U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C28H27NO4S
Molecular Weight 473.5854
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RALOXIFENE

SMILES

C1CCN(CC1)CCOc2ccc(cc2)C(=O)c3c4ccc(cc4sc3-c5ccc(cc5)O)O

InChI

InChIKey=GZUITABIAKMVPG-UHFFFAOYSA-N
InChI=1S/C28H27NO4S/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29/h4-13,18,30-31H,1-3,14-17H2

HIDE SMILES / InChI

Molecular Formula C28H27NO4S
Molecular Weight 473.5854
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: https://www.drugbank.ca/drugs/DB00481 | https://www.drugs.com/pro/raloxifene-hydrochloride-tablets.html | https://www.ncbi.nlm.nih.gov/pubmed/11836973 | http://reference.medscape.com/drug/evista-raloxifene-342794

Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. Raloxifene binds to estrogen receptors, resulting in differential expression of multiple estrogen-regulated genes in different tissues. Raloxifene produces estrogen-like effects on bone, reducing resorption of bone and increasing bone mineral density in postmenopausal women, thus slowing the rate of bone loss. The maintenance of bone mass by raloxifene and estrogens is, in part, through the regulation of the gene-encoding transforming growth factor-β3 (TGF-β3), which is a bone matrix protein with antiosteoclastic properties. Raloxifene activates TGF-β3 through pathways that are estrogen receptor-mediated but involve DNA sequences distinct from the estrogen response element. The drug also binds to the estrogen receptor and acts as an estrogen agonist in preosteoclastic cells, which results in the inhibition of their proliferative capacity. This inhibition is thought to contribute to the drug's effect on bone resorption. Other mechanisms include the suppression of the activity of the bone-resorbing cytokine interleukin-6 promoter activity. Raloxifene also antagonizes the effects of estrogen on mammary tissue and blocks uterotrophic responses to estrogen. By competing with estrogens for the estrogen receptors in reproductive tissue, raloxifene prevents the transcriptional activation of genes containing the estrogen response element. As well, raloxifene inhibits the estradiol-dependent proliferation of MCF-7 human mammary tumor cells in vitro. The mechanism of action of raloxifene has not been fully determined, but evidence suggests that the drug's tissue-specific estrogen agonist or antagonist activity is related to the structural differences between the raloxifene-estrogen receptor complex (specifically the surface topography of AF-2) and the estrogen-estrogen receptor complex. Also, the existence of at least 2 estrogen receptors (ERα, ERβ) may contribute to the tissue specificity of raloxifene. Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. It is also used for reduction of risk and treatment of invasive breast cancer, and it also reduces breast density. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Common adverse events considered to be drug-related were hot flashes and leg cramps.

CNS Activity

Curator's Comment:: The penetration of raloxifene in blood–brain barrier protected regions is low and may render the detection of any brain effect difficult at the dosage currently used in practice

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
EVISTA

Approved Use

EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2)

Launch Date

881625600000
Primary
EVISTA

Approved Use

EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2)

Launch Date

881625600000
Primary
EVISTA

Approved Use

EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2)

Launch Date

881625600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.5 ng/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RALOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
27.2 ng × h/mL
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RALOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
27.7 h
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RALOXIFENE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Other AEs: Ataxia, Dizziness...
Other AEs:
Ataxia
Dizziness
Vomiting
Rash
Diarrhea
Tremor
Flushing
Alkaline phosphatase increased
Sources:
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, Mean age 53.2 years
Health Status: healthy
Age Group: Mean age 53.2 years
Sex: F
Sources:
Other AEs: Hot flashes...
Other AEs:
Hot flashes
Sources:
60 mg 1 times / day multiple, oral
Recommended
unhealthy, Mean age 68 years
Other AEs: Deep vein thrombosis, Pulmonary embolism...
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Disc. AE: Vomiting, Nausea...
AEs leading to
discontinuation/dose reduction:
Vomiting (0.3%)
Nausea (0.6%)
Oedema (0.6%)
Muscle spasms (0.7%)
Muscle related signs and symptoms NEC (1.6%)
Headache (0.3%)
Paralysis (0.1%)
Hot flush (1.4%)
Peripheral vascular disorder (1.6%)
Sources:
180 mg multiple, oral
Studied dose
Dose: 180 mg
Route: oral
Route: multiple
Dose: 180 mg
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
Other AEs: Leg cramps, Dizziness...
1.5 g 1 times / day single, oral
Studied dose
Dose: 1.5 g, 1 times / day
Route: oral
Route: single
Dose: 1.5 g, 1 times / day
Sources:
unhealthy
AEs

AEs

AESignificanceDosePopulation
Alkaline phosphatase increased
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Ataxia
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Diarrhea
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Dizziness
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Flushing
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Rash
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Tremor
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Vomiting
180 mg 1 times / day single, oral
Studied dose
Dose: 180 mg, 1 times / day
Route: oral
Route: single
Dose: 180 mg, 1 times / day
Sources:
healthy, 18 months
Health Status: healthy
Age Group: 18 months
Sources:
Hot flashes
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
healthy, Mean age 53.2 years
Health Status: healthy
Age Group: Mean age 53.2 years
Sex: F
Sources:
Deep vein thrombosis
60 mg 1 times / day multiple, oral
Recommended
unhealthy, Mean age 68 years
Pulmonary embolism
60 mg 1 times / day multiple, oral
Recommended
unhealthy, Mean age 68 years
Stroke
60 mg 1 times / day multiple, oral
Recommended
unhealthy, Mean age 68 years
Paralysis 0.1%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Headache 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Vomiting 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Nausea 0.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Oedema 0.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Muscle spasms 0.7%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Hot flush 1.4%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Muscle related signs and symptoms NEC 1.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Peripheral vascular disorder 1.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
unhealthy, Mean age 68 years
Dizziness
180 mg multiple, oral
Studied dose
Dose: 180 mg
Route: oral
Route: multiple
Dose: 180 mg
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
Leg cramps
180 mg multiple, oral
Studied dose
Dose: 180 mg
Route: oral
Route: multiple
Dose: 180 mg
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [IC50 2.4 uM]
yes [IC50 3.7 uM]
yes [IC50 4.8 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
yes [Km 0.33 uM]
yes
yes
yes
yes
yes
yes
yes
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Raloxifene and prevention of vertebral fracture (cont'd): mainly when oestrogen is contraindicated.
2000 Dec
Initiation of osteoporosis treatment after bone mineral density testing.
2001
Alendronate: an update of its use in osteoporosis.
2001
Chemoprevention of breast cancer with fenretinide.
2001
In silico discovery of novel retinoic acid receptor agonist structures.
2001
[Modern approaches to hormone therapy of breast cancer as a reflection of pathogenesis of the disease].
2001
Update on endocrine aspects of breast cancer: report from the 23rd San Antonio Breast Cancer Symposium, San Antonio, Texas, USA, 6-9 December 2000.
2001
[An alternative to postmenopausal Hormone Replacement Therapy? Selective Estrogens Receptors Modulators (SERMs)].
2001 Apr
Can estrogen or selective estrogen-receptor modulators preserve cognitive function in elderly women?
2001 Apr 19
Cognitive function in postmenopausal women treated with raloxifene.
2001 Apr 19
Raloxifene fails to slow cognitive decline in older women.
2001 Apr 21
Raloxifene for breast cancer prevention.
2001 Apr 25
[SERM--selective estrogen receptor modulators].
2001 Apr 9
Bone builders: preventing and treating osteoporosis.
2001 Aug
Familiar drugs may prevent cancer.
2001 Aug
Estrogen-like activity of tamoxifen and raloxifene on NMDA receptor binding and expression of its subunits in rat brain.
2001 Aug
Paradoxical interactions among estrogen receptors, estrogens and SERMS: mutual annihilation and synergy.
2001 Jan-Mar
Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351.
2001 Jan-Mar
Effects of raloxifene treatment on uterine leiomyomas in postmenopausal women.
2001 Jul
Raloxifene effect on frequency of surgery for pelvic floor relaxation.
2001 Jul
Gonadotropins at menopause: the influence of obesity, insulin resistance, and estrogens.
2001 Jul
Rheumatology: 15. Osteoporosis.
2001 Jul 10
Effects of raloxifene and hormone replacement therapy on markers of serum atherogenicity in healthy postmenopausal women.
2001 Jul 25
Tamoxifen and contralateral breast cancer: the other side.
2001 Jul 4
Estradiol regulates monocyte chemotactic protein-1 in human coronary artery smooth muscle cells: a mechanism for its antiatherogenic effect.
2001 Jul-Aug
Tamoxifen, screening and new oestrogen receptor modulators.
2001 Jun
A non-calcemic analog of 1 alpha,25 dihydroxy vitamin D(3) (JKF) upregulates the induction of creatine kinase B by 17 beta estradiol in osteoblast-like ROS 17/2.8 cells and in rat diaphysis.
2001 Jun
Estrogenic and antiestrogenic effects of raloxifene on collagen metabolism in breast cancer MCF-7 cells.
2001 Jun
Medication update.
2001 Jun
NIH Consensus Development Panel on Osteoporosis Prevention, Diagnosis, and Therapy, March 7-29, 2000: highlights of the conference.
2001 Jun
Tibolone and its effects on bone: a review.
2001 Jun
Osteoporosis.
2001 Jun
Tamoxifen to raloxifene and beyond.
2001 Jun
Breast cancer chemoprevention: current status and future directions.
2001 Jun
Effects of the selective estrogen receptor modulator, raloxifene, on the somatotropic axis and insulin-glucose homeostasis.
2001 Jun
Effect of physicians opinion on patients' choice of treatment.
2001 Jun
Oestrogenic effects of neonatal administration of raloxifene on hypothalamic-pituitary-gonadal axis in male and female rats.
2001 Jun
Chemoprevention of breast cancer. A joint guideline from the Canadian Task Force on Preventive Health Care and the Canadian Breast Cancer Initiative's Steering Committee on Clinical Practice Guidelines for the Care and Treatment of Breast Cancer.
2001 Jun 12
Indicators of lifetime estrogen exposure: effect on breast cancer incidence and interaction with raloxifene therapy in the multiple outcomes of raloxifene evaluation study participants.
2001 Jun 15
Systemic therapy for older women with breast cancer.
2001 Mar
Selective estrogen receptor modulators. An aid in unraveling the links between estrogen and breast cancer.
2001 Mar
Anti-oestrogenic drugs and endometrial cancers.
2001 Mar 31
Differential SERM activation of the estrogen receptors (ERalpha and ERbeta) at AP-1 sites.
2001 May
Effects of postmenopausal hormone replacement therapy on lipid, lipoprotein, and apolipoprotein (a) concentrations: analysis of studies published from 1974-2000.
2001 May
Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex.
2001 May 1
Flexible alignment of small molecules.
2001 May 10
Effect of tibolone and raloxifene on the tail temperature of oestrogen-deficient rats.
2001 May 4
From adjuvant therapy to breast cancer prevention: BCPT and STAR.
2001 May-Jun
Cardiovascular effects of raloxifene hydrochloride.
2001 Spring
Regression to the mean: what does it mean? Using bone density results to monitor treatment of osteoporosis.
2001 Spring
Patents

Sample Use Guides

60 mg tablet orally once daily
Route of Administration: Oral
MCF-7 cells were obtained from the ATCC and grown in Growth Medium (GM). The cells are grown to 80% confluency and trypsinized and washed to remove phenol red, then plated at 10,000 cells/well in Starve Medium (SM). After 2 days, the medium is removed from the cells and either fresh SM or SM plus Raloxifene is added (100 mL total volume). The next day the bDNA assay is started by adding Capture Hybridization Buffer to each capture well of the bDNA plate (all solutions supplied with QuantiGene kit). Subsequently, medium is removed from the 96-well plate containing cells and then the solution of lysis buffer and oligomers (designed by ProbeDesigner 1.0 for the gene of interest) is added to the 96-well plate (100 mL/well). The cell and lysis/
Substance Class Chemical
Created
by admin
on Fri Jun 25 22:04:18 UTC 2021
Edited
by admin
on Fri Jun 25 22:04:18 UTC 2021
Record UNII
YX9162EO3I
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RALOXIFENE
HSDB   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
EVIDEN
Brand Name English
RALOXIFENE [HSDB]
Common Name English
RAXETO
Brand Name English
NSC-747974
Code English
LY-139481
Code English
RALOXIFENE [VANDF]
Common Name English
RALOXIFENE [MI]
Common Name English
RALOXIPHENE
Common Name English
RALOXIFENE [WHO-DD]
Common Name English
RALOXIFENE [INN]
Common Name English
J22.982B
Code English
KEOXIFENE
Common Name English
Classification Tree Code System Code
NDF-RT N0000175826
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
WHO-ATC G03XC01
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
LIVERTOX NBK548475
NDF-RT N0000000168
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
NCI_THESAURUS C1821
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
FDA ORPHAN DRUG 197504
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
WHO-VATC QG03XC01
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
LIVERTOX NBK548475
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
Code System Code Type Description
MESH
D020849
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
CAS
84449-90-1
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
NCI_THESAURUS
C1518
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
EPA CompTox
84449-90-1
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
PUBCHEM
5035
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
MERCK INDEX
M9485
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY Merck Index
RXCUI
72143
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY RxNorm
FDA UNII
YX9162EO3I
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
WIKIPEDIA
RALOXIFENE
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
ChEMBL
CHEMBL81
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
HSDB
7460
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
INN
5388
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
DRUG CENTRAL
2351
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
DRUG BANK
DB00481
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
IUPHAR
2820
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
EVMPD
SUB10243MIG
Created by admin on Fri Jun 25 22:04:18 UTC 2021 , Edited by admin on Fri Jun 25 22:04:18 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
Raloxifene is primarily excreted in feces, and less than 0.2% is excreted unchanged in urine.
MAJOR
FECAL
METABOLIC ENZYME -> INHIBITOR
IC50
EXCRETED UNCHANGED
URINE
TARGET -> AGONIST
METABOLIC ENZYME -> SUBSTRATE
SALT/SOLVATE -> PARENT
BINDER->LIGAND
Raloxifene and its two monoglucoronide conjugates are highly bound (.95%) to plasma proteins Raloxifene is primarily excreted in feces, and less than including bot.h albumin and a-1 acid glycoprotein
BINDING
Related Record Type Details
METABOLITE -> PARENT
MAJOR
FECAL; PLASMA; URINE
METABOLITE -> PARENT
FECAL; PLASMA; URINE
METABOLITE -> PARENT
FECAL; PLASMA; URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC Elimination
PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC ORAL ADMINISTRATION

SINGLE DOSE