Ligandrol (LGD-4033)
Potent oral SARM with significant lean mass effects in Phase I trials
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