U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C28H31NO2
Molecular Weight 413.5512
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LASOFOXIFENE

SMILES

OC1=CC=C2[C@H]([C@H](CCC2=C1)C3=CC=CC=C3)C4=CC=C(OCCN5CCCC5)C=C4

InChI

InChIKey=GXESHMAMLJKROZ-IAPPQJPRSA-N
InChI=1S/C28H31NO2/c30-24-11-15-27-23(20-24)10-14-26(21-6-2-1-3-7-21)28(27)22-8-12-25(13-9-22)31-19-18-29-16-4-5-17-29/h1-3,6-9,11-13,15,20,26,28,30H,4-5,10,14,16-19H2/t26-,28+/m1/s1

HIDE SMILES / InChI

Molecular Formula C28H31NO2
Molecular Weight 413.5512
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Lasofoxifene is an active component of Fablyn. Fablyn is used for the treatment of osteoporosis in postmenopausal women. Lasofoxifene is a nonsteroidal selective estrogen receptor modulator. Lasofoxifene has no effect on CYP2E1- or CYP2D6-mediated drug metabolism and should not affect drugs metabolized by other cytochrome P450 isoenzymes. Common adverse reactions considered to be related to Fablyn therapy were muscle spasms, hot flush and vaginal discharge. Lasofoxifene approved in the EU in 2009 is now withdrawn from use in the European Union.

Originator

Curator's Comment: # Ligand Pharmaceuticals; Pfizer

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.218 μg/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
0.09 ng/mL
0.01 mg 1 times / day steady-state, oral
dose: 0.01 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
0.25 ng/mL
0.03 mg 1 times / day steady-state, oral
dose: 0.03 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
0.74 ng/mL
0.1 mg 1 times / day steady-state, oral
dose: 0.1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
2.08 ng/mL
0.3 mg 1 times / day steady-state, oral
dose: 0.3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
6.43 ng/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
0.169 ng/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.173 ng/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.214 ng/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.25 ng/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
0.5 ng/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
0.1 ng/mL
0.1 mg single, oral
dose: 0.1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
0.24 ng/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
0.44 ng/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
0.09 ng/mL
0.1 mg single, oral
dose: 0.1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
52.7 ng × h/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
1.67 ng × h/mL
0.01 mg 1 times / day steady-state, oral
dose: 0.01 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
5.14 ng × h/mL
0.03 mg 1 times / day steady-state, oral
dose: 0.03 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
15.7 ng × h/mL
0.1 mg 1 times / day steady-state, oral
dose: 0.1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
43.2 ng × h/mL
0.3 mg 1 times / day steady-state, oral
dose: 0.3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
137 ng × h/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
38.1 ng × h/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
37.1 ng × h/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
52.6 ng × h/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FASTED
45.8 ng × h/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
85.5 ng × h/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
14.5 ng × h/mL
0.1 mg single, oral
dose: 0.1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
45.6 ng × h/mL
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
77.5 ng × h/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
14.5 ng × h/mL
0.1 mg single, oral
dose: 0.1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
196 h
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
182 h
0.03 mg 1 times / day steady-state, oral
dose: 0.03 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
171 h
0.1 mg 1 times / day steady-state, oral
dose: 0.1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
147 h
0.3 mg 1 times / day steady-state, oral
dose: 0.3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
134 h
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
193 h
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
195 h
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
252 h
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FASTED
151.1 h
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
134.8 h
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
164.3 h
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
146.3 h
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.508%
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.717%
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.433%
0.25 mg single, oral
dose: 0.25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASOFOXIFENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Other AEs: Hot flushes, Leg cramps...
Other AEs:
Hot flushes (18 patients)
Leg cramps (15 patients)
Leukorrhea (7 patients)
Vaginal bleeding (2 patients)
Fractures (5 patients)
Leg cramps (7%)
Leg cramps (2%)
Sources:
0.25 mg single, oral
Studied dose
Dose: 0.25 mg
Route: oral
Route: single
Dose: 0.25 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Other AEs: somnolence, Headache...
Other AEs:
somnolence (2 patients)
Headache (1 pt)
nausea (1 pt)
Sources:
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Other AEs: Breast pain, Hot flushes...
Other AEs:
Breast pain (4 patients)
Hot flushes (24 patients)
Leg cramps (20 patients)
Leukorrhea (12 patients)
Vaginal bleeding (3 patients)
Fractures (3 patients)
hot flushes (4%)
Sources:
20 mg single, oral
Studied dose
Dose: 20 mg
Route: oral
Route: single
Dose: 20 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M
Food Status: UNKNOWN
Sources:
AEs

AEs

AESignificanceDosePopulation
Leg cramps 15 patients
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Hot flushes 18 patients
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Vaginal bleeding 2 patients
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Leg cramps 2%
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Fractures 5 patients
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Leukorrhea 7 patients
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Leg cramps 7%
1 mg 1 times / day steady-state, oral
Highest studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 1 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Headache 1 pt
0.25 mg single, oral
Studied dose
Dose: 0.25 mg
Route: oral
Route: single
Dose: 0.25 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
nausea 1 pt
0.25 mg single, oral
Studied dose
Dose: 0.25 mg
Route: oral
Route: single
Dose: 0.25 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
somnolence 2 patients
0.25 mg single, oral
Studied dose
Dose: 0.25 mg
Route: oral
Route: single
Dose: 0.25 mg
Sources:
healthy, ADULT
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Leukorrhea 12 patients
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Leg cramps 20 patients
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Hot flushes 24 patients
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Fractures 3 patients
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Vaginal bleeding 3 patients
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
Breast pain 4 patients
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
hot flushes 4%
0.25 mg 1 times / day steady-state, oral
Studied dose
Dose: 0.25 mg, 1 times / day
Route: oral
Route: steady-state
Dose: 0.25 mg, 1 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: F
Food Status: UNKNOWN
Sources:
PubMed

PubMed

TitleDatePubMed
SERMs: current status and future trends.
2002 Jul
Target specificity of selective estrogen receptor modulators within human endometrial cancer cells.
2003 Jul
Long-term treatment of lasofoxifene preserves bone mass and bone strength and does not adversely affect the uterus in ovariectomized rats.
2004 Apr
Embryo/fetal toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in rats and rabbits.
2004 Jun
Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in female rats.
2004 Jun
A new selective estrogen receptor modulator, CHF 4227.01, preserves bone mass and microarchitecture in ovariectomized rats.
2005 Dec
Estrogen receptors as therapeutic targets in breast cancer.
2006
Emerging selective estrogen receptor modulators: special focus on effects on coronary heart disease in postmenopausal women.
2006
[Next generation selective estrogen receptor modulators].
2006 Jan
Effects of steady-state lasofoxifene on CYP2D6- and CYP2E1-mediated metabolism.
2006 Jan
Lasofoxifene enhances vaginal mucus formation without causing hypertrophy and increases estrogen receptor beta and androgen receptor in rats.
2006 Jul-Aug
Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis.
2006 Jun
Effects of lasofoxifene on the pharmacokinetics and pharmacodynamics of single-dose warfarin.
2006 Jun
Clinical pharmacology of lasofoxifene in Japanese and white postmenopausal women.
2006 Jun
Update on bazedoxifene: a novel selective estrogen receptor modulator.
2007
Effects of three cytochrome P450 inhibitors, ketoconazole, fluconazole, and paroxetine, on the pharmacokinetics of lasofoxifene.
2007 Jan
Bazedoxifene: bazedoxifene acetate, TSE 424, TSE-424, WAY 140424.
2008
Effects of lasofoxifene on the uterus, vagina, and breast in ovariectomized cynomolgus monkeys (Macaca fascicularis).
2008 Aug
Bazedoxifene for the prevention of postmenopausal osteoporosis.
2008 Dec
Disposition of lasofoxifene, a next-generation selective estrogen receptor modulator, in healthy male subjects.
2008 Jul
Hormone-dependent aging problems in women.
2008 Jun 30
Metabolism, distribution, and excretion of a next generation selective estrogen receptor modulator, lasofoxifene, in rats and monkeys.
2008 Sep
Lasofoxifene for the prevention and treatment of postmenopausal osteoporosis.
2009
Progress in osteoporosis and fracture prevention: focus on postmenopausal women.
2009
Clinical issues regarding cardiovascular disease and selective estrogen receptor modulators in postmenopausal women.
2009
Docking study of triphenylphosphonium cations as estrogen receptor alpha modulators.
2009
Treatment of osteoporosis with annual iv zoledronic acid: effects on hip fracture.
2009 Apr
Thresholds for therapies: highlights of the St Gallen International Expert Consensus on the primary therapy of early breast cancer 2009.
2009 Aug
Lasofoxifene: new drug. Osteoporosis: no better than raloxifene.
2009 Dec
A randomised, double-blinded, placebo-controlled, trial to determine the individual response in bone turnover markers to lasofoxifene therapy.
2009 Dec
Recent advances in managing osteoporosis.
2009 Dec 15
New selective estrogen and androgen receptor modulators.
2009 Jul
Designing the ideal selective estrogen receptor modulator--an achievable goal?
2009 May-Jun
Current and emerging pharmacologic therapies for the management of postmenopausal osteoporosis.
2009 Oct
Lasofoxifene, a new selective estrogen receptor modulator for the treatment of osteoporosis and vaginal atrophy.
2009 Sep
Modulators of androgen and estrogen receptor activity.
2010
An innovative method to classify SERMs based on the dynamics of estrogen receptor transcriptional activity in living animals.
2010 Apr
Long-term safety and efficacy of raloxifene in the prevention and treatment of postmenopausal osteoporosis: an update.
2010 Aug 9
Lasofoxifene in osteoporosis and its place in therapy.
2010 Dec
Another selective estrogen-receptor modulator for osteoporosis.
2010 Feb 25
Lasofoxifene in postmenopausal women with osteoporosis.
2010 Feb 25
Gene expression profiling studies of three SERMs and their conjugated estrogen combinations in human breast cancer cells: insights into the unique antagonistic effects of bazedoxifene on conjugated estrogens.
2010 Jan
SERMs in the prevention and treatment of postmenopausal osteoporosis: an update.
2010 Mar
Endometrial safety: a key hurdle for selective estrogen receptor modulators in development.
2010 May-Jun
Third-generation SERMs may face uphill battle.
2010 Nov 17
Tipping the balance for the primary prevention of breast cancer.
2010 Nov 17
Breast cancer incidence in the randomized PEARL trial of lasofoxifene in postmenopausal osteoporotic women.
2010 Nov 17
Selective estrogen receptor modulator (SERM) lasofoxifene forms reactive quinones similar to estradiol.
2012 Jul 16
Patents

Sample Use Guides

500 ug daily. The tablet may be taken any time of day without regard to food and beverage intake.
Route of Administration: Oral
In Vitro Use Guide
Lasofoxifene was determined to be an extremely potent antagonist to the growth of estrogen-dependent MCF-7 breast cancer cell line (IC50 =0.05 nM).
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:17:56 GMT 2025
Edited
by admin
on Mon Mar 31 18:17:56 GMT 2025
Record UNII
337G83N988
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LASOFOXIFENE
EMA EPAR   INN   MART.   MI   WHO-DD  
INN  
Official Name English
LASOFOXIFENE [EMA EPAR]
Preferred Name English
Lasofoxifene [WHO-DD]
Common Name English
LASOFOXIFENE [MI]
Common Name English
LASOFOXIFENE [MART.]
Common Name English
(-)-CIS-5,6,7,8-TETRAHYDRO-6-PHENYL-5-(P-(2-(1-PYRROLIDINYL)ETHOXY)PHENYL)-2-NAPHTHOL
Common Name English
lasofoxifene [INN]
Common Name English
Classification Tree Code System Code
WHO-VATC QG03XC03
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
NCI_THESAURUS C1821
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
WHO-ATC G03XC03
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
Code System Code Type Description
CHEBI
135938
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
SMS_ID
100000092767
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
PUBCHEM
216416
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
DRUG CENTRAL
4308
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
EPA CompTox
DTXSID50171037
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
DRUG BANK
DB06202
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
CAS
180916-16-9
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
NCI_THESAURUS
C80679
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
FDA UNII
337G83N988
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
MERCK INDEX
m6700
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY Merck Index
WIKIPEDIA
Lasofoxifene
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
EVMPD
SUB27754
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
INN
7875
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
ChEMBL
CHEMBL328190
Created by admin on Mon Mar 31 18:17:56 GMT 2025 , Edited by admin on Mon Mar 31 18:17:56 GMT 2025
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
FECAL
METABOLIC ENZYME -> SUBSTRATE
TARGET -> AGONIST
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
ACTIVE MOIETY