Raloxifene (Evista)
Benzothiophene SERM, FDA-approved (1997 Lilly) for postmenopausal osteoporosis + ER+ breast cancer chemoprevention. AAS-context niche use: existing gynecomastia reversal with stronger breast selectivity than Nolvadex. NOT a primary HPTA-restart SERM.
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WHAT IS RALOXIFENE (EVISTA)?
Detailed overview
Raloxifene (Evista) is a benzothiophene-class selective estrogen receptor modulator (SERM), chemically distinct from triphenylethylene-class Nolvadex/Clomid. Eli Lilly received FDA approval in 1997 for postmenopausal osteoporosis (MORE trial Cummings 1999 PMID 10580020), and in 2007 the indication was expanded for invasive ER+ breast cancer chemoprevention in high-risk postmenopausal women (STAR trial Vogel 2006 PMID 16754727 – Raloxifene vs Tamoxifen head-to-head: similar prevention efficacy, lower VTE risk). Tissue-specific profile: ER-α antagonist in breast + endometrium, agonist in bone. In AAS context, Raloxifene occupies a niche position: REVERSAL of existing gynecomastia (NOT HPTA axis restart) – Lawrence 2004 PMID 14744776 demonstrated 50%+ reduction of pubertal gyno tissue over 6 months. Provides stronger anti-estrogenic breast-tissue selectivity than Nolvadex, explaining its breast-targeted use. Glucuronidation is the primary metabolism (NOT CYP2D6 like Tamoxifen), avoiding SSRI interaction – one practical advantage. FDA Evista label: venous thromboembolism (VTE) black-box warning, 3-fold relative risk elevation vs placebo (MORE trial data).
Mechanism
Benzothiophene SERM, ER-α antagonist in breast+uterus, agonist in bone
Dosing (AAS gyno-reversal)
60 mg/day × 6-12 weeks
Half-life
~27 h (once-daily dose)
Onset
Gyno-tissue regression 6-12 weeks
Legal status
FDA + EMA Rx (postmenopausal osteo + breast-cancer prevention), WADA S4 (banned)
Data console
Lab data
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Venous thromboembolism (deep vein thrombosis, pulmonary embolism) – FDA Evista black-box warning, roughly 3-fold increased relative risk vs placebo, highest during the first 4 months.
- Hot flashes – common (around 25-30%), especially in the first months of treatment, a consequence of the SERM estrogen-antagonist effect.
- Leg cramps and muscle spasms – well-documented, common adverse effect in the Evista trials.
- Peripheral edema (fluid retention, leg swelling) – a common complaint.
- Flu-like syndrome, joint pain (arthralgia) and sweating – among the milder, frequently reported side effects.
- Increased risk of fatal stroke documented in women with proven coronary heart disease or at high cardiovascular risk (RUTH trial) – overall stroke incidence was not raised, but fatal outcomes were.
Contraindications · 7
- Active or past venous thromboembolic event (deep vein thrombosis, pulmonary embolism, retinal vein thrombosis) – absolute contraindication per FDA Evista label.
- Pregnancy and women who may become pregnant, plus breastfeeding – Pregnancy Category X, teratogenic, contraindicated in women of childbearing potential.
- Prolonged immobilization (post-surgical recovery, long travel, bed rest) – due to VTE risk; should be stopped at least 72 hours before immobilization and not resumed until full mobility returns.
- Established coronary heart disease, prior stroke or high cardiovascular risk – fatal stroke risk was increased in the RUTH trial.
- Severe hepatic impairment (liver insufficiency) – insufficient safety data, caution or avoidance advised.
- Severe renal impairment – limited data, cautious use required.
- Unexplained uterine bleeding or endometrial abnormality – must be investigated before starting raloxifene.
Related Performance Compounds
Same therapeutic category
Studies
Related research and clinical findings
The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation.
Cummings SR, Eckert S, Krueger KA, Grady D, Powles TJ, Cauley JA, Norton L, Nickelsen T, Bjarnason NH, Morrow M, Lippman ME, Black D, Glusman JE, Costa A, Jordan VC
Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial
Vogel VG, Costantino JP, Wickerham DL, et al.
Beneficial effects of raloxifene and tamoxifen in the treatment of pubertal gynecomastia.
Lawrence SE, Faught KA, Vethamuthu J, Lawson ML
Treatment of adolescents with gynecomastia.
Malozowski S, Stadel BV
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The information here is for educational and scientific purposes only. Performance-enhancing compounds (AAS, prohormones, stimulants, doping agents) are illegal without prescription in Hungary and most of the EU, and carry serious health and legal risks. WADA bans them in competitive sport. This is NOT a usage guide, and we do not encourage any illegal use. If you do use them, medical supervision and regular bloodwork are ESSENTIAL. Severe endocrine, cardiovascular, hepatic and psychiatric side effects are possible.