At a glance
Effects
- Bone density preservation: Acts as an estrogen agonist in bone, inhibiting osteoclast-driven bone resorption and increasing bone mineral density in both the short and long term [1][2].
- Breast cancer risk reduction: Acts as an estrogen antagonist in breast tissue, blocking estrogen-driven cell proliferation and reducing invasive breast cancer risk in high-risk postmenopausal women [2][7].
- Favourable lipid profile: Decreases total and LDL cholesterol and fibrinogen levels; does not meaningfully raise HDL or triglycerides [5][8].
- No uterine stimulation: Unlike tamoxifen (a first-generation SERM), raloxifene has an estrogen-antagonistic effect in the uterus and does not promote endometrial proliferation or increase uterine cancer risk [1][6].
- Anti-gynecomastia (off-label): Used off-label in male performance contexts to block estrogen receptors in breast tissue, targeting gynecomastia. This use is not FDA-approved and clinical evidence in males is limited; no approved dosing guidance exists for this population [2].
Second-generation SERM
~27 hours
Oral (tablet)
60 mg/day
1997 (osteoporosis / breast cancer risk)
About Raloxifene
Every point here is drawn from public medical and harm-reduction sources. A bracketed number after a claim — like [1]— is a reference: tap it to open the exact source it's based on (numbered list at the bottom). It is not a rating or score. Educational information, not medical advice.
Product specifics
- Est. delivery
- 3–7 business days · EU tracked
Product details as stated by the vendor (claims, not independently verified). Delivery is our standard EU estimate.
What it is
Raloxifene (brand name Evista) is a second-generation selective estrogen receptor modulator (SERM) — a non-steroidal compound that acts as an estrogen agonist in some tissues and an estrogen antagonist in others [1]. It is FDA-approved for the treatment and prevention of postmenopausal osteoporosis and for the reduction of invasive breast cancer risk in postmenopausal women [2].
How it works
Raloxifene crosses the cell membrane and binds directly to estrogen receptors (ERs) in the nucleus [3]. The precise agonist or antagonist outcome depends on which co-activators or co-repressors are recruited to ER target gene promoters in each tissue [4]. In bone, it acts as an estrogen agonist — suppressing bone resorption and increasing bone mineral density [5]. In breast and uterine tissue it acts as an antagonist, blocking estrogen-driven cell proliferation [6]. It does not aromatise and does not meaningfully stimulate the uterus [7]. It also exerts favourable effects on LDL-cholesterol and fibrinogen through its partial estrogen-agonist activity in the liver [8].
Risks & side effects
Most important: Raloxifene significantly increases the risk of venous thromboembolism (VTE), including deep vein thrombosis (DVT) and pulmonary embolism — the highest risk period is the first 4 months of use [9]. It may also increase risk of fatal stroke in women with pre-existing coronary heart disease or major cardiovascular risk factors [10].
Common
Serious
Safety & harm reduction
- Active or past history of venous thromboembolism (DVT, pulmonary embolism, retinal vein occlusion) [9][10]
- Pregnancy or women of reproductive potential — may harm the fetus [10]
- Breastfeeding — not recommended [10]
- Severe renal impairment — contraindicated in absence of safety data [13]
- Men — not indicated; FDA approval and clinical trials are exclusively in postmenopausal women [2]
- Prothrombin time (PT) if co-administered with warfarin — raloxifene can reduce PT by ~10% [12][14]
- Signs and symptoms of DVT or PE (leg pain/swelling, chest pain, shortness of breath) throughout treatment [9]
- Liver function — raloxifene clearance is significantly reduced in hepatic impairment; bilirubin levels correlate with plasma exposure [12]
- Breast and uterine changes — report any unexpected vaginal bleeding or breast changes to a clinician [7]
- Cholestyramine (and other anion exchange resins) — reduces raloxifene absorption and enterohepatic cycling by ~60%; co-administration is not recommended [14]
- Warfarin / coumarin anticoagulants — minor interaction via protein-binding competition; monitor prothrombin time closely when starting or stopping raloxifene [12][14]
- Systemic estrogens (HRT) — concurrent use not recommended [13]
- Ampicillin — reduces peak raloxifene concentration by ~28% [4]
- Ospemifene — synergistic estrogen-receptor modulation; monitor closely [13]
- Apalutamide, levothyroxine, famciclovir — monitor for altered effects when co-administered [13]
- Discontinue raloxifene at least 3 days before any prolonged immobility (surgery, long-haul travel) and restart only when fully mobile — to minimise VTE risk [10]
- Supplement with calcium and vitamin D if dietary intake is inadequate when using for osteoporosis prevention [2]
- Off-label use in male performance contexts (e.g., gynecomastia) is not supported by approved prescribing information — seek specialist medical guidance before use [2]
Dosage context
The FDA-approved dose for both osteoporosis treatment/prevention and breast cancer risk reduction is 60 mg once daily, taken orally at any time of day without regard to meals [2]. This is the only clinically established and approved dosage. Off-label use in males (e.g., for gynecomastia) is not covered by prescribing information, and no validated dosing guidance exists for this population — sources are thin and any dose used off-label should be discussed with a qualified clinician [2].
Sources
- 1.StatPearls – Raloxifene (NIH/NCBI Bookshelf)
- 2.RxList – Evista (Raloxifene) Prescribing Information
- 3.ClinicalTrials.gov – Raloxifene Pharmacology Protocol (Phase 2/3)
- 4.ScienceDirect – Raloxifene Overview (Pharmacology/Toxicology)
- 5.AAFP – Raloxifene: A Selective Estrogen Receptor Modulator
- 6.Drugs.com – Raloxifene Side Effects
- 7.Mayo Clinic – Raloxifene (Oral Route)
- 8.Cleveland Clinic – Raloxifene (Evista): Uses & Side Effects
- 9.Drugs.com – Raloxifene Monograph (Uses, Warnings)
- 10.DailyMed – Raloxifene Hydrochloride Tablet (FDA Label)
- 11.WebMD – Raloxifene (Evista): Uses, Side Effects, Dosing
- 12.Drugs.com – Raloxifene Hydrochloride Tablets Prescribing Information
- 13.FDA – Evista (Raloxifene) Label (accessdata.fda.gov)
- 14.PMC – Pharmacotherapeutic Considerations of SERMs for Vascular Protection
This information is provided for educational and harm-reduction purposes only. It is not medical advice. These substances can carry serious health risks; effects and safe use vary by individual. Consult a qualified healthcare professional before use. Legal status varies by country — it is your responsibility to know your local law. We do not encourage misuse.
Substance reviews(2)
Independent reviews of this compound from the wider market — about the substance, not our delivery.
- ★★★★★11 months ago
Best
- ★★★★★2 years ago
Thanks for the fast delivery. As always reliable and professional.