Lasofoxifene (CAS 180916-16-9)
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Lasofoxifene, a third-generation selective estrogen receptor modulator (SERM. With a non-steroidal nature and derived from naphthalene, lasofoxifene selectively binds to estrogen receptor alpha (ERα ESR1) and estrogen receptor beta (ERβ ESR2) with high affinity. By mimicking the effects of endogenous estradiol, it exerts varying agonist and antagonist effects in tissues expressing these receptors. Lasofoxifene′s mechanism of action involves exerting an agonist effect on estrogen receptors expressed in bone tissue, mimicking the positive effects of estrogen. It reduces the production and lifespan of osteoclasts by altering the NF-kappaB ligand (RANKL)/RANK/osteoprotegerin system, stimulates osteoblast activity, and influences calcium homeostasis. However, it acts as an antagonist by suppressing estrogen signaling in oncogenic pathways and inhibiting downstream gene transcription. Additionally, studies suggest that lasofoxifene may act as an inverse agonist at the CB2 cannabinoid receptor expressed in bone, inhibiting osteoclast formation and resorptive activity.
Lasofoxifene (CAS 180916-16-9) References
- Lasofoxifene (CP-336,156), a selective estrogen receptor modulator, prevents bone loss induced by aging and orchidectomy in the adult rat. | Ke, HZ., et al. 2000. Endocrinology. 141: 1338-44. PMID: 10746637
- Long-term treatment of lasofoxifene preserves bone mass and bone strength and does not adversely affect the uterus in ovariectomized rats. | Ke, HZ., et al. 2004. Endocrinology. 145: 1996-2005. PMID: 14726439
- Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in female rats. | Terry, KK., et al. 2004. Birth Defects Res B Dev Reprod Toxicol. 71: 150-60. PMID: 15282736
- Lasofoxifene enhances vaginal mucus formation without causing hypertrophy and increases estrogen receptor beta and androgen receptor in rats. | Wang, XN., et al. 2006. Menopause. 13: 609-20. PMID: 16837883
- Disposition of lasofoxifene, a next-generation selective estrogen receptor modulator, in healthy male subjects. | Prakash, C., et al. 2008. Drug Metab Dispos. 36: 1218-26. PMID: 18372400
- Effects of lasofoxifene on the uterus, vagina, and breast in ovariectomized cynomolgus monkeys (Macaca fascicularis). | Cline, JM., et al. 2008. Am J Obstet Gynecol. 199: 158.e1-8. PMID: 18501325
- Lasofoxifene for the prevention and treatment of postmenopausal osteoporosis. | Lewiecki, EM. 2009. Ther Clin Risk Manag. 5: 817-27. PMID: 19898646
- Lasofoxifene: Evidence of its therapeutic value in osteoporosis. | Gennari, L., et al. 2010. Core Evid. 4: 113-29. PMID: 20694069
- The gynecologic effects of lasofoxifene, an estrogen agonist/antagonist, in postmenopausal women. | Archer, DF. 2011. Menopause. 18: 6-7. PMID: 21173718
- Lasofoxifene, from the preclinical drug discovery to the treatment of postmenopausal osteoporosis. | Gennari, L., et al. 2011. Expert Opin Drug Discov. 6: 205-17. PMID: 22647137
- CB2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene. | Kumar, P. and Song, ZH. 2014. Biochem Biophys Res Commun. 443: 144-9. PMID: 24275139
- Efficacy of Pharmacological Therapies for the Prevention of Fractures in Postmenopausal Women: A Network Meta-Analysis. | Barrionuevo, P., et al. 2019. J Clin Endocrinol Metab. 104: 1623-1630. PMID: 30907957
- Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. | Lainé, M., et al. 2021. Breast Cancer Res. 23: 54. PMID: 33980285
- Selective estrogen receptor modulator lasofoxifene suppresses spondyloarthritis manifestation and affects characteristics of gut microbiota in zymosan-induced SKG mice. | Jeong, H., et al. 2021. Sci Rep. 11: 11923. PMID: 34099783
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Lasofoxifene, 5 mg | sc-211721 | 5 mg | $388.00 | |||
Lasofoxifene, 25 mg | sc-211721A | 25 mg | $1510.00 |