Measure the inhibition of ERα-SRC3 binding by T6Is, showing varying degrees of inhibition
NPJ Breast Cancer. 2022 Dec 14;8(1):130
T47D cells
1 μM
24 hours
Measure the effect of T6Is on ERα accumulation, most T6Is show SERM-like increases
NPJ Breast Cancer. 2022 Dec 14;8(1):130
MCF7 cells
1 μM
24 hours
Measure the effect of T6Is on ERα levels, showing T6Is increase ERα levels similar to SERM
NPJ Breast Cancer. 2022 Dec 14;8(1):130
Lasofoxifene/酒石酸拉索昔芬 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NSG mice
MIND model
Subcutaneous injection
10 mg/kg
5 days/week, 90–93 days of treatment
To evaluate the antitumor activity of lasofoxifene alone or combined with palbociclib in a letrozole-resistant breast tumor model without ESR1 mutations. Results showed that lasofoxifene alone or combined with palbociclib significantly reduced primary tumor growth and bone metastases.
Breast Cancer Res. 2024 Jun 7;26(1):95
NSG mice
Mammary intraductal model
Subcutaneous injection
1, 5, or 10 mg/kg
5 days/week for 70 days
To evaluate the anti-tumor activity of lasofoxifene in breast cancer xenograft models expressing Y537S and D538G ER α mutants. Results showed that lasofoxifene was more effective than fulvestrant at inhibiting primary tumor growth and reducing metastases.
Breast Cancer Res. 2021 May 12;23(1):54
Mice
C451A mice (lacking mERα signaling)
Subcutaneous injections
8 μg/mouse/day
Daily for 3 weeks
To evaluate the effects of Lasofoxifene on uterus, bone, thymus, and fat tissue. Results showed that Lasofoxifene effects on uterine weight were mERα-independent, while its effects on bone and thymus were mERα-dependent. Additionally, Lasofoxifene reduced fat percentage in mice lacking functional mERα signaling.
J Endocrinol. 2022 Mar 29;253(2):75-84
Mice
Renal ischemia-reperfusion injury model
Injection
10 mg/kg
Administered at 16 and 1 h before IRI
Lasofoxifene treatment did not significantly ameliorate renal ischemia-reperfusion injury
Transplantation. 2022 Nov 1;106(11):2166-2171
Female DBA/1 mice
OVX mice with collagen-induced arthritis
Subcutaneous injection
4 mg/mouse/day
5 days a week, starting from the first signs of arthritis (day 18)
Lasofoxifene significantly reduced the clinical severity of arthritis, decreased the histological grade of synovitis, and erosions on cartilage and bone. Moreover, Lasofoxifene protected against generalised bone loss in CIA by increasing trabecular BMD. Lasofoxifene also decreased serum markers of cartilage destruction and reduced serum IL-6 levels.
Rheumatology (Oxford). 2016 Mar;55(3):553-63
SKG mice
Zymosan-induced spondyloarthritis model
Subcutaneous osmotic pump
1.5 µg/day
Continuous for 6 weeks
Lasofoxifene inhibited joint inflammation and enhanced BMD, while also affecting the composition and biodiversity of gut microbiota.
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