General
Preferred name
OSPEMIFENE
Synonyms
FC-1271a ()
Osphena ()
Tore iii ()
Ospemifeno ()
Senshio ()
(deaminohydroxy) toremifene ()
FC-1271 ()
Ospemifene-d4 ()
P&D ID
PD009346
CAS
128607-22-7
Tags
available
drug
Approved by
EMA
FDA
First approval
2013
Drug indication
reproductive system disease
Postmenopausal vaginal atrophy
Dyspareunia
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
ABSORPTION When a single oral dose of ospemifene 60 mg is given to postmenopausal women under fasted conditions, the pharmacokinetic parameters are as follows:; Tmax = 2 hours (range of 1 - 8 hours);; Cmax = 533 ng/mL;; AUC (0-inf) = 4165 ng•hr/mL. ; When the same aforementioned dose is given to postmenopausal women under fed conditions, the pharmacokinetic parameters are as follows:; Tmax = 2.5 hours (1 - 6 hours); ; Cmax = 1198 ng/mL;; AUC (0-inf) = 7521 ng•hr/mL. ; Accumulation occurs following repeated doses. ; Time to steady state = 9 days. ; Although the bioavailability of ospemifene has not been formally evaluated, it is expected to have a low bioavailability because of its lipophilic nature.
DESCRIPTION Ospemifene is a selective estrogen receptor modulator (SERM) . Like other SERMs it has mixed agonist/antagonist activities that are tissue-dependent. (GtoPdb)
DESCRIPTION Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor ¦Á (ER¦Á) and ER¦Â, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer[1][2][3][4][5][6].
Cell lines
1
Organisms
2
Compound Sets
16
AdooQ Bioactive Compound Library
A14261
Cayman Chemical Bioactives
23755
33465
ChEMBL Approved Drugs
CHEMBL2105395
ChEMBL Drugs
CHEMBL2105395
Drug Repurposing Hub
DrugBank
DB04938
DrugBank Approved Drugs
DB04938
DrugCentral
4749
DrugCentral Approved Drugs
4749
DrugMAP
DMC4GEI
DrugMAP Approved Drugs
DMC4GEI
Guide to Pharmacology
7349
MedChem Express Bioactive Compound Library
HY-B0723
NCATS Inxight Approved Drugs
B0P231ILBK
ReFrame library
Selleckchem Bioactive Compound Library
ospemifene
External IDs
32
Properties
(calculated by RDKit )
Molecular Weight
378.14
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
3
Aromatic Ring Count
3
cLogP
5.65
TPSA
29.46
Fraction CSP3
0.17
Chiral centers
0.0
Largest ring
6.0
QED
0.41
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Disease Area
obstetrics/gynecology, endocrinology
Indication
vaginal atrophy, dyspareunia, menopause
Target
ESR1, ESR2
Caspase
Estrogen Receptor/ERR
Estrogen/progestogen Receptor
MOA
Selective Estrogen Receptor Modulator (SERM)
Pathway
Apoptosis
Vitamin D Related/Nuclear Receptor
Source data