---|---|---|
| Fulvestrant (Faslodex) | Induces ER degradation, nonsteroidal selective estrogen receptor degrader (SERD) | FDA approved | [288,289,290,291,292] |
| Tamoxifen | Nonsteroidal selective estrogen receptor modulator (SERM) | FDA approved | [6,294,, 288, 293–295] |
| Raloxifene hydrochloride | Nonsteroidal selective estrogen receptor modulator (SERM) | FDA approved | [296,297,298,299,300,301] |
| Toremifene (Fareston) | Nonsteroidal selective estrogen receptor modulator (SERM) | FDA approved | [301, 302] |
| ARN-810 | Nonsteroidal selective estrogen receptor degrader (SERD) | Clinical trial | [303, 304] |
| AZD9496 | Nonsteroidal selective estrogen receptor degrader (SERD) | Clinical trial | [305, 306] |
| RAD1901 | Nonsteroidal selective estrogen receptor degrader (SERD) | Clinical trial | [307,308,309] |
| Letrozole (Femara) | Nonsteroidal inhibitor of estrogen synthesis (aromatase inhibitor) | FDA approved | [310,311,312,313] |
| Anastrozole (Arimidex) | Nonsteroidal inhibitor of estrogen synthesis (aromatase inhibitor) | FDA approved | [314,315,316,317] |
| Exemestane (Aromasin) | Nonsteroidal inhibitor of estrogen synthesis (aromatase inhibitor) | FDA approved | [318,319,320,321] |
| BEZ235 | Dual inhibitor of PI3K and mTOR | Clinical trial | [322,323,324,325] |
| SAR245409 | PI3K inhibitor | Clinical trial | [285, 313] |
| Taselisib | Class I PI3K alpha inhibitor | Clinical trial | [326,327,328] |
| Buparlisib | PI3K inhibitor, competes for the ATP binding | Clinical trial | [63, 326] |
| Venetoclax (ABT-199) | Bcl-2 inhibitor | Clinical trial | [329, 330] |
| Everolimus (Afinitor) | Inhibitor of mTORC1 used both in luminal A and in HER2-positive tumors | FDA approved | [277,278,279, 283] |
| Temsiroliums | Inhibitors of mTORC1 used in luminal A, TNBC, and HER2-positive tumors | Clinical trial | [331] |
| Vorinostat (SAHA) | Global inhibitor of HDAC | Clinical trial | [332,333,334] |
| Entinostat | Inhibitor of HDAC1 and HDAC3 | Clinical trial | [335, 336] |
| Panobinostat | Specific inhibitor of HDAC | Clinical trial | [337,338,339] |
| Rapamycin | mTOR inhibitor | HER- and ER-positive breast cancer cells | [340,341,342,343,344] |
| SNIPER(ER) | PROTAC-mediated ER degradation in breast cancer cells | ER-positive breast cancer cells | [98, 345] |
| BHPI | Modulator of ER-dependent UPR response | ER-positive breast cancer cells | [168, 187, 188, 346] |
| MAb159 | Monoclonal antibody against BiP | ER-positive breast cancer cells | [222] |
| Plumbagin | BiP downregulator, induces BIK levels | ER-positive breast cancer cells | [220] |
| Epigallocatechin gallate (EGCG) | Inhibits cellular oxidation and DNA methyltransferase to block EGFR and HER2 activation and can induce UPR response by binding BiP | TNBC, ER- and HER2-positive breast cancer cells | [347,348,349,350,351,352] |
| Resveratrol | Activates SIRT-1 and inhibits TNF-induced activation of NFkB. Used in combination with bortezomib, reduces cell viability through autophagy inhibition | ER- and HER2-positive breast cancer cells | [353, 354] |
| Hydroxychloroquine | Autophagy inhibitor, suppresses lysosomal acidification | Clinical trial | [167, 225] |