Name: | Raloxifene |
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PubChem Compound ID: | 11071264 |
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. |
Molecular formula: | C28H28ClNO4S |
Molecular weight: | 510.045 g/mol |
Name: | Raloxifene |
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Name (isomeric): | DB00481 |
Drug Type: | small molecule |
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. |
Synonyms: |
Raloxifene Hcl; Raloxifenum [Latin]; Raloxifene Hydrochloride; RAL; LY-139481; Raloxifeno [Spanish]
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Brand: | Evista, Keoxifene |
Category: | Antihypocalcemic Agents, Estrogen Antagonists, Osteoporosis Prophylactic, Bone Density Conservation Agents, Selective Estrogen Receptor Modulators |
CAS number: | 84449-90-1 |
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 with osteoporosis or have a high risk for developing breast cancer. |
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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 breast and uterine tissue. Raloxifene differs chemically and pharmacologically from naturally occuring estrogens, synthe...
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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, thus slowing the rate of bone loss. The maintenance of bone mass by raloxi...
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Absorption: | Approximately 60% of an oral dose is absorbed, but presystemic glucuronide conjugation is extensive. Absolute bioavailability of raloxifene is 2.0% |
Protein binding: | 95% |
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 |
Route of elimination: | Raloxifene is primarily excreted in feces, and less than 0.2% is excreted unchanged in urine. |
Half Life: | 27.7 |
Clearance: | 44.1 L/kg•hr [Healthy Postmenopausal Woman with Single Dose] 47.4 L/kg•hr [Healthy Postmenopausal Woman with Multiple Dose] Oral cl=44.1 L/kg•hr |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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