- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | LY-139481; RAL; Raloxifene Hcl; Raloxifene Hydrochloride; Raloxifeno [Spanish]; Raloxifenum [Latin]; raloxifene |
|---|---|
| Trade Names: | Evista; Keoxifene |
| PharmGKB Accession Id: | PA451221 |
Description
A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue. PubChem (source: Drug Bank)
Indication
For the prevention of osteoporosis in post-menopausal women (source: Drug Bank)
ATC Therapeutic Category
- G03XC:Selective estrogen receptor modulators
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
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. Raloxifene also antagonizes the effects of estrogen on mammary tissue and blocks uterotrophic responses to estrogen. (source: Drug Bank)
Pharmacology
Raloxifene, a selective estrogen receptor modulator (SERM) of the benzothiophene class, is similar to tamoxifen in that it produces estrogen-like effects on bone and lipid metabolism, while antagonizing the effects of estrogen on mammary tissue. Raloxifene decreases bone resorption, increases bone mineral density (BMD) and decreases incidence of fractures. Raloxifene is used in the prevention of postmenopausal osteoporosis and breast cancer. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic, raloxifene undergoes extensive first-pass metabolism to the glucuronide conjugates: raloxifene-4'-glucuronide, raloxifene-6-glucuronide, and raloxifene-6, 4'-diglucuronide. No other metabolites have been detected, providing strong evidence that raloxifene is not metabolized by cytochrome P450 pathways (source: Drug Bank)
Protein Binding
95% (source: Drug Bank)
Absorption
Approximately 60% of an oral dose is absorbed, but presystemic glucuronide conjugation is extensive. Absolute bioavailability of raloxifene is 2.0% (source: Drug Bank)
Isomeric SMILES Code:
c1cc(ccc1c2c(c3ccc(cc3s2)O)C(=O)c4ccc(cc4)OCCN5CCCCC5)O (source: Drug Bank)
Curated Annotations (
)
-
rs1544411
at chr7:10786072
This variant is associated with alendronate response in Caucasian (Italian) postmenopausal women, with bb genotype associated with lower increase in bone mineral density (BMD) after bisphosphonate treatments. BsmI VDR genotypes influenced the efficacy of antiresorptive drugs particularly when used in combination.- Variant Name:
- VDR: BsmI
- Related Drugs:
- alendronate, calcium, raloxifene
- Related Diseases:
- Osteoporosis, Osteoporosis, Postmenopausal
- Evidence:
-
PMID:15739035
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
HTR1D |
|
Publications |
|
NR1I2 |
|
Publications |
|
|
SULT1E1 |
|
Publications |
|
|
VDR |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ESR1 |
|
(source: Drug Bank) |
| ESR2 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
warfarin |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| cholestyramine |
|
The resin decreases the effect of raloxifene (source: Drug Bank) |
| clomifene |
|
Association not recommended (source: Drug Bank) |
| colestipol |
|
The resin decreases the effect of raloxifene (source: Drug Bank) |
| diethylstilbestrol |
|
Association not recommended (source: Drug Bank) |
| estradiol |
|
Association not recommended (source: Drug Bank) |
| ethinyl estradiol |
|
Association not recommended (source: Drug Bank) |
| levothyroxine |
|
Raloxifene decreases absorption of levothyroxine (source: Drug Bank) |
| mestranol |
|
Association not recommended (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Osteoporosis |
|
Publications, Variants |
|
|
Osteoporosis, Postmenopausal |
|
Publications, Variants |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.