RAD-140 vs Raloxifene
Emerging vs FDA Approved
avoid Mechanism-based · 53% Both RAD-140 and Raloxifene carry hepatotoxic risk. Combining hepatotoxic compounds significantly increases liver damage potential. If unavoidable, include liver support (TUDCA/NAC) and monitor ALT/AST frequently.
Molecular Data
RAD-140 Raloxifene
Weight 393.83 Da 473.58 Da
Half-life ~60 hours ~28 hours
Type Nonsteroidal selective androgen receptor modulator (C20H16ClN5O2) Benzothiophene-derived selective estrogen receptor modulator
Key Benefits
RAD-140
01 Potent anabolic activity in muscle tissue with high oral bioavailability
02 Tissue-selective action sparing the prostate and other androgen-sensitive organs
03 No aromatization to estrogen (no estrogen-related side effects such as water retention or gynecomastia)
04 No conversion to DHT (reduced risk of hair loss and prostate stimulation compared to testosterone)
05 Long half-life (~60 hours) permitting convenient once-daily oral dosing
06 Neuroprotective properties observed in preclinical models
07 Increased lean body mass and reduced fat mass in preclinical studies
Raloxifene
01 Superior breast tissue estrogen receptor antagonism makes it the preferred SERM for gynecomastia reversal
02 No estrogen agonist activity in the uterus, avoiding the endometrial risks associated with tamoxifen
03 Estrogen agonist activity in bone preserves bone mineral density and reduces fracture risk
04 Lower overall thromboembolic risk compared to tamoxifen
05 Metabolized via glucuronidation rather than CYP2D6, avoiding the drug interaction concerns that affect tamoxifen
06 Simple once-daily oral dosing with a manageable 28-hour half-life
07 FDA-approved with decades of clinical safety data in postmenopausal women
Side Effects
RAD-140
Testosterone suppression (dose-dependent, occurs in virtually all users by week 4-6)
Liver enzyme elevation (ALT, AST increases reported in clinical and anecdotal data)
Hair shedding (temporary, typically resolves after discontinuation)
Headaches (most common in the first 1-2 weeks, often transient)
Nausea (mild, usually with initial doses or on an empty stomach)
Lipid disruption (HDL suppression, LDL elevation)
Mild insomnia or sleep disturbance
Reduced libido and mood changes related to testosterone suppression
Raloxifene
Hot flashes and increased sweating
Leg cramps and muscle spasms
Joint pain or stiffness
Peripheral edema (mild swelling in extremities)
Flu-like symptoms during initial weeks
Contraindications
Pre-existing liver disease or elevated liver enzymes at baseline
Hormone-sensitive cancers (prostate cancer, certain breast cancers not being treated under clinical supervision)
Pregnancy or potential pregnancy (teratogenic risk from androgen receptor agonism)
Breastfeeding
Age under 25 (incomplete endocrine system maturation and higher risk of HPG axis disruption)
Concurrent use of hepatotoxic medications without medical supervision
Known cardiovascular disease (insufficient safety data for this population)
History of deep vein thrombosis, pulmonary embolism, retinal vein thrombosis, or other venous thromboembolic events
Active or past history of stroke or transient ischemic attack
Known hypersensitivity to raloxifene hydrochloride or any excipients
Pregnancy or planned pregnancy (category X -- contraindicated)
Prolonged immobilization (e.g., post-surgical recovery, extended bed rest) due to elevated DVT risk
Severe hepatic impairment
Research Evidence
RAD-140 Raloxifene
Status Emerging FDA Approved
References 5 studies 4 studies
Latest July 2020 —
FDA Approved No Yes
This comparison is for educational and research purposes only. Consult a healthcare professional before use.