Raloxifene powder, sold under the brand name Evista among others, is a medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids. For osteoporosis it is less preferred than bisphosphonates. It is also used to reduce the risk of breast cancer in those at high risk.
02 Raloxifene powder (84449-90-1) video
03 Raloxifene powder Base Information
|Chemical name||Raloxifene; Pharoxifene; Raloxifenum;|
|Molecular Weight||473.584 g/mol|
|Melting Point||267.3-268.5 °C|
|Appearance||White to Off-white powder|
|Half Life||27.7 hours|
|Solubility||Raloxifene (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of raloxifene (hydrochloride) in thesesolvents is approximately 0.1, 15, and 10 mg/ml, respectively.|
|Storage Condition||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Application||Raloxifene used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids.|
04 Raloxifene powder (84449-90-1) General Description
EVISTA (raloxifene hydrochloride) is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM) that belongs to the benzothiophene class of compounds.
Raloxifene powder is a selective estrogen receptor modulator (SERM); acts as an anti-estrogen in both breast and uterine tissue while being estrogenic in bone. May have efficacy against estrogen-sensitive cancers.
05 Raloxifene powder (84449-90-1) History
Raloxifene powder is a second generation selective estrogen receptor modulator (SERM) that mediates anti-estrogenic effects on breast and uterine tissues, and estrogenic effects on bone, lipid metabolism, and blood coagulation.6,12 Exhibiting tissue-specific effects distinct from estradiol, raloxifene is the first of the benzothiophene group of antiestrogens to be labelled a SERM.7 Available in many countries worldwide, raloxifene was initially approved by the FDA in December, 1997 under the market name Evista® for the management and prevention of osteoporosis in postmenopausal women and reduction in risk for invasive breast cancer in postmenopausal women with osteoporosis or those who are at high risk for invasive breast cancer. However, it has a negligible effect on altering the development and progression of breast cancer itself.Label The most common causes of osteoporosis include postmenopausal deficiency of estrogen and age-related deterioration in bone homeostasis. Due to the risk of bone fractures that may lead to morbidities and reduced quality of life, the management of osteoporosis in postmenopausal women with the use of therapeutic agents in addition to concurrent therapies is critical. Due to the decline in estrogen levels in postmenopausal osteoporosis, hormone replacement therapy (HRT), such as estradiol, has been used to ameliorate the condition. However, due to the off-target actions by HRT, newer non-hormonal agents such as raloxifene and tamoxifen have been developed to reduce adverse events through selective pharmacological actions on tissue-specific therapeutic targets.
06 Raloxifene (84449-90-1) Mechanism Of Action
Hormones are chemical substances that are produced by glands in the body, which enter the bloodstream and cause effects in other tissues. For example, the hormone testosterone, made in the testicles and is responsible for male characteristics such as deepening voice and increased body hair. The use of hormone therapy to treat cancer is based on the observation that receptors for specific hormones that are needed for cell growth are on the surface of some tumor cells. Hormone therapy can work by stopping the production of a certain hormone, blocking hormone receptors, or substituting chemically similar agents for the active hormone, which cannot be used by the tumor cell. The different types of hormone therapies are categorized by their function and/or the type of hormone that is affected.
Selective Estrogen Receptor Modulator: [Raloxifene] SERM (Selective Estrogen Receptor Modulator) describes drugs that act like estrogen in some organs and as an anti-estrogen in others.
Raloxifene acts like estrogen to prevent bone loss and improve lipid profiles (decreases total and LDL cholesterol but does not raise triglycerides), but it has the potential to block some estrogen effects such as those that lead to breast cancer and uterine cancer.
Note: We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in this website is meant to be helpful and educational, but is not a substitute for medical advice.
07 Raloxifene (84449-90-1) Application
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. Raloxifene has been found to be effective in the treatment of gynecomastia (male breast development) in adolescents. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate.
08 Raloxifene (84449-90-1) More research
Raloxifene is used to prevent and treat osteoporosis (condition in which the bones become thin and weak and break easily) in postmenopausal (women who have experienced a change of life; end of menstrual periods) women. Raloxifene is also used to decrease the risk of developing invasive breast cancer (breast cancer that has spread outside of the milk ducts or lobules into the surrounding breast tissue) in postmenopausal women who are at high risk of developing this type of cancer or who have osteoporosis. Raloxifene cannot be used to treat invasive breast cancer or to prevent invasive breast cancer from coming back in women who have already had the condition. Raloxifene also cannot be used to decrease the risk of developing noninvasive breast cancer. Raloxifene should not be used in women who have not yet experienced menopause. Raloxifene is in a class of medications called selective estrogen receptor modulators (SERMs). Raloxifene prevents and treats osteoporosis by mimicking the effects of estrogen (a female hormone produced by the body) to increase the density (thickness) of bone. Raloxifene decreases the risk of developing invasive breast cancer by blocking the effects of estrogen on breast tissue. This may stop the development of tumors that need estrogen to grow
09 Raloxifene (84449-90-1) Document Download
10 Raloxifene (84449-90-1) Reference
Battani S, Pawar H, Suresh S. Evaluation of oral bioavailability and anticancer potential of raloxifene solid lipid nanoparticles. J Nanosci Nanotechnol. 2014 Aug;14(8):5638-45. PubMed PMID: 25935981.
Meme L, Santarelli A, Marzo G, Emanuelli M, Nocini PF, Bertossi D, Putignano A, Dioguardi M, Lo Muzio L, Bambini F. Novel hydroxyapatite biomaterial covalently linked to raloxifene. Int J Immunopathol Pharmacol. 2014 Jul-Sep;27(3):437-44. PubMed PMID: 25280036.
Kumar P, Song ZH. Identification of raloxifene as a novel CB2 inverse agonist. Biochem Biophys Res Commun. 2013 May 24;435(1):76-81. doi: 10.1016/j.bbrc.2013.04.040. Epub 2013 Apr 20. PubMed PMID: 23611779; PubMed Central PMCID: PMC5084446.
- 01. Overview
- 02. Raloxifene powder (84449-90-1) video
- 03. Raloxifene powder Base Information
- 04. Raloxifene powder (84449-90-1) General Description
- 05. Raloxifene powder (84449-90-1) History
- 06. Raloxifene (84449-90-1) Mechanism Of Action
- 07. Raloxifene (84449-90-1) Application
- 08. Raloxifene (84449-90-1) More research
- 09. Raloxifene (84449-90-1) Document Download
- 10. Raloxifene (84449-90-1) Reference