Raloxifene CAS No. 84449-90-1

Product Description

Raloxifene (brand name Evista and others) is a second-generation selective estrogen receptor modulator (SERM) taken once daily at 60 mg to prevent and treat osteoporosis in postmenopausal women and to cut the risk of invasive breast cancer in those who are at high risk or already have osteoporosis. It works like estrogen in bone—strengthening mineral density—while blocking estrogen’s effects in breast and uterine tissue, thereby reducing the likelihood of hormone-driven cancers without stimulating the endometrium. Common side effects include hot flashes, leg cramps and joint pain, whereas its most serious, though rare, risks are blood clots (DVT, PE) and stroke, leading to boxed warnings and contraindications in anyone with a history of venous thromboembolism, pregnancy, or breastfeeding. Compared with tamoxifen, raloxifene offers a safer profile for the uterus, yet it is somewhat less potent in preventing breast cancer; calcium and vitamin D supplementation and routine breast monitoring remain recommended throughout therapy.

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Product Use & Characteristics

Chemical Identity

• IUPAC Name: [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone

• Molecular Formula: C₂₈H₂₇NO₄S

• Molecular Weight: 473.6 g mol⁻¹

Therapeutic Class

• Second-generation Selective Estrogen Receptor Modulator (SERM).

Mechanism of Action

• Bone: Estrogen-agonist → ↑ osteoblasts, ↓ osteoclasts → ↑ bone mineral density & ↓ fractures.

• Breast & Uterus: Estrogen-antagonist → ↓ ER-positive cell proliferation → ↓ invasive breast-cancer risk.

• Cardiovascular/CNS: Estrogen-like endothelial & neuro-protective effects.

Approved Uses

• Prevention & treatment of postmenopausal osteoporosis.

• Reduction of invasive breast-cancer risk in postmenopausal women (with osteoporosis or high risk).

Investigational / Off-label Uses

• Osteopenia.

• Prostate, pancreatic, lung, bladder, cervical, hepatocellular cancers.

• Cognitive adjunct in schizophrenia.

• Broad-spectrum antiviral (RNA-dependent RNA-polymerase inhibitor) including COVID-19.

Dosage & Administration

• 60 mg orally once daily, with or without food.

• Co-supplement calcium & vitamin D if dietary intake inadequate.

Efficacy Summary

• ↑ Lumbar-spine BMD 2.6–4 %.

• ↓ Vertebral fractures 30–76 %.

• ↓ Invasive ER-positive breast cancer 55–90 %.

• RdRP inhibition shown in-silico (binding energy ≈ –8.8 kcal/mol).

Common Adverse Effects

• Hot flashes, leg cramps, peripheral edema, flu-like symptoms.

Serious / Rare Adverse Effects

• ↑ Venous thrombo-embolism (DVT/PE) & stroke (boxed warning).

• Reversible ovarian cysts; no ↑ endometrial cancer.

Contra-indications

• History of venous thrombo-embolism.

• Pregnancy or women who may become pregnant (teratogenic).

• Active or past endometrial cancer (relative).

Drug Interactions & Monitoring

• Avoid systemic estrogens.

• Separate levothyroxine by ≥12 h.

• Monitor INR with warfarin.

• Baseline & periodic: BMD, mammography, VTE risk factors.

Pharmacokinetics

• Oral bioavailability ~2 %; half-life 27–32 h.

• Hepatic glucuronidation; faecal (60 %) & renal (25 %) excretion.

Available Formulations & Brands

• Evista® (60 mg tablets).

• Generics: Raloxifeno, Keoxifene, RaboneD® (60 mg + cholecalciferol 800 IU).

Why us!

Qingdao Sigma Chemical Co., Ltd., established in January 2017 and headquartered in Qingdao, China, is a reliable chemical supplier. Specializing in pharmaceuticals, biochemical intermediates, and research chemicals, the company offers a diverse product portfolio, including peptides (e.g., Tirzepatide, Semaglutide), nootropics, veterinary products, and APIs, often marketed with ≥99% purity and COA certification. We provides R&D, custom synthesis, and contract manufacturing services at various scales, while claiming a global export presence across 100+ countries. With international warehouses in the USA, Europe, Australia, and Canada, Qingdao Sigma Chemical also facilitates drop-shipping and reshipments, positioning itself as a key supplier for laboratory and research applications.