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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, 293295]
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]