LGD-3303

The company Ligand Pharmaceuticals originally developed the parent compound LGD-4033. In 2007, they synthesized a derivative known as 9-Chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo[3,2-f]quinolin-7(6H)-one, better recognized as LGD-3303. This commercially available SARM is an orally-administered, non-steroidal compound. Preliminary animal studies have shown that it can increase both bone mineral density (BMD) and muscle mass. Due to its high bioavailability and reported efficacy, LGD-3303 is currently under investigation for its ability to prevent muscle wasting and osteoporosis.

Key Research Findings on LGD-3303

1. Increases muscle mass without adversely affecting prostate weight in male Sprague-Dawley rats that have undergone orchidectomy.

2. Increases both bone mineral content (BMC) and BMD in female Sprague-Dawley rats post-ovariectomy.

Methodology

Experiment 1: Male Rats

Male Sprague-Dawley rats, approximately 7-8 weeks old and weighing around 200 grams each, were purchased from Harlan for experimental testing. After a 14-day recovery period, the rats were treated with varying doses of LGD-3303 or testosterone propionate. After two weeks, the rats were euthanized for further analyses.

Experiment 2: Female Rats

Female Sprague-Dawley rats, approximately 3 months old and weighing between 175-200 grams, were also purchased from Harlan. After a 7-week recovery period, the rats were divided into different treatment groups and treated over a span of 12 weeks.

Discussion

1. The study found that both LGD-3303 and testosterone propionate could enhance anabolic activity in male rats that had undergone orchidectomy. However, unlike testosterone, LGD-3303 increased muscle weight without a significant increase in prostate weight.

2. In female rats, treatment with LGD-3303 led to a significant increase in both bone mineral content and bone mineral density. This suggests that LGD-3303 has effective anabolic activity on bone.

In biomechanical tests, it was confirmed that all three treatment groups showed improvements, but the combination treatment was the most successful, although not significantly more so than the treatment with LGD-3303 alone.

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Data sheet LGD-3303