SARMs

Ligandrol (LGD-4033)

Potent oral SARM with significant lean mass effects in Phase I trials

Evidence: 7 articles
Goals: 1

Mechanism of Action

Ligandrol (LGD-4033, VK5211) is a potent non-steroidal oral SARM that binds the androgen receptor with high affinity (Ki ~1 nM) and demonstrates marked tissue selectivity. In a Phase I multiple ascending dose study, LGD-4033 produced dose-dependent increases in lean body mass (up to 2.67 lbs at 1.0 mg/day) with improvements in physical function. The compound does not aromatize to estrogen and is not a substrate for 5-alpha reductase. LGD-4033 shows minimal effect on prostate-specific antigen (PSA) and hematocrit at therapeutic doses, distinguishing it from traditional AAS.

Evidence Level

Clinical Trial - Human

7 studies published

Pharmacology

Molecular Weight

392.3 g/mol

Half-Life

Approximately 24-36 hours (oral, human)

Bioavailability

Good oral bioavailability; ~100% in preclinical, not fully quantified in humans

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