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
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
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 Lasofoxifene approved in the EU in 2009 is now withdrawn from use in the European Union.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
Sources: http://adisinsight.springer.com/drugs/800007522
Curator's Comment: # Ligand Pharmaceuticals; Pfizer
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
15.0 nM [IC50] | |||
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Fablyn Approved UseTreatment of osteoporosis in postmenopausal women at increased risk of fracture Launch Date2009 |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.218 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16822276/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
52.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16822276/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
196 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16822276/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397284/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16707415/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.508% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16397281/ |
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
Dose | Population | Adverse 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) Sources: Leg cramps (15 patients) Leukorrhea (7 patients) Vaginal bleeding (2 patients) Fractures (5 patients) Leg cramps (7%) Leg cramps (2%) |
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) Sources: Headache (1 pt) nausea (1 pt) |
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) Sources: Hot flushes (24 patients) Leg cramps (20 patients) Leukorrhea (12 patients) Vaginal bleeding (3 patients) Fractures (3 patients) hot flushes (4%) |
20 mg single, oral Studied dose |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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
Title | Date | PubMed |
---|---|---|
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 |
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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 |
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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 |
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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 |
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Lasofoxifene in osteoporosis and its place in therapy. | 2010 Dec |
|
Another selective estrogen-receptor modulator for osteoporosis. | 2010 Feb 25 |
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Lasofoxifene in postmenopausal women with osteoporosis. | 2010 Feb 25 |
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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 |
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SERMs in the prevention and treatment of postmenopausal osteoporosis: an update. | 2010 Mar |
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Endometrial safety: a key hurdle for selective estrogen receptor modulators in development. | 2010 May-Jun |
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Third-generation SERMs may face uphill battle. | 2010 Nov 17 |
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Tipping the balance for the primary prevention of breast cancer. | 2010 Nov 17 |
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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 |
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9685230
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
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Record UNII |
337G83N988
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WHO-VATC |
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NCI_THESAURUS |
C1821
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WHO-ATC |
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m6700
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Lasofoxifene
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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FECAL
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TARGET -> AGONIST | |||
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URINE
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLITE -> PARENT |
FECAL
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METABOLITE -> PARENT |
FECAL
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
PLASMA
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ACTIVE MOIETY |