Ligandrol (LGD-4033)

Technical data

INN name

Ligandrol

Development code

LGD-4033

Identity and composition

Ligandrol (LGD-4033) is an orally administered non-steroidal selective androgen receptor modulator (SARM), investigated for its tissue-selective interaction with the androgen receptor (AR), with the design premise of favoring an anabolic effect in muscle and bone with lower androgenic activity in other tissues. Product for research use.

Unlike peptides, LGD-4033 is not a chain of amino acids, but a small molecule; therefore it has no peptide sequence. Its reference chemical identity constants are:

• Name / synonyms: Ligandrol, LGD-4033, VK5211 / VK-5211
• CAS: 1165910-22-4
• Molecular formula: C14H12F6N2O
• Molecular weight: ~338.25 g/mol
• PubChem CID: 44137686
• IUPAC name: 4-[(2R)-2-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-2-(trifluoromethyl)benzonitrile

This presentation corresponds to 10 mg per tablet, 100 tablets per package.

Mechanism of action

LGD-4033 acts as androgen receptor (AR) ligand with activity described as tissue-selective: the SARM class hypothesis is to achieve preferential anabolic signaling in muscle and bone with lower prostatic androgenic activity. It is a non-steroidal small molecule, not a peptide.

In the early-phase clinical trial, administration was associated with dose-dependent suppression of total testosterone, SHBG, HDL cholesterol, and triglycerides, with suppression of FSH and free testosterone only at the highest dose; these findings are consistent with modulation of the androgenic axis (Basaria et al., 2013; PMID 22459616).

These descriptions are of an educational nature about the investigated mechanism and do not constitute a claim of clinical efficacy.

Pharmacokinetics

In the phase 1 trial, LGD-4033 showed linear / dose-proportional pharmacokinetics in the studied range (0.1-1 mg/day). A ... was described long elimination half-life, with dose-proportional accumulation after repeated administration (levels approximately 3 times higher on day 21 versus day 1) (Basaria et al., 2013; PMID 22459616).

Transparency note: the specific numerical half-life value that circulates in secondary sources was not extracted from the peer-reviewed abstract, so here it is described qualitatively as "long" without assigning an exact figure.

Scientific evidence

La peer-reviewed clinical evidence is limited and early-phase. The main study (Basaria et al., 2013, J Gerontol A Biol Sci Med Sci; PMID 22459616) was a trial of phase 1, randomized, placebo-controlled, and dose-escalation in 76 healthy young men (21-50 years), with doses of 0.1, 0.3 and 1.0 mg/day for 21 days, whose stated objective was to evaluate safety, pharmacokinetics and effects on body composition.

The SARM class has been investigated as a possible approach for lean mass loss conditions, but LGD-4033 has no regulatory approval and its documented clinical development is early-stage. The data on long-term efficacy and in clinical populations are scarce; the available evidence should be interpreted as preliminary.

Research applications

Product for research use.

Ideal for:

• Research in vitro and laboratory studies on selective androgen receptor modulators (SARMs).
• Chemical-analytical reference work and characterization of the SARM class.
• Educational research on androgen receptor pharmacology.

Not applicable for:

• clinical, dietary, therapeutic, or supplementation use.
• Sport use: LGD-4033 is banned in sport by WADA.
• Any application involving administration to people or animals outside an authorized research framework.

Research protocols

In the only available peer-reviewed clinical trial (phase 1), the doses investigated were 0.1, 0.3, and 1.0 mg/day for 21 days in healthy young men (Basaria et al., 2013; PMID 22459616). These values correspond to the study design and do not constitute a recommendation for use nor a dosing regimen for people.

In the open peer-reviewed literature, there are no validated protocols beyond phase 1 or efficacy schemes in clinical populations. Any handling must be restricted to the researcher's laboratory experimental design.

Reconstitution

This presentation is a small molecule in tablet format (10 mg), so does not require reconstitution like lyophilized peptides: it does not dissolve with bacteriostatic water for its intended use.

As a general laboratory reference: bacteriostatic water (water with ~0.9% benzyl alcohol) is the standard diluent for reconstituting lyophilized peptide vials, which does not apply to this product in tablet form. If a research protocol requires preparing a solution of LGD-4033, the appropriate solvents should be used according to the laboratory's technique, not bacteriostatic water.

Stability and storage

As a general laboratory-handling standard, the tablets should be stored in a place cool, dry and protected from light, in its closed container and away from moisture. Unlike reconstituted peptides, a solid in tablet form does not require immediate refrigeration after opening, although a cool, stable environment favors preservation.

If a working solution for research is prepared, it is usually less stable than the solid and should be kept refrigerated or frozen according to the protocol, minimizing freeze-thaw cycles. These are qualitative handling guidelines, not validated stability specifications for this product.

Safety profile

In the 21-day phase 1 trial, LGD-4033 was well tolerated, with no serious adverse events related to the drug and no significant changes in hemoglobin, PSA, liver enzymes, or cardiac markers during the studied period (Basaria et al., 2013; PMID 22459616). There was observed dose-dependent suppression of the hormonal axis (total testosterone, SHBG) and of lipids (HDL, triglycerides); these parameters returned to baseline values after discontinuation.

Important considerations:

• La long-term safety is not established in peer-reviewed literature.
• Outside the study context there are independent reports (case reports) of hepatotoxicity associated with commercial products containing SARMs, although they were not part of the cited controlled trial.
• Reinforcing the framing: product for research use.

Comparative context

LGD-4033 belongs to the class of Non-steroidal SARMs, along with compounds such as ostarine (MK-2866 / enobosarm) y RAD-140 (testolone).

Compared with anabolic androgenic steroids, the design premise of SARMs is a greater tissue anabolic selectivity (muscle and bone) with lower prostatic androgenic activity. It is important to emphasize that the direct head-to-head comparison with other SARMs in the peer-reviewed clinical literature is limited; these notes are at the class level and do not imply demonstrated superiority of one compound over another.

History and development

LGD-4033, also known as Ligandrol and under the development code VK5211 / VK-5211, was developed as an oral non-steroidal selective androgen receptor modulator. Its published clinical characterization corresponds to a phase 1 trial in healthy young men (Basaria et al., 2013; PMID 22459616), focused on safety, pharmacokinetics and body composition.

Its class (SARMs) has been investigated as a possible approach for muscle/lean mass loss conditions, but LGD-4033 has not reached regulatory approval for clinical use and its documented clinical development remains in an early phase. It is banned in sport by WADA.

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Scientific references (4)

Peer-reviewed literature on Ligandrol (LGD-4033), with its PubMed identifier where available:

• Variation of Sequential Ligandrol (LGD-4033) Metabolite Levels in Routine Anti-Doping Urine Samples Detected with or without Other Xenobiotics (Kwiatkowska D et al. · Molecules (Basel, Switzerland) · 2023) PMID 37764261.
• LGD-4033 and MK-677 use impacts body composition, circulating biomarkers, and skeletal muscle androgenic hormone and receptor content: A case report (Cardaci TD et al. · Experimental physiology · 2022) PMID 36303408.
• Ligandrol (LGD-4033)-Induced Liver Injury (Barbara M et al. · ACG case reports journal · 2020) PMID 32637435.
• The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men. (Basaria S, et al. · J Gerontol A Biol Sci Med Sci · 2013) PMID 22459616.

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