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. 2023 Mar 9;11(3):826. doi: 10.3390/biomedicines11030826

Table 2.

Application of SERMs in castration-resistant prostate cancer treatments.

Treatment Number (n) Findings Author
ADT+ toremifene 300–640 mg/m2 15 No cancer inhibitory effect [109]
Raloxifene 60 mg 13 Partial effect (5 of 13 patients) [108]
Fulvestrant 500 mg,
250 mg
20 No patients
reduced PSA by >50%
[111]
Raloxifene (60 mg) +
bicaltamide (50 mg)
18 Partial effect (4 of 18 patients) [107]
Concentrations of 5 µM and 25 µM of ERβ-selective agonist, 8-VE2, and 8β-VE2 in VCaP cells n/a The expression of AR protein ↓ by 52%
AR mRNA ↓ by 40%
[112]
Nano-targeted delivery of toremifene (1.0 to 100 μM) in PC3M cancer cell line n/a Prostate tumor growth ↓ by blocking ERα [110]

Abbreviations: ↑: increase; ↓: decrease; PSA: prostate-specific antigen; ADT: androgen deprivation receptor, AR: androgen receptor; mRNA: messenger ribonucleic acid.