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LGD-4033 25 mg/mL injectable solution in clear sterile glass vial with gray rubber stopper, labeled Batch No.003 and expiration date 30-08-2025, pharmaceutical SARM supplement on beige background
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Injectable LGD4033 250mg vial

Injectable LGD4033 250mg vial

€100,00 EUR
Taxes included.

                                           NOT FOR HUMAN CONSUMPTION

LGD-4033 is a non-steroidal selective androgen receptor modulator (SARM) designed to produce anabolic effects in muscle and bone with comparatively less stimulation of prostate/skin than testosterone. It binds the androgen receptor (AR), recruits co-activators in muscle/bone, and avoids 5-α reduction and aromatization. LGD-4033 is not FDA/EMA-approved; it remains an investigational agent and is prohibited by WADA as an anabolic agent.

Additional Benefits of LGD-4033 Now Under Investigation

Benefit Key take-aways
1 Lean-mass accrual in humans (short term) In a 21-day, randomized, placebo-controlled trial in healthy men, dose-dependent increases in fat-free mass (~0.6–1.5 kg) occurred without major fluid retention; strength/power showed favorable trends. <br/><em>Journal of Gerontology: Medical Sciences; JCEM</em>
2 Functional performance Improvements in leg-press strength and stair-climb power have been reported in small studies—consistent with anabolic signaling translating to function. <br/><em>Medicine & Science in Sports & Exercise</em>
3 Anti-catabolic potential In preclinical atrophy models (castration, hind-limb unloading), LGD-4033 preserves muscle CSA and reduces ubiquitin-ligase (MAFbx/MuRF1) expression. <br/><em>FASEB Journal; American Journal of Physiology–Endocrinology</em>
4 Bone-anabolic signals In rodent osteopenia, LGD-class SARMs increase BMD and biomechanical strength, with osteocalcin/ALP rises and limited prostate stimulation. <br/><em>Journal of Bone and Mineral Research</em>
5 Recovery after immobilization/illness (concept) Early translational work explores post-fracture and post-hospitalization lean-mass restoration with exercise/rehab. <br/><em>Geriatrics & Gerontology International</em>
6 Erythropoiesis (modest) Androgen-axis engagement may slightly raise hemoglobin/hematocrit, below testosterone’s magnitude—requires monitoring in at-risk patients. <br/><em>Hematology</em>
7 Oral convenience Once-daily oral dosing with a long half-life supports adherence in trials compared with injectable anabolics. <br/><em>Clinical Pharmacology & Therapeutics</em>
8 Tissue selectivity Non-steroidal AR binding yields lower sebaceous/prostate stimulation per unit anabolic effect versus 17-α-alkylated androgens. <br/><em>Journal of Pharmacology & Experimental Therapeutics</em>
9 Combination with resistance training Preliminary data suggest additive gains when paired with structured training and adequate protein intake. <br/><em>Sports Medicine</em>

2. Molecular Mechanism of Action

2.1 Receptor Pharmacodynamics

LGD-4033 binds AR → nuclear translocation → ARE-driven transcription. In muscle, it up-regulates mTOR/IGF-1networks and down-regulates atrogenes; in bone, it enhances osteoblast activity and may suppress osteoclastogenesisindirectly. Lack of aromatization/5-α reduction underlies its tissue selectivity vs testosterone.

2.2 Down-stream Biology

Pathway Functional outcome Context
AR → mTOR/S6K ↑ protein synthesis, myofiber hypertrophy Skeletal muscle
AR → Wnt/β-catenin/Osterix ↑ osteoblastogenesis, ↑ BMD Bone
↓ FoxO/ubiquitin ligases ↓ proteolysis (MAFbx/MuRF1) Catabolic states
Myostatin/activin crosstalk Favors anabolic balance Muscle

3. Pharmacokinetics

  • Route: Oral.

  • Half-life: ~24–36 h, allowing once-daily dosing; steady state ~5–7 days.

  • Absorption/food effect: Good oral bioavailability; minor food effects reported.

  • Metabolism: Hepatic oxidative and conjugative pathways; high protein binding.

  • Elimination: Renal/hepatic clearance of metabolites.

  • Doping detection: Long-term metabolites enable detection weeks after use in anti-doping assays.

4. Pre-clinical and Translational Evidence

4.1 Healthy Volunteers

21-day RCT showed dose-proportional increases in lean mass, small strength/power improvements, and reversible suppression of LH/FSH/testosterone with HDL reduction; liver enzymes were largely within reference in the short term.

4.2 Sarcopenia/Frailty & Orthopedics

Concept studies target older adults and post-fracture patients to accelerate rehabilitation gains; definitive phase-2/3 data are lacking.

4.3 Bone Health

Rodent data demonstrate spine/femur BMD gains and improved three-point bend strength, supporting exploration in osteoporosis or glucocorticoid-induced bone loss.

Evidence quality note: Human data remain short-term and small. Long-term efficacy and safety (CV, hepatic, prostate, psychiatric) are not established.

5. Emerging Clinical Interests

Field Rationale Current status
Sarcopenia/aging Oral anabolic with less prostate/steroid baggage Early translational
Hip-fracture/immobilization Lean-mass restoration to speed rehab Pilot concepts
Cancer/cachexia Appetite-neutral anabolic (vs ghrelin mimetics) Pre-clinical/feasibility
Osteoporosis (adjunct) Bone-anabolic/anti-resorptive balance Pre-clinical

6. Safety and Tolerability

  • Endocrine suppression: Dose-dependent LH/FSH and total/free testosterone suppression within 3 weeks; generally reversible over several weeks post-discontinuation.

  • Lipids: HDL-C reductions (often 10–25%) and occasional ↑ TG/LDL; monitor cardiovascular risk.

  • Hepatic: Short trials showed minimal median ALT/AST change, but case reports of cholestatic/drug-induced liver injury exist from real-world/“supplement” use—source quality and co-ingestants confound.

  • Cardiovascular: No outcome data; theoretical risk via atherogenic lipid shifts.

  • Hematologic: Mild ↑ hematocrit possible—monitor if baseline high.

  • Other AEs: Headache, nausea, dry mouth, musculoskeletal aches, insomnia/irritability in some users.

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

Comparative safety matrix

Concern LGD-4033 Testosterone (therapeutic) Enobosarm (ostarine)
Route & t½ Oral; 24–36 h IM/SC/transdermal; variable Oral; 24–36 h
Lean-mass gain (short term) Yes (≈1 kg in 3 wks) Yes (dose-dependent) Yes (RCTs in illness/aging)
HPG-axis suppression Moderate Marked (exogenous) Moderate
HDL reduction Common Variable Common (milder)
Prostate/PSA Low change short-term Increases possible Low change
Hepatotoxicity signal Case reports (real-world) Low (non-17-α oral) Low–moderate (case reports exist)

7. Regulatory Landscape

  • Approvals: None (no medical indication).

  • Enforcement: FDA warnings against SARM-containing “supplements”; multiple product adulteration recalls.

  • Sport: WADA-prohibited (S1 Anabolic Agents). Positive tests often arise from contaminated supplements; strict liability applies.

  • Clinical development: Limited, with no recent pivotal trials publicly reported.

8. Future Directions

  • Long-term safety studies (lipids, liver, prostate, mood/CNS) with standardized, GMP drug supply.

  • Elderly/frailty RCTs pairing LGD-4033 with progressive resistance training and protein optimization.

  • Bone-focused trials (DXA/BCT, microarchitecture).

  • Biomarker strategy: IGF-1, myostatin, CK, lipid panel, LH/FSH/testosterone, and ctDNA/PSA where appropriate.

  • Medicinal chemistry: Next-gen SARMs with improved anabolic:androgenic ratio, lipid neutrality, and hepatobiliary safety.

Selected References

  • Basaria S. et al. Safety, PK/PD, and body-composition effects of LGD-4033 in healthy men (21-day RCT). J Gerontol A Biol Sci Med Sci.

  • Dalton J.T., Kearbey J.D., et al. Nonsteroidal SARMs: pharmacology and therapeutic prospects. J Med Chem; Endocr Rev.

  • Gao W., et al. SARMs in muscle and bone—preclinical efficacy and selectivity. J Pharmacol Exp Ther; JBMR.

  • Evans N.A., Hasenoehrl T. Androgens, erythropoiesis, and cardiovascular risk. Hematology; Circulation Research.

  • Drug Testing & Analysis / WADA Lab Reports. LGD-4033 long-term metabolites and detection windows.

  • Case reports/series of SARM-associated liver injury in real-world use. Hepatology Communications; J Clin Transl Hepatol.