Injectable RAD140 500mg vial

                                          NOT FOR HUMAN CONSUMPTION

RAD-140 (testolone) is an oral, non-steroidal selective androgen receptor modulator (SARM) engineered to deliver anabolic effects in muscle and bone with comparatively less stimulation of prostate/skin than testosterone. It binds the androgen receptor (AR), recruits muscle/bone-biased co-activators, and—unlike testosterone—does not aromatize to estradiol or undergo 5-α reduction. RAD-140 is not FDA/EMA-approved and is prohibited by WADA as an anabolic agent.

Additional Benefits of RAD-140 Now Under Investigation

2. Molecular Mechanism of Action

2.1 Receptor Pharmacodynamics

RAD-140 binds AR → nuclear translocation → ARE-driven transcription. In muscle it up-regulates mTOR/S6K/4E-BP1 and local IGF-1, while suppressing FoxO-atrogenes; in bone, AR signaling promotes osteoblastogenesis (Wnt/β-catenin/Osterix) and may indirectly restrain resorption. Lack of aromatization/5-α reduction contributes to tissue selectivity vs testosterone.

2.2 Down-stream Biology

3. Pharmacokinetics

• Route: Oral.

• Exposure/half-life: Human PK has not been formally published; industry/forensic reports suggest a long terminal half-life compatible with once-daily dosing and multi-week metabolite detection in urine.

• Metabolism: Hepatic oxidative/conjugative clearance; no aromatase/5-α pathways.

• Protein binding: High (class feature).

• Food effect: Not well characterized publicly.

4. Pre-clinical and Translational Evidence

4.1 Muscle & Function

Robust lean-mass and force improvements in rodent models, with lower prostate stimulation than testosterone for comparable anabolic effects.

4.2 Bone

In ovariectomized models, spine/femur BMD and three-point-bend strength improve, supporting exploration as an osteopenia adjunct (preclinical).

4.3 Neuro/CNS

Androgen-axis agonism with RAD-class ligands shows neuronal survival and synaptic plasticity benefits in injury/aging models; human translation is untested.

4.4 Oncology (AR⁺/ER⁺ breast)

Selective AR activation via non-steroidal ligands can inhibit ER-driven proliferation in preclinical systems; RAD-140 is part of this research space.

Evidence quality note: For RAD-140 specifically, human efficacy/safety data are sparse. Most signals derive from animal/in-vitro work and anti-doping forensics rather than registrational trials.

5. Emerging Clinical Interests

6. Safety and Tolerability

• Endocrine: Dose-dependent HPG-axis suppression (↓ LH/FSH/testosterone) expected; recovery often weeks–months after cessation.

• Lipids: HDL-C reduction (± ↑ LDL/TG) common across SARMs—monitor CV risk.

• Hepatic: Short controlled datasets are limited; case reports of cholestatic/drug-induced liver injury exist with unregulated RAD-140–containing products (purity/co-ingestants confound).

• CV: No outcome data; lipid shifts and possible BP effects warrant caution.

• Dermatologic/androgenic: Acne/oily skin, hair shedding in predisposed individuals.

• Neuropsych: Insomnia, irritability, anxiety occasionally described in uncontrolled settings.

• Hematologic: Mild ↑ hematocrit possible—monitor in at-risk populations.

• Drug interactions: Potential with drugs affecting hepatic enzymes/lipids; avoid hepatotoxins and use in pregnancy.

Comparative safety matrix

7. Regulatory Landscape

• Approvals: None for any medical indication.

• Sport: WADA-prohibited (S1, Other Anabolic Agents) at all times; detection of long-term metabolites enables weeks-long windows.

• Market quality: Grey-market products frequently show adulteration/mislabeling; medical use outside trials is unsafe.

8. Future Directions

• First-in-human PK/PD with GMP material to define half-life, metabolites, exposure–response.

• Head-to-head vs other SARMs for anabolic:androgenic ratio, lipid neutrality, and HPG suppression.

• Long-term safety: lipids/CV outcomes, hepatic profile, endocrine recovery, mood/CNS effects.

• Oncology programs in AR⁺/ER⁺ breast cancer, rational combos (CDK4/6 inhibitors, endocrine therapy).

• Rehab/sarcopenia RCTs paired with progressive resistance training and protein targets; standardized functional endpoints (SPPB, stair-climb power, 6MWT).

• Doping science: Comprehensive metabolite ID, hair/urine detection windows, and contamination risk mapping.

Selected References

• Journal of Pharmacology & Experimental Therapeutics; FASEB Journal — Anabolic and anti-catabolic signaling of RAD-class SARMs in muscle.

• Journal of Bone and Mineral Research; Bone — SARM effects on BMD and biomechanical strength in osteopenic models.

• Neurobiology of Aging; Brain Research — AR-mediated neuroprotection and synaptic support (preclinical).

• Cancer Research; Annals of Oncology — Selective AR agonism in ER⁺/AR⁺ breast cancer models.

• Medicine & Science in Sports & Exercise; AJP–Endocrinology — Strength/function correlates under AR activation.

• Drug Testing & Analysis — Identification of RAD-140 long-term metabolites and detection windows.

• Hepatology Communications; J Clin Transl Hepatol — Case reports of liver injury associated with unregulated SARM products (class context).

• Clinical Pharmacology & Therapeutics — Oral PK/PD considerations for non-steroidal SARMs.