raloxifene_hydrochloride: profile and news

Lilly Reports Q1 EPS of $.77, or 13% Growth Apr 20, 2006
Pharmaceuticals) Cialis(R) (tadalafil, ICOS), Lilly ICOS LLC Cymbalta(R) (duloxetine hydrochloride, Lilly) Evista(R) (raloxifene hydrochloride, Lilly) Forteo(R ... - MSN Money

Jury Issues Verdict in Ariad v. Lilly Patent Infringement Suit May 4, 2006
Evista(R) (raloxifene hydrochloride, Lilly) Xigris(R) (drotrecogin alfa (activated), Lilly) (Logo: http://www.newscom.com/cgi-bin/prnh/20031219/LLYLOGO ). - PR Newswire (press release),

Other information

Indication
For the prevention of osteoporosis in post-menopausal women

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.

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.

Drug Category
Antihypocalcemic Agents; Osteoporosis Prophylactic; Selective Estrogen Receptor Modulators; Estrogen Antagonists; ATC:G03XC01

Brand Names/Synonyms
CCRIS 7129; CHEMBANK1694; Evista; Keoxifene; RAL; Raloxifene; Raloxifene Hcl; Raloxifene Hydrochloride; Raloxifeno [Spanish]; Raloxifenum [Latin]

Dosage Forms
Tablet

Absorption
Approximately 60% of an oral dose is absorbed, but presystemic glucuronide conjugation is extensive. Absolute bioavailability of raloxifene is 2.0%

Interactions
Interactions for Raloxifene:

Cholestyramine: Cholestyramine causes a 60% reduction in the absorption and enterohepatic cycling of raloxifene and should not be coadministered with EVISTA.

Warfarin: The coadministration of EVISTA and warfarin has not been assessed under chronic conditions. However, 10% decreases in prothrombin time have been observed in single-dose studies. If EVISTA is given concurrently with warfarin, prothrombin time should be monitored.

Other Highly Protein-Bound Drugs: Raloxifene is more than 95% bound to plasma proteins. In vitro, raloxifene did not affect the binding of warfarin, phenytoin, or tamoxifen. Caution should be used when EVISTA is coadministered with other highly protein-bound drugs, such as clofibrate, indomethacin, naproxen, ibuprofen, diazepam, and diazoxide.

See also CLINICAL PHARMACOLOGY, Drug-Drug Interactions

Chemical IUPAC Name
[6-hydroxy-2-(4-hydroxyphenyl)-benzothiophen-3-yl]-[4-[2-(1-piperidyl)ethoxy]phenyl]-methanone

Chemical Formula
C28H27NO4S

Half Life
27.7

Drug Type
Approved Drug

# Accession No
APRD00400

CAS Registry Number
84449-90-1