Related Experiment Videos
[Lasofoxifene, a next generation estrogen receptor modulator: preclinical studies]
Tomoko Maeda1, Hua Zhu Ke, Hollis Simmons
1Pfizer Japan Inc., Pfizer Global Research and Development, Tokyo laboratories.
Clinical Calcium
|December 4, 2004
Summary
Selective estrogen receptor modulators (SERMs) offer a promising alternative to estrogen therapy for preventing osteoporosis. Lasofoxifene, a novel SERM, demonstrated efficacy in preclinical models for bone protection and breast cancer prevention without adverse uterine effects.
Area of Science:
- Pharmacology
- Endocrinology
- Oncology
Context:
- Estrogen replacement therapy (ERT) effectively prevents osteoporotic fractures but carries significant risks, limiting its use in postmenopausal women.
- A medical need exists for osteoporosis prevention modalities without estrogen's side effects.
- Selective estrogen receptor modulators (SERMs) aim to replicate estrogen's skeletal benefits while mitigating risks of uterine and breast cancer.
Purpose:
- To evaluate the efficacy and safety of lasofoxifene, a novel nonsteroidal SERM, as a potential therapy for postmenopausal osteoporosis and breast cancer prevention.
Summary:
- Lasofoxifene demonstrated potent binding to estrogen receptors, acting as a tissue-selective antagonist or agonist.
- In preclinical models, lasofoxifene inhibited bone turnover, prevented bone loss, and blocked estrogen-induced uterine hypertrophy.
- Lasofoxifene also inhibited breast tumor formation in preclinical cancer models and reduced serum cholesterol.
Impact:
- Preclinical data suggest lasofoxifene is a potential next-generation therapy for preventing estrogen deficiency-induced bone loss and breast cancer in postmenopausal women.
- Lasofoxifene's tissue-selective action may offer a favorable risk-benefit profile compared to traditional ERT.
- Further clinical investigation is warranted to confirm lasofoxifene's therapeutic potential.