Lasofoxifene Pharmacology and History

Lasofoxifene selectively binds to both ERα and ERβ with top affinity.Its IC50 for ERα (1.5 nM) is agnate to that of estradiol (4.8 nM) and is at atomic 10-fold college than those of tamoxifen and raloxifene.Raloxifene aswell has appreciably bigger articulate bioavailability about to tamoxifen and raloxifene, and this may aswell be complex in its greater potency.

In September 2005, Pfizer accustomed a non-approvable letter from the U.S. Food and Drug Administration apropos lasofoxifene (trade name Oporia), a careful estrogen receptor modulator for the blockage of osteoporosis.

On January 2008, Ligand Pharmaceuticals, through its business partner, Pfizer, submitted a New Drug Application for lasofoxifene, which is accepted to be marketed beneath the tradename Fablyn. Lasofoxifene was accustomed in the EU beneath the cast name Fablyn by the EMEA in March 2009.


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