Ospemifene produces significant improvements in the structure of the vagina and its pH, and significantly reduces dyspareunia, the main complaint of the women treated. Ospemifene has less carcinogenic potential than tamoxifen. Ospemifene has an agonist action on bone and reduces the growth of all breast cancer models in animal studies, providing they expressed estrogen receptor-α.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Ospemifene for the treatment of dyspareunia in postmenopausal women.
Paton DM. Drugs Today (Barc). 2014 May;50(5):357-64. PMID: 24918836.
|Related Estrogen Receptor Products|
27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.
SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.
4-Hydroxytamoxifen is a selective estrogen receptor modulator.
Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.
|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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