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A photograph of a white plastic pill bottle labeled "RAD-140, 10 mg, Batch No.002, 11-05-2025." The bottle stands on a beige surface with two white capsules placed neatly in front. Minimalist beige background and bold black typography emphasize the clean, professional pharmaceutical design
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RAD-140 100x10mg

RAD-140 100x10mg

€75,00 EUR
Taxes included.

                                    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

Benefit Key take-aways
1 Potent lean-mass accrual (preclinical → early translational) In castrate/ovariectomy and diet-induced models, RAD-140 increases fat-free mass and myofiber CSA with limited prostate stimulation—per-mg potency among the higher in the SARM class. <br/><em>Journal of Pharmacology & Experimental Therapeutics; FASEB Journal</em>
2 Strength & function Improves specific force, grip strength, and stair/peak torque surrogates in animal/bench models; human functional datasets remain limited. <br/><em>Medicine & Science in Sports & Exercise; AJP–Endocrinology</em>
3 Bone-anabolic effects Raises BMD, enhances trabecular architecture, and improves biomechanical strength with modest prostate changes. <br/><em>Journal of Bone and Mineral Research; Bone</em>
4 Anti-catabolic under stress Down-shifts atrogenes (MAFbx/MuRF1) and preserves CSA during glucocorticoids, disuse, or illness in preclinical studies. <br/><em>Endocrine Reviews; Molecular Metabolism</em>
5 Body-composition “repartitioning” In obese models, reduces fat mass while preserving or increasing lean tissue—largely via AR-mTOR activation and improved oxidative programs. <br/><em>Obesity; Metabolism</em>
6 Neuroprotection signals AR agonism with RAD-class ligands protects hippocampal neurons, enhances synaptic markers, and improves memory tasks in injury/aging models (translational relevance pending). <br/><em>Neurobiology of Aging; Brain Research</em>
7 AR-positive breast cancer (preclinical) In ER⁺/AR⁺ models, selective AR agonism inhibits proliferation and shows additivity with CDK4/6 inhibitors—clinical validation needed. <br/><em>Cancer Research; Annals of Oncology</em>
8 Rehab synergy Pairing with progressive resistance training yields additive hypertrophy/function vs either alone in translational paradigms. <br/><em>Sports Medicine; Journal of Physiology</em>
9 Oral convenience Once-daily oral administration with long detection metabolites supports adherence in trials—also increases anti-doping scrutiny. <br/><em>Clinical Pharmacology & Therapeutics; Drug Testing & Analysis</em>

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

Pathway Functional outcome Context
AR → mTOR/S6K/4E-BP1 ↑ protein synthesis, myofiber hypertrophy Skeletal muscle
AR ↔ Wnt/β-catenin/Osterix ↑ osteoblast activity, ↑ BMD Bone
FoxO → MAFbx/MuRF1↓ ↓ proteolysis (anti-catabolic) Catabolic stress
Myostatin/activin crosstalk Net anabolic bias Muscle
Neurotrophic signaling (AR-dependent) Synaptic support, neuroprotection (preclinical) CNS

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

Field Rationale Current status
Sarcopenia/frailty Oral anabolic with prostate-sparing intent Preclinical/early translational
Rehabilitation/immobilization Preserve/restore FFM & function Concept pilots
Osteopenia/osteoporosis (adjunct) Bone-anabolic + anti-resorptive balance Preclinical
Cachexia Appetite-neutral anabolism vs ghrelin mimetics Preclinical
AR⁺/ER⁺ breast cancer Selective AR agonism as antitumor strategy Preclinical/early clinical exploration

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

Concern RAD-140 LGD-4033 Enobosarm (MK-2866)
Human evidence Very limited Small RCT (21 d) Multiple Phase 2
HPG suppression Moderate–strong Moderate Moderate
HDL impact ↓ Common ↓ Common ↓ Common
Prostate stimulation Low (preclinical) Low Low
Hepatotoxicity signal Case reports (unregulated) Case reports Case reports (rarer)
Route / t½ Oral; long (inferred) Oral; 24–36 h Oral; ~24 h

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.