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    LGD-4033 (Ligandrol) molecular structure

    LGD-4033 (Ligandrol)

    PerformancePhase 2

    Also known as: Ligandrol, LGD4033, LGD 4033, VK5211, VK-5211, Anabolicum

    LGD-4033, usually sold as ligandrol, is a nonsteroidal selective androgen receptor modulator that Viking Therapeutics took into clinical development under the code VK5211 (NCT02578095). The stated development goal was an oral drug that produces the muscle and bone effects of testosterone with less action on prostate and skin, aimed at conditions such as recovery after hip fracture and other causes of muscle loss.

    Half-Life: Long elimination half-life in humans with dose-proportional accumulation over 21 days of daily dosing in healthy young men; the report describes the profile without giving a single value in its summary (PMID: 22459616)Route: OralMW: 338.25 g/molCAS: 1165910-22-4
    Last reviewed:
    Performance
    Category
    Phase 2
    Research Stage

    Overview

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    At A Glance

    Mechanism

    LGD-4033 binds the androgen receptor with high affinity and selectivity and acts as a nonsteroidal agonist, driving transcription of androgen-responsive genes in skeletal muscle and bone while sparing prostate to a greater degree than testosterone (PMID: 22459616). Because the re

    Half-Life
    Long elimination half-life in humans with dose-proportional accumulation over 21 days of daily dosing in healthy young men; the report describes the profile without giving a single value in its summary (PMID: 22459616)
    Routes
    Oral
    Potential Benefits
    Increased lean body mass without a change in fat mass over 21 days in healthy young men in a placebo-controlled phase 1 study (PMID: 22459616)Improved muscle tissue in ovariectomized rats (PMID: 33042018)Improved trabecular bone structural properties at the highest dose tested in ovariectomized rats (PMID: 37407738)

    Overview

    LGD-4033, usually sold as ligandrol, is a nonsteroidal selective androgen receptor modulator that Viking Therapeutics took into clinical development under the code VK5211 (NCT02578095). The stated development goal was an oral drug that produces the muscle and bone effects of testosterone with less action on prostate and skin, aimed at conditions such as recovery after hip fracture and other causes of muscle loss. It has not been approved by any regulator, and clinical development has not progressed past phase 2. Mechanistically it binds the androgen receptor with high affinity and selectivity and acts as an agonist in muscle and bone. The consequences of that binding are visible in the human phase 1 data: over three weeks of daily dosing in healthy young men, total testosterone, sex hormone binding globulin, HDL cholesterol and triglycerides all fell in a dose-dependent way, follicle-stimulating hormone and free testosterone fell at the top dose, and lean body mass rose without a change in fat mass (PMID: 22459616). Hormone levels and lipids returned to baseline after the drug was stopped in that 21-day study, which is a short exposure compared with how the compound is used outside research. Animal work supports an anabolic signal but is mixed on whether that translates to performance. In ovariectomized rats, ligandrol improved muscle tissue (PMID: 33042018) and improved trabecular bone structure at the highest dose tested in ovariectomized rats (PMID: 37407738). In male rats, however, ligandrol lowered endurance and worsened lipid and hormonal profiles (PMID: 40087185). Human safety reports are the strongest reason for caution. Published case reports describe severe cholestatic liver injury confirmed on biopsy after ligandrol use, including a 32-year-old man with cholestatic hepatitis and fibrosis (PMID: 32637435), a 37-year-old man with bilirubin about thirty times the upper limit of normal and ductopenia on biopsy (PMID: 36257328), a further case in an otherwise healthy adult (PMID: 39421081) and cases involving ligandrol together with post-cycle drugs (PMID: 34141767). A retrospective Australian series of drug-induced liver injury from anabolic steroids, SARMs and bodybuilding supplements collected 23 cases, most of whom were admitted to hospital, with a median 175 days to normal liver biochemistry and one liver transplant (PMID: 38372012). A self-reported case of ligandrol taken with the growth hormone secretagogue MK-677 recorded alanine aminotransferase up about 205 percent, HDL cholesterol down about 36 percent and total testosterone down about 62 percent (PMID: 36303408). In sport, LGD-4033 is prohibited at all times under the World Anti-Doping Agency class S1.2 and has been found in athlete urine samples (PMID: 27168428). Its human urinary metabolites are well characterized for testing purposes (PMID: 30255601). FDA has issued warning letters to firms selling it as an unapproved new drug (FDA warning letter to Titan SARMs LLC, 12 December 2025). What is sold as ligandrol is often mislabeled: in an analysis of 44 SARM-marketed products, only about half contained any SARM and the label amount matched the assay in 41 percent (PMID: 29183075).

    Potential Research Fields

    Muscle wasting and sarcopeniaBone and fracture recoverySports drug testingHepatotoxicity surveillance

    Chemical Information

    IUPAC Name

    Not yet available

    CAS Number

    1165910-22-4

    Molecular Formula

    C14H12F6N2O

    Molecular Mass

    338.25 g/mol

    Dosing & Protocols

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    Interactions

    Contraindications

    Mechanism-based: contraindicated in pregnancy because androgen receptor agonists can virilize a female fetus, and in men with known or suspected prostate cancer. Existing liver disease or raised transaminases is a case-report-based reason to avoid it (PMID: 32637435, PMID: 36257328). Because it suppresses endogenous testosterone and gonadotropins (PMID: 22459616), it works against men being treated for infertility. Prohibited for athletes in tested sport at all times (PMID: 28137616).

    Research Disclaimer

    This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.

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    Vendors Selling LGD-4033 (Ligandrol)

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    Ostarine (Enobosarm, MK-2866)

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    Ostarine is the market name for enobosarm, a nonsteroidal selective androgen receptor modulator first developed by GTx Inc under the codes GTx-024, MK-2866 and S-22.

    t½ Not established from a retrieved human report; in rats the mean elimination half-life of radiolabeled GTx-024 was 0.6 h in males and 16.4 h in females (PMID: 24074268). Human plasma pharmacokinetics were characterized in phase 1 drug-interaction studies (PMID: 27105861)
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    t½ Native MGF: very short (minutes) due to rapid proteolysis. PEG-MGF: PEGylation is intended to extend this substantially (community estimates up to roughly 1 day), but there are no published human pharmacokinetic data to confirm a specific value. 200
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    RAD-140 (Testolone)

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    RAD-140, sold as testolone and given the international nonproprietary name vosilasarm, is a nonsteroidal selective androgen receptor modulator developed at Radius Health, whose scientists reported the first-in-human trial (PMID: 34565686), and first described in the medicinal chemistry literature as a compound with an oxadiazole core designed for oral androgen receptor activity with tissue selectivity (PMID: 24900290).

    t½ Terminal half-life 44.7 hours in humans, measured in a first-in-human phase 1 study in postmenopausal women with metastatic breast cancer (PMID: 34565686)
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    View Full Dosage Guide →

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    1 vendors · 1 listings

    Research Score

    30

    0 PubMed studies

    Quality Indicators

    Data Completeness

    63%
    Description
    Mechanism of Action
    Chemical Data
    Dosing Protocols
    Safety Profile
    PubMed Studies
    Interactions
    Vendor Listings

    Quick Facts

    Half-Life

    Long elimination half-life in humans with dose-proportional accumulation over 21 days of daily dosing in healthy young men; the report describes the profile without giving a single value in its summary (PMID: 22459616)

    Molecular Weight

    338.25 g/mol

    Administration

    Oral

    CAS Number

    1165910-22-4

    Trial Phase

    Phase 2

    0

    Research Disclaimer

    This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.

    Frequently Asked Questions

    What is LGD-4033 (Ligandrol) used for in research?

    LGD-4033, usually sold as ligandrol, is a nonsteroidal selective androgen receptor modulator that Viking Therapeutics took into clinical development under the code VK5211 (NCT02578095). The stated development goal was an oral drug that produces the muscle and bone effects of testosterone with less action on prostate and skin, aimed at conditions such as recovery after hip fracture and other causes of muscle loss. It has not been approved by any regulator, and clinical development has not progressed past phase 2.

    Mechanistically it binds the androgen receptor with high affinity and selectivity and acts as an agonist in muscle and bone. The consequences of that binding are visible in the human phase 1 data: over three weeks of daily dosing in healthy young men, total testosterone, sex hormone binding globulin, HDL cholesterol and triglycerides all fell in a dose-dependent way, follicle-stimulating hormone and free testosterone fell at the top dose, and lean body mass rose without a change in fat mass (PMID: 22459616). Hormone levels and lipids returned to baseline after the drug was stopped in that 21-day study, which is a short exposure compared with how the compound is used outside research.

    Animal work supports an anabolic signal but is mixed on whether that translates to performance. In ovariectomized rats, ligandrol improved muscle tissue (PMID: 33042018) and improved trabecular bone structure at the highest dose tested in ovariectomized rats (PMID: 37407738). In male rats, however, ligandrol lowered endurance and worsened lipid and hormonal profiles (PMID: 40087185).

    Human safety reports are the strongest reason for caution. Published case reports describe severe cholestatic liver injury confirmed on biopsy after ligandrol use, including a 32-year-old man with cholestatic hepatitis and fibrosis (PMID: 32637435), a 37-year-old man with bilirubin about thirty times the upper limit of normal and ductopenia on biopsy (PMID: 36257328), a further case in an otherwise healthy adult (PMID: 39421081) and cases involving ligandrol together with post-cycle drugs (PMID: 34141767). A retrospective Australian series of drug-induced liver injury from anabolic steroids, SARMs and bodybuilding supplements collected 23 cases, most of whom were admitted to hospital, with a median 175 days to normal liver biochemistry and one liver transplant (PMID: 38372012). A self-reported case of ligandrol taken with the growth hormone secretagogue MK-677 recorded alanine aminotransferase up about 205 percent, HDL cholesterol down about 36 percent and total testosterone down about 62 percent (PMID: 36303408).

    In sport, LGD-4033 is prohibited at all times under the World Anti-Doping Agency class S1.2 and has been found in athlete urine samples (PMID: 27168428). Its human urinary metabolites are well characterized for testing purposes (PMID: 30255601). FDA has issued warning letters to firms selling it as an unapproved new drug (FDA warning letter to Titan SARMs LLC, 12 December 2025). What is sold as ligandrol is often mislabeled: in an analysis of 44 SARM-marketed products, only about half contained any SARM and the label amount matched the assay in 41 percent (PMID: 29183075).

    What forms does LGD-4033 (Ligandrol) come in?

    LGD-4033 (Ligandrol) is available in liquid form.

    How much does LGD-4033 (Ligandrol) cost?

    Prices start at $84.99 across 1 verified vendor.

    How do I compare LGD-4033 (Ligandrol) vendors?

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    Research Tools

    Related Compounds

    View All

    ITPP

    PerformancePreclinical

    ITPP (myo-inositol trispyrophosphate, sometimes written myo-inositol tripyrophosphate or OXY111A in NormOxys trial documents) is a small-molecule allosteric effector of hemoglobin designed to increase the amount of oxygen red blood cells release to tissues.

    Research compound — IV infusion in studies, no established oral doses
    36 studiesView Profile

    Ostarine (Enobosarm, MK-2866)

    PerformancePhase 3

    Ostarine is the market name for enobosarm, a nonsteroidal selective androgen receptor modulator first developed by GTx Inc under the codes GTx-024, MK-2866 and S-22.

    t½ Not established from a retrieved human report; in rats the mean elimination half-life of radiolabeled GTx-024 was 0.6 h in males and 16.4 h in females (PMID: 24074268). Human plasma pharmacokinetics were characterized in phase 1 drug-interaction studies (PMID: 27105861)
    PreclinicalView Profile

    PEG-MGF

    PerformancePreclinical

    PEG-MGF (Pegylated Mechano Growth Factor) is a synthetic, PEGylated form of Mechano Growth Factor (MGF) — an alternatively spliced variant of IGF-1 produced locally in muscle and other tissues in response to mechanical loading or damage.

    t½ Native MGF: very short (minutes) due to rapid proteolysis. PEG-MGF: PEGylation is intended to extend this substantially (community estimates up to roughly 1 day), but there are no published human pharmacokinetic data to confirm a specific value. 200
    PreclinicalView Profile

    RAD-140 (Testolone)

    PerformancePhase 1

    RAD-140, sold as testolone and given the international nonproprietary name vosilasarm, is a nonsteroidal selective androgen receptor modulator developed at Radius Health, whose scientists reported the first-in-human trial (PMID: 34565686), and first described in the medicinal chemistry literature as a compound with an oxadiazole core designed for oral androgen receptor activity with tissue selectivity (PMID: 24900290).

    t½ Terminal half-life 44.7 hours in humans, measured in a first-in-human phase 1 study in postmenopausal women with metastatic breast cancer (PMID: 34565686)
    PreclinicalView Profile

    SLU-PP-332

    PerformancePreclinical

    SLU-PP-332 is the first-generation synthetic pan-agonist of the estrogen-related receptors (ERRα, ERRβ, ERRγ) developed by the laboratory of Thomas Burris at Saint Louis University and reported in a landmark 2023 publication that established ERR pan-agonism as a pharmacologically tractable exercise-mimetic drug mechanism.

    Research compound — no established human doses. Animal studies: 10-50 mg/kg
    8 studiesView Profile

    YK-11

    PerformancePreclinical

    YK-11 is a synthetic steroid, not a nonsteroidal SARM, despite being sold alongside them.

    t½ Not established. In a human elimination study using deuterium-labeled YK-11, no intact parent compound was seen in urine; unconjugated metabolites disappeared within 24 hours and glucuronidated and sulfated metabolites remained traceable beyond 48 hours (PMID: 30379415)
    PreclinicalView Profile

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