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 | |
Tamoxifen | Nonsteroidal selective estrogen receptor modulator (SERM) | FDA approved | |
Raloxifene hydrochloride | Nonsteroidal selective estrogen receptor modulator (SERM) | FDA approved | |
Toremifene (Fareston) | Nonsteroidal selective estrogen receptor modulator (SERM) | FDA approved | |
ARN-810 | Nonsteroidal selective estrogen receptor degrader (SERD) | Clinical trial | |
AZD9496 | Nonsteroidal selective estrogen receptor degrader (SERD) | Clinical trial | |
RAD1901 | Nonsteroidal selective estrogen receptor degrader (SERD) | Clinical trial | |
Letrozole (Femara) | Nonsteroidal inhibitor of estrogen synthesis (aromatase inhibitor) | FDA approved | |
Anastrozole (Arimidex) | Nonsteroidal inhibitor of estrogen synthesis (aromatase inhibitor) | FDA approved | |
Exemestane (Aromasin) | Nonsteroidal inhibitor of estrogen synthesis (aromatase inhibitor) | FDA approved | |
BEZ235 | Dual inhibitor of PI3K and mTOR | Clinical trial | |
SAR245409 | PI3K inhibitor | Clinical trial | |
Taselisib | Class I PI3K alpha inhibitor | Clinical trial | |
Buparlisib | PI3K inhibitor, competes for the ATP binding | Clinical trial | |
Venetoclax (ABT-199) | Bcl-2 inhibitor | Clinical trial | |
Everolimus (Afinitor) | Inhibitor of mTORC1 used both in luminal A and in HER2-positive tumors | FDA approved | |
Temsiroliums | Inhibitors of mTORC1 used in luminal A, TNBC, and HER2-positive tumors | Clinical trial | [331] |
Vorinostat (SAHA) | Global inhibitor of HDAC | Clinical trial | |
Entinostat | Inhibitor of HDAC1 and HDAC3 | Clinical trial | |
Panobinostat | Specific inhibitor of HDAC | Clinical trial | |
Rapamycin | mTOR inhibitor | HER- and ER-positive breast cancer cells | |
SNIPER(ER) | PROTAC-mediated ER degradation in breast cancer cells | ER-positive breast cancer cells | |
BHPI | Modulator of ER-dependent UPR response | ER-positive breast cancer cells | |
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 | |
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 | |
Hydroxychloroquine | Autophagy inhibitor, suppresses lysosomal acidification | Clinical trial |