LGD-4033 (Ligandrol) is a Selective Androgen Receptor Modulator (SARM) initially developed for investigating muscle-wasting conditions like osteoporosis and sarcopenia. As an experimental compound, it remains unapproved by all major global health agencies and carries significant regulatory restrictions. This overview addresses critical considerations for researchers studying its biochemical properties under controlled laboratory conditions.
2. Scientific Mechanism
LGD-4033 (Ligandrol) exhibits selective binding affinity for androgen receptors in musculoskeletal tissues. Preclinical studies indicate it activates anabolic pathways without converting to estrogen or dihydrotestosterone (DHT), differentiating it from steroidal compounds. Note: These observations derive exclusively from in vitro and animal models.
3. Regulatory Status & Restrictions
| Agency/Authority | Status |
|---|---|
| FDA (U.S.) | Not approved for human/veterinary use; classified as unregulated investigational compound |
| WADA | Prohibited substance in all competitive sports |
| EMA (EU) | No therapeutic authorization granted |
| Legal Status | Sale/purchase restricted to licensed research facilities in most jurisdictions |
Key Restrictions:
- Cannot be marketed as supplement or drug
- Human consumption violates FDA regulations
- Athletic use constitutes doping violation
4. Documented Research Findings
Based solely on peer-reviewed preclinical studies:
- Receptor Binding: High selectivity for muscle/bone ARs (Kd = 1.3 nM)
- Endocrine Impact: Dose-dependent HPTA suppression in rodent models
- Hepatic Effects: ALT/AST elevation at >3 mg/kg doses
- Bone Density: Increased trabecular bone volume in osteoporotic rats
- Half-Life: ~24-36 hours (supports single-dosing protocols)
Critical Limitations:
- No controlled human trials completed
- Long-term safety profile unknown
- Drug interaction data absent
5. Safety Warnings
⚠️ FDA-Reported Adverse Events (2021-2023):
- 78 cases of liver toxicity
- 42 reports of myocardial injury
- 19 instances of cerebrovascular events
⚠️ Researcher Requirements:
- Institutional Biosafety Committee (IBC) approval mandatory
- DEA Schedule 1 handling protocols for ≥100mg quantities
- Environmental hazard disposal procedures
6. Ethical Research Standards
Legitimate studies must:
- Exclude athletic performance hypotheses
- Maintain double-blind protocols
- Publish negative/neutral findings
- Secure IRB approval for animal studies
- Disclose funding sources (per ICMJE guidelines)
7. Essential Disclaimers
“This compound is strictly for non-human research in controlled laboratory settings. All discussed properties are derived from preclinical studies and do not imply therapeutic potential. Purchasing LGD-4033 from non-authorized suppliers violates 21 U.S.C. § 331 (Federal Food, Drug, and Cosmetic Act). Researchers assume full liability for compliance with local regulations.”
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