Lasofoxifene
| 202px | |
| Systematic (IUPAC) name | |
|---|---|
|
(5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol | |
| Identifiers | |
| CAS Number | 180916-16-9 |
| ATC code | G03XC (WHO) |
| PubChem | CID 216416 |
| Chemical data | |
| Formula | C28H31NO2 |
| Molar mass |
413.55 g/mol 563.64 g/mol (tartrate)[[Script error: No such module "String".]] |
Lasofoxifene (INN) (proposed tradename Fablyn) is a non-steroidal selective estrogen receptor modulator (SERM) which is under development by Pfizer for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy[1], and the result of an exclusive research collaboration with Ligand Pharmaceuticals (LGND).
In September 2005, Pfizer received a non-approvable letter from the U.S. Food and Drug Administration regarding lasofoxifene (trade name Oporia), a selective estrogen receptor modulator for the prevention of osteoporosis.
On January 2008, Ligand Pharmaceuticals, through its marketing partner, Pfizer, submitted a New Drug Application for lasofoxifene, which is now to be marketed under the tradename Fablyn.
Lasofoxifene was approved in the EU under the brand name Fablyn by the EMEA in March 2009.(see)
Lasofoxifene is a desmethyl dihydro analog of nafoxidine.[2]
Treatment
In postmenopausal women with osteoporosis, lasofoxifene at a dose of 0.5 mg per day was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events.[3][4]
Chemical Synthesis
Cameron, C. O.; Dasilva Jardine, P. A.; Rosati, R. L.; 1996, U.S. Patent 5,552,412.
References
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<references />, or <references group="..." />External links
- "Reference site for lasofoxifene information". Anakena Internet Services SL. Retrieved 2008-03-18.
| 40px | This drug article relating to the genito-urinary system is a stub. You can help ssf by expanding it. |
- ↑ Gennari L, Merlotti D, Martini G, Nuti R (2006). "Lasofoxifene: a third-generation selective estrogen receptor modulator for the prevention and treatment of osteoporosis". Expert Opin Investig Drugs. 15 (9): 1091–103. doi:10.1517/13543784.15.9.1091. PMID 16916275.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Gennari L, Merlotti D, Nuti R (2010). "Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene". Clin Interv Aging. 5: 19–29. PMC 2817938 Freely accessible. PMID 20169039.
- ↑ Cummings SR, Ensrud K, Delmas PD, LaCroix AZ, Vukicevic S, Reid DM, Goldstein S, Sriram U, Lee A, Thompson J, Armstrong RA, Thompson DD, Powles R, Zanchetta J, Kendler D, Neven P, Eastell R, the PEARL Study Investigators (2010). "Lasofoxifene in Postmenopausal Women with Osteoporosis". N Engl J Med. 362 (8): 686–696. doi:10.1056/NEJMoa0808692. PMID 20181970.
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