LGD-4033 is a 3rd generation non-steroidal oral SARM with a high affinity for the androgen receptor (Ki of ~1 nM). LGD 4033 is currently the second most popular SARM on the market. LGD-4033 has high selectivity for receptors in skeletal muscle, bone, and connective tissue, with minimal affinity for receptors in the prostate, scalp and skin.
It was developed by Ligand Pharmaceuticals for conditions such as muscle wasting and osteoporosis without the virilizing side effects of anabolic steroids.
Preclinical primate data showed a significant quantity-dependent increase in lean body mass for male and female monkeys during 13 weeks of testing at either 0.6, 3, 15, or 75 MG/KG of bodyweight. In addition to this, 70% of the increased body mass was retained after a 4 week recovery period.
Only the 75mg/kg group stopped testing after 48 days due to toxicity. This quantity is significantly higher than the highest quantity administered in other mammalian clinical trials.
A Phase 1 clinical trial with 76 adult male subjects showed a quanity-dependent increase in lean body mass and was well tolerated by all 76 subjects for 21 days. Phase 2 clinical trials consisted of 120 subjects recovering from hip fracture surgery.
The subjects either received a placebo, 0.5, 1, or 2mg LGD-4033 over 12 weeks. All quantities of LGD-4033 created significant increases in total lean body mass and subjects exhibited quantity dependent decreases in mean fat mass.
Subjects showed improvements in serum procollagen type 1 propeptide (s-P1NP), a marker of bone anabolism, and improvements in 6-minute walk distance as compared to placebo. No significant adverse effects were reported in any of the study groups.
Subjects were assessed 12 weeks after completion of the trial, at which they maintained the muscle mass that they had gained from the LGD-4033.
LGD 4033 Ligandrol SARM Research on Mice
In the context of postmenopausal women, hormonal decline can have negative impacts on muscle tissues and muscle and bone cells. LGD 4033 Ligandrol and other SARMs, have been identified as potential solutions to increase muscle mass and muscle-building properties such as the muscle’s physical performance, with relatively low-risk profiles.
However, little is known about the side effects of these SARMs on muscle structure and metabolism. To address this gap, two experiments were conducted using ovariectomized rats as a standard model for postmenopausal conditions.
In these animal studies, 3-month old Sprague-Dawley rats were divided into five groups (n = 12 to 15). One test subject group remained intact (Non-OVX), while the other four groups were ovariectomized (OVX) and remained untreated for eight (OS Experiment) or nine (ligandrol LGD 4033 Experiment) weeks.
Three of the four OVX test subjects were then treated with OS or ligandrol LGD 4033. Uterus, gastrocnemius, and soleus muscles were weighed, and muscle fiber size, capillary density, and enzyme activity were analyzed. The body recomposition, body fat, cortical bone, half life, prostate specific antigen, fat loss or gain, cancellous bone, and sex drive were not tested in this study.
In the LG 4033 experiment, intramuscular fat content was also determined in the quadriceps femoris muscle. Results indicated that all OS treatments resulted in positive effects for capillary density in the gastrocnemius and longissimus muscles compared to the Non-OVX and OVX rats.
All ligandrol LGD 4033 treatments showed a higher capillary density compared to the Non-OVX group. However, muscle fiber size and distribution patterns were not altered under either SARM. Liver toxicity and bone mineral density was not mentioned in this study.
What Are the Experimental Benefits of LGD-4033?
1. Whether or not it is the most potent SARM for overall effects on muscle tissue.
2. Its effects and side effects on muscle strength or muscle loss, bone strength or bone loss, and connective tissue post-injury and post-surgery.
Sports Technology Labs and Research
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AT THIS TIME, LIGANDROL / LGD-4033 IS ONLY APPROVED FOR LABORATORY RESEARCH AND IS NOT SOLD FOR HUMAN CONSUMPTION.
LGD-4033 is an investigational compounds still awaiting FDA approval and are not dietary supplements. At Sports Technology Labs we are chemical suppliers, not medical doctors, and our expertise is sourcing and quality control.
Sports Technology Labs does not encourage or condone consumer use of SARMs products, they are for research purposes only. Anecdotal reports and guides may not match those used in carefully designed medical research protocols and may pose a serious risk of adverse effects in users.
Individual variables, comorbidities, and polypharmacy can also contribute significantly to the risk of health problems.
LGD-4033 is banned in competitive sports as these chemicals are not for human consumption and are for research use only. Competitive athletes should not participate in clinical research using SARMs.
1. Basaria et al. The Safety, Pharmacokinetics, and Effects of LGD-4033, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men. The Journals of Gerontology: Series A, Volume 68, Issue 1, January 2013, Pages 87–95.
2. Fragkaki et al. Human in vivo metabolism study of LGD-4033. Drug Test Analysis. Drug Test Anal. 2018 Nov;10(11-12):1635-1645. doi: 10.1002/dta.2512. Epub 2018 Nov 8.
3. “Viking Therapeutics Initiates Phase 2 Trial of VK5211 in Patients Recovering From Hip Fracture.” FierceBiotech. Questex LLC, 03 Nov. 2015. Web. 21 Nov. 2016.
4. Roch, P. J., Henkies, D., Carstens, J. C., Krischek, C., Lehmann, W., Komrakova, M., & Sehmisch, S. (2020). Ostarine and ligandrol improve muscle tissue in an ovariectomized rat model. Frontiers in endocrinology, 11, 556581.