Rx00205 - Raloxifene


Name:
Raloxifene
Rx ID:
Rx00205
Validation Level:
Phenomic Similarity:
0.467
Reference ID:
DB00481
Primary Indications:
Breast cancer; prostate cancer
Orphan Indications:
No annotated orphan indications.
Rare Indications:
No annotated rare indications.
Common Indications:
Osteoporosis
Pathways:
Estrogen signaling pathway; Estrogen signaling pathway - Homo sapiens (human)
Drug Interactions:
Chlorotrianisene; Cholestyramine; Clomifene; Colesevelam; Colestipol; Conjugated Estrogens; Diethylstilbestrol; Estradiol; Estriol; Estropipate; ...
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Food Interactions:
Avoid alcohol. Take without regard to meals.

Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00205
Primary Indication
Secondary Indication

Visualize Chemical Properties

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Disease prevalence from Electronic Health Records

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Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
Breast cancer Osteoporosis 2992 22462 31300 17.171 0 0.0
prostate cancer Osteoporosis 334 15329 31300 2.809 1.27E-57 4.09e-54

Chemical, Pharmacological and Biological Annotations


ATC Code:
G03XC01
Brand:
Keoxifene
Categories:
Bone Density Conservation Agents; Estrogen Antagonists; Selective Estrogen Receptor Modulators; Antihypocalcemic Agents
ChEBI ID:
8772
PubChem ID:
5035
SMILE:
OC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(OCCN3CCCCC3)C=C2)C2=C(S1)C=C(O)C=C2
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
Classification:
Kingdom:
Organic Compounds
Superclass:
Phenylpropanoids and Polyketides
Class:
Stilbenes
Subclass:
Indication:
For the prevention and treatment of osteoporosis in post-menopausal women, as well as prevention and treatment of corticosteroid-induced bone loss. Also for the reduction in the incidence of invasive breast cancer in postmenopausal women wi...
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Pharmacodynamics:
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 breast and...
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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 mamma...
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Mechanism:
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 miner...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
-
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Non-inhibitor
P-glycoprotein inhibitor II:
Inhibitor
Renal organic cation transporter:
Inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Inhibitor
CYP450 2C19 substrate:
Inhibitor
CYP450 inhibitory promiscuity:
High CYP Inhibitory Promiscuity
Ames test:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.5287 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
One Gustave L. Levy Place, Box 1498
Manhattan, New York City, NY
repurposedb@dudleylab.org