LASOFOXIFENE

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 Search

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

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000977/WC500020092.pdf | https://www.ncbi.nlm.nih.gov/pubmed/16916275 | https://www.ncbi.nlm.nih.gov/pubmed/16368922

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 Lasofoxifene approved in the EU in 2009 is now withdrawn from use in the European Union.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

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Estrogen receptor alpha 134 Target ID: CHEMBL206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16916275 \| http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000977/WC500020092.pdf	Modulator 846		15.0 nM [IC50]
Estrogen receptor beta 113 Target ID: CHEMBL242 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16916275 \| http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000977/WC500020092.pdf	Modulator 846

Conditions

Condition	Modality	Highest Phase	Product
Osteoporosis in postmenopausal women 6 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000977/WC500020092.pdf	Primary	Withdrawn	Fablyn Approved Use Treatment of osteoporosis in postmenopausal women at increased risk of fracture Launch Date 2009
Advanced breast cancer 6 Sources: http://adisinsight.springer.com/trials/700282284	Primary	Phase III 665	Unknown Approved Use Unknown
Female sexual dysfunction 5 Sources: http://adisinsight.springer.com/drugs/800007522	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	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	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

T_1/2

Value	Dose	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

F_unbound

Value	Dose	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: https://pubmed.ncbi.nlm.nih.gov/16735934/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/16735934/	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: https://pubmed.ncbi.nlm.nih.gov/16735934/
0.25 mg single, oral Studied dose Dose: 0.25 mg Route: oral Route: single Dose: 0.25 mg Sources: https://pubmed.ncbi.nlm.nih.gov/16397281/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/16397281/	Other AEs: somnolence, Headache... Other AEs: somnolence (2 patients) Headache (1 pt) nausea (1 pt) Sources: https://pubmed.ncbi.nlm.nih.gov/16397281/
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: https://pubmed.ncbi.nlm.nih.gov/16735934/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/16735934/	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: https://pubmed.ncbi.nlm.nih.gov/16735934/
20 mg single, oral Studied dose Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: https://pubmed.ncbi.nlm.nih.gov/18372400/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18372400/	Sources: https://pubmed.ncbi.nlm.nih.gov/18372400/

AEs

PubMed

Title	Date	PubMed
SERMs: current status and future trends.	2002 Jul	12098608
Target specificity of selective estrogen receptor modulators within human endometrial cancer cells.	2003 Jul	12943742
Long-term treatment of lasofoxifene preserves bone mass and bone strength and does not adversely affect the uterus in ovariectomized rats.	2004 Apr	14726439
Embryo/fetal toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in rats and rabbits.	2004 Jun	15282737
Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in female rats.	2004 Jun	15282736
A new selective estrogen receptor modulator, CHF 4227.01, preserves bone mass and microarchitecture in ovariectomized rats.	2005 Dec	16294271
Estrogen receptors as therapeutic targets in breast cancer.	2006	16515478
Emerging selective estrogen receptor modulators: special focus on effects on coronary heart disease in postmenopausal women.	2006	16451093
[Next generation selective estrogen receptor modulators].	2006 Jan	16397365
Effects of steady-state lasofoxifene on CYP2D6- and CYP2E1-mediated metabolism.	2006 Jan	16368922
Lasofoxifene enhances vaginal mucus formation without causing hypertrophy and increases estrogen receptor beta and androgen receptor in rats.	2006 Jul-Aug	16837883
Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis.	2006 Jun	16845439
Effects of lasofoxifene on the pharmacokinetics and pharmacodynamics of single-dose warfarin.	2006 Jun	16722839
Clinical pharmacology of lasofoxifene in Japanese and white postmenopausal women.	2006 Jun	16707415
Update on bazedoxifene: a novel selective estrogen receptor modulator.	2007	18044180
Effects of three cytochrome P450 inhibitors, ketoconazole, fluconazole, and paroxetine, on the pharmacokinetics of lasofoxifene.	2007 Jan	16822276
Bazedoxifene: bazedoxifene acetate, TSE 424, TSE-424, WAY 140424.	2008	18457472
Effects of lasofoxifene on the uterus, vagina, and breast in ovariectomized cynomolgus monkeys (Macaca fascicularis).	2008 Aug	18501325
Bazedoxifene for the prevention of postmenopausal osteoporosis.	2008 Dec	19337430
Disposition of lasofoxifene, a next-generation selective estrogen receptor modulator, in healthy male subjects.	2008 Jul	18372400
Hormone-dependent aging problems in women.	2008 Jun 30	18581581
Metabolism, distribution, and excretion of a next generation selective estrogen receptor modulator, lasofoxifene, in rats and monkeys.	2008 Sep	18515329
Lasofoxifene for the prevention and treatment of postmenopausal osteoporosis.	2009	19898646
Progress in osteoporosis and fracture prevention: focus on postmenopausal women.	2009	19849819
Clinical issues regarding cardiovascular disease and selective estrogen receptor modulators in postmenopausal women.	2009	19811253
Docking study of triphenylphosphonium cations as estrogen receptor alpha modulators.	2009	19293997
Treatment of osteoporosis with annual iv zoledronic acid: effects on hip fracture.	2009 Apr	19536314
Thresholds for therapies: highlights of the St Gallen International Expert Consensus on the primary therapy of early breast cancer 2009.	2009 Aug	19535820
Lasofoxifene: new drug. Osteoporosis: no better than raloxifene.	2009 Dec	20020572
A randomised, double-blinded, placebo-controlled, trial to determine the individual response in bone turnover markers to lasofoxifene therapy.	2009 Dec	19665601
Recent advances in managing osteoporosis.	2009 Dec 15	20948681
New selective estrogen and androgen receptor modulators.	2009 Jul	19412100
Designing the ideal selective estrogen receptor modulator--an achievable goal?	2009 May-Jun	19182697
Current and emerging pharmacologic therapies for the management of postmenopausal osteoporosis.	2009 Oct	19857095
Lasofoxifene, a new selective estrogen receptor modulator for the treatment of osteoporosis and vaginal atrophy.	2009 Sep	19640205
Modulators of androgen and estrogen receptor activity.	2010	21395502
An innovative method to classify SERMs based on the dynamics of estrogen receptor transcriptional activity in living animals.	2010 Apr	20197311
Long-term safety and efficacy of raloxifene in the prevention and treatment of postmenopausal osteoporosis: an update.	2010 Aug 9	21072271
Lasofoxifene in osteoporosis and its place in therapy.	2010 Dec	21080249
Another selective estrogen-receptor modulator for osteoporosis.	2010 Feb 25	20181977
Lasofoxifene in postmenopausal women with osteoporosis.	2010 Feb 25	20181970
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	19914376
SERMs in the prevention and treatment of postmenopausal osteoporosis: an update.	2010 Mar	20485909
Endometrial safety: a key hurdle for selective estrogen receptor modulators in development.	2010 May-Jun	20107426
Third-generation SERMs may face uphill battle.	2010 Nov 17	21060064
Tipping the balance for the primary prevention of breast cancer.	2010 Nov 17	21051657
Breast cancer incidence in the randomized PEARL trial of lasofoxifene in postmenopausal osteoporotic women.	2010 Nov 17	21051656
Selective estrogen receptor modulator (SERM) lasofoxifene forms reactive quinones similar to estradiol.	2012 Jul 16	22642258

Patents

Sample Use Guides

In Vivo Use Guide

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

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Name

Type

Language

LASOFOXIFENE

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