Raloxifene (Evista)

Raloxifene, sold as Evista, is a pill taken once a day. It belongs to a group of drugs called SERMs — selective estrogen receptor modulators (medicines that switch estrogen’s effects on or off depending on which part of the body they reach). It’s a legitimate, well-studied prescription drug. It helps to be clear about what it is and isn’t: raloxifene is not a peptide, it’s not an aromatase inhibitor (a different kind of anti-estrogen drug that works in another way), and it’s not an anabolic steroid. It’s a benzothiophene (a specific type of molecule) that latches onto the estrogen receptor and acts like estrogen in some tissues (bone and blood fats) while blocking estrogen in others (breast and uterus). For postmenopausal women, it has a solid, repeatedly published track record for protecting bone and lowering breast-cancer risk. In bodybuilding circles, some people use it off-label (outside its approved purpose) to block estrogen in breast tissue — a practice that isn’t approved, has barely been studied in men, is banned in sport, and carries genuine risks of blood clots and stroke. This page is meant to inform and reduce harm. It contains no doses, cycles, stacks, or post-cycle protocols, and no information on where to buy anything.

What it is

Raloxifene is a second-generation SERM and a benzothiophene (a particular molecule shape). It binds to estrogen receptors (the docking sites estrogen normally uses, called ERα and ERβ) and then either mimics estrogen or blocks it — depending on the tissue and which helper proteins are present. In bone, it acts like estrogen: it slows down the cells that break bone down (osteoclasts), which keeps or builds up bone density (the strength of your bones, measured as bone mineral density, or BMD). It also lowers LDL cholesterol (the “bad” cholesterol). In breast and uterine (womb-lining) tissue, it does the opposite — it blocks estrogen.

This on-in-some-places, off-in-others behavior is what sets it apart from older anti-estrogen drugs. Unlike tamoxifen, raloxifene does not stir up the uterine lining, so it doesn’t carry tamoxifen’s risk of uterine cancer. And unlike aromatase inhibitors (anastrozole, letrozole, exemestane) — which lower estrogen by shutting down the enzyme that makes it — raloxifene doesn’t reduce the amount of estrogen in your blood at all. Instead, it just blocks the receptor in the tissues that matter. The approved product is 60 mg of raloxifene HCl taken once a day.

The claims

Medically, raloxifene is used in postmenopausal women to prevent and treat osteoporosis (weak, brittle bones), and to lower the risk of invasive breast cancer in the two labeled groups (women with osteoporosis and women at high risk of invasive breast cancer). It’s used in women and is not approved for men.

In the performance-enhancing-drug (PED) world — off-label, illicit, and unapproved — male anabolic-androgenic steroid users take SERMs like raloxifene, tamoxifen, and clomiphene as estrogen blockers in breast tissue. The usual stated goals are to manage or try to reverse gynecomastia (breast-tissue growth in men, driven by high-dose steroids converting into estrogen), and as part of “post-cycle” attempts to kick-start the body’s own testosterone again (SERMs can nudge up the hormones that signal the testes, and testosterone, in men). Raloxifene is sometimes chosen over tamoxifen specifically for managing breast-tissue gynecomastia. None of this is an approved use, the evidence in men is thin, and no doses, cycles, stacks, or post-cycle protocols are given here.

What the evidence actually shows

The evidence in postmenopausal women is large and solid — and it’s honest about where raloxifene falls short.

• Spine fractures (the MORE trial): Among 7,705 postmenopausal women with osteoporosis followed over 3 years, raloxifene raised bone density in the spine and hip and lowered the risk of spine fractures — for example, 6.6% in the 60 mg group versus 10.1% on placebo (a dummy pill) at 36 months (Ettinger et al., JAMA 1999).
• No proven benefit for hip or other fractures: The strong fracture evidence is for spine fractures only. In MORE, the risk of fractures elsewhere in the body was not meaningfully different (relative risk about 0.9). Raloxifene hasn’t been shown to prevent hip fractures or other non-spine fractures — an important limitation compared with bisphosphonates (another class of bone drugs).
• Breast-cancer prevention (the STAR / NSABP P-2 trial): Among 19,747 high-risk postmenopausal women, raloxifene was compared head-to-head with tamoxifen. In the updated results, raloxifene was about 76% as effective as tamoxifen at preventing invasive breast cancer (risk ratio of raloxifene to tamoxifen about 1.24) — but it caused fewer blood clots (relative risk about 0.75) and fewer uterine cancers (relative risk about 0.55) than tamoxifen (Vogel et al., Cancer Prev Res (Phila) 2010).
• Heart health (the RUTH trial): Among 10,101 postmenopausal women who already had heart disease or were at high risk for it (followed a median of about 5.6 years), raloxifene did not reduce heart attacks or other coronary events (hazard ratio 0.95). It did lower invasive breast cancer (hazard ratio 0.56) and spine fractures, but it was tied to a clear rise in fatal strokes (hazard ratio about 1.49) and more blood clots in the veins (hazard ratio about 1.44). Bottom line: no heart protection, and real damage to blood vessels (Barrett-Connor et al., NEJM 2006).

About PED use specifically: all the human evidence above comes from postmenopausal women, not healthy male athletes. There are no good-quality trials showing raloxifene works for blocking estrogen or restoring testosterone in men who use steroids. So any claims about how well it works — or how safe it is — for that purpose are mostly guesswork and poorly studied.

Legal and regulatory status

US — prescription (Rx) drug. Raloxifene (Evista) is legal only with a valid prescription. It is not a controlled substance — SERMs and aromatase inhibitors aren’t on the controlled-substance schedules. Buying or selling it without a prescription, or as a so-called “research chemical,” is against the law, and those products are unregulated and unchecked.

To keep the legal picture clear, here’s how it compares with the other compounds that often come up alongside it in the PED world:

• Mesterolone (Proviron) and fluoxymesterone (Halotestin) are anabolic-androgenic steroids — Schedule III controlled substances under the US Controlled Substances Act.
• DNP (2,4-dinitrophenol) is NOT approved for people to consume. The FDA banned it for weight loss back in the 1930s and considers it unfit for human consumption. It has a long history of deadly poisonings, is sold illegally as a “fat burner,” and has no antidote (nothing that reverses it).
• T3 (liothyronine) and insulin are real prescription drugs, not controlled substances, but they’re dangerous when misused to change body composition (see Safety).

Anti-doping (WADA 2026 Prohibited List, in force 1 January 2026). SERMs, including raloxifene, are banned at all times — both in and out of competition — under Section S4, “Hormone and Metabolic Modulators.”

• S4.2 Anti-estrogenic substances — raloxifene, tamoxifen, clomifene, toremifene, cyclofenil, fulvestrant, ospemifene, and bazedoxifene. This is where raloxifene sits.
• S4.1 Aromatase inhibitors — anastrozole, letrozole, exemestane, and others.
• S4.4 Metabolic modulators — includes insulins and insulin-mimetics (specifically S4.4.2).
• S1 Anabolic agents — mesterolone, fluoxymesterone, and other anabolic-androgenic steroids.

Two things to note about the 2026 list. First, the 2026 S4 additions are α-naphthoflavone (7,8-benzoflavone) as an aromatase inhibitor (S4.1) and BAM15 as an AMPK activator (S4.4) — both flagged because they keep showing up in supplements and “research chemicals.” Second, a point people often get wrong: DNP is NOT an S4 substance. It’s covered under S0 (Non-Approved Substances) and is banned at all times. T3 (liothyronine) isn’t specifically named on the WADA list, though misusing it is medically dangerous.

Safety

Raloxifene’s own harms are well understood — but the truly catastrophic, sudden dangers in this PED landscape come from the other compounds people combine with it.

Raloxifene’s own harms (the real ones):

• Blood clots in the veins (the most important serious risk). Raloxifene raises the risk of deep-vein thrombosis (DVT — a clot, usually in the leg) and pulmonary embolism (PE — a clot that travels to the lungs), and the risk is highest in the first few months of use. Women with a current or past clot shouldn’t take it. This is a labeled Warning in the EVISTA label (not the FDA’s strongest “boxed” warning).
• Fatal stroke. The RUTH trial showed an increased risk of dying from a stroke in women who were already at high risk for heart and blood-vessel problems, and the label carries a matching warning. Raloxifene does not prevent heart disease, even though it improves cholesterol.
• Other: hot flashes, leg cramps, and swelling in the legs and feet (peripheral edema). Because of the clot risk, it should be stopped before and during long periods of staying still (surgery, long travel).

Dangers of the drug class and the wider PED world (covered honestly):

• DNP — the deadliest item here. It jams up the way cells produce energy, so that energy escapes as runaway heat instead. This causes fatal overheating (core body temperature can climb toward about 44 °C / 111 °F), a racing heart, heavy sweating, dangerously acidic blood (metabolic acidosis), multiple organs shutting down, and cardiac arrest. There is no antidote. People have died even at “fat-loss” amounts, often going downhill fast, and frequently despite full hospital treatment. DNP kills people; it is flatly unsafe for humans to consume and should never be swallowed.
• Insulin (misused to change body composition): can cause severe, deadly low blood sugar — seizures, permanent brain damage, coma, and death — especially without medical monitoring and a quick carbohydrate rescue. It’s a well-documented cause of death among bodybuilders misusing metabolic drugs.
• Aromatase inhibitors (used to crush estrogen): pushing estrogen too low harms bone density (raising osteoporosis and fracture risk) and worsens cholesterol and heart risk, along with joint pain and effects on mood and libido.
• SERMs in general (raloxifene, tamoxifen): blood clots (DVT/PE, stroke) are the standout serious risk. Tamoxifen also carries a risk of uterine cancer (raloxifene does not) and reported vision problems.
• T3 (liothyronine): forcing the body into an overactive-thyroid state for fat loss causes strain on the heart (irregular and racing heartbeats, including atrial fibrillation), bone loss, and muscle breakdown, and it can shut down the body’s own thyroid system, sometimes taking a long time to recover.

Bottom line

Raloxifene is a properly approved, well-studied SERM for postmenopausal bone and breast-cancer-risk needs — not a peptide, not an aromatase inhibitor, and not an anabolic steroid. Its defining serious risks are blood clots and fatal stroke, and it has no proven benefit for hip fractures or for the heart. Its non-medical use in men is off-label and barely studied, and it’s banned in sport at all times under WADA S4.2. The truly catastrophic, sudden dangers in the surrounding PED-support landscape are DNP (no antidote, fatal overheating) and insulin (deadly low blood sugar).

Evidence grade: 10/10 · Established.

Sources

• Ettinger B et al., 1999 — MORE trial, reduction of vertebral fracture risk with raloxifene, JAMA 282(7):637-645 (PMID 10517716)
• Barrett-Connor E et al., 2006 — RUTH trial, raloxifene and cardiovascular events in postmenopausal women, N Engl J Med 355(2):125-137 (PMID 16837676)
• Vogel VG et al., 2010 — STAR / NSABP P-2 updated analysis, raloxifene vs tamoxifen, Cancer Prev Res (Phila) 3(6):696-706 (PMID 20404000)
• FDA-approved EVISTA (raloxifene HCl) label, 2007
• FDA EVISTA (raloxifene HCl) label, 2018 update
• Raloxifene — StatPearls (NCBI Bookshelf, NIH)
• Eli Lilly press release — FDA approval of EVISTA for breast-cancer risk reduction (2007)
• NCI — Study of Tamoxifen and Raloxifene (STAR) Q&A
• WADA — The Prohibited List
• USADA — 2026 WADA Prohibited List athlete advisory (S4.1 α-naphthoflavone, S4.4 BAM15)
• Sport Integrity Australia — 2026 Prohibited List
• 2,4-Dinitrophenol — FDA history, mechanism, lethality (Wikipedia)
• ACEP Now — case report, hyperthermic death from the diet pill DNP