Journal: Breast Cancer Research and Treatment

Article Title: Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy

doi: 10.1007/s10549-019-05454-y

Figure Lengend Snippet: Clinically relevant oral SERDs exhibit similar efficacy in tumor growth inhibition. a Tamoxifen-treated Nu:J mice bearing TamR xenograft tumors were randomized to treatment with vehicle (po qd), AZD9496 (10 mg/kg po qd), GDC0810 (25 mg/kg po qd), or BZA (12.5 mg/kg po qd). Data presented indicate the average tumor volume for each group (mean ± SEM) at each time point. *As compared to the vehicle control, significant ( p > 0.05) inhibition of tumor growth was observed for all treatments, while no significant differences were noted between treatments (2-way ANOVA analysis followed by Bonferroni multiple comparison test). b ER levels present in tumors harvested from mice included in a were analyzed by western blotting of tissue extracts. *A significant decrease in ER levels was observed for all SERD treatments (1-way ANOVA analysis followed by Bonferroni multiple comparison test). # p < 0.05: Significantly less ER turnover was observed following GDC0810 treatment as compared to AZD9496. Primary western blot images are included in Suppl. Fig. 2

Article Snippet: Fulvestrant, AZD9496, GDC0810, and bazedoxifene were purchased from MedChemExpress.

Techniques: Inhibition, Control, Comparison, Western Blot

Journal: Breast Cancer Research and Treatment

Article Title: Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy

doi: 10.1007/s10549-019-05454-y

Figure Lengend Snippet: % Tumor growth inhibition of TamR tumors over 4 weeks of treatment

Article Snippet: Fulvestrant, AZD9496, GDC0810, and bazedoxifene were purchased from MedChemExpress.

Techniques: Inhibition

Journal: Breast Cancer Research and Treatment

Article Title: Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy

doi: 10.1007/s10549-019-05454-y

Figure Lengend Snippet: The clinically relevant doses of SERDs exhibited similar efficacy when compared using an estrogen deprived model of aromatase inhibitor resistance. a Ovariectomized Nu:J mice bearing LTED (long-term estrogen deprived) xenograft tumors were randomized to treatment with vehicle (po qd), AZD9496 (10 mg/kg po qd), GDC0810 (25 mg/kg po qd), BZA (12.5 mg/kg po qd) or fulvestrant (25 mg/kg sc qw). Data presented indicate the average tumor volume for each group (mean ± SEM) at each time point. *As compared to the vehicle control, significant ( p > 0.05) inhibition of tumor growth was observed for all treatments, while no significant differences were noted between treatments (2-way ANOVA analysis followed by Bonferroni multiple comparison test). b ER levels present in tumors harvested from mice included in a were analyzed by western blotting of tissue extracts. A significant ( p < 0.05) decrease in ER levels was observed for all SERD treatments (1-way ANOVA analysis followed by Bonferroni multiple comparison test). Primary western blot images are included in Online Resource Fig. 3b. c Weights of uteri excised after euthanasia were recorded as a measure of uterine stimulation. *A significant ( p < 0.05) increase in uterine weight was observed for all AZD9496 and GDC0810 (1-way ANOVA analysis followed by Bonferroni multiple comparison test)

Article Snippet: Fulvestrant, AZD9496, GDC0810, and bazedoxifene were purchased from MedChemExpress.

Techniques: Control, Inhibition, Comparison, Western Blot