LGD-3033

LGD 3033

LGD-3033 is a drug that acts as a selective androgen receptor modulator (SARM). It was initially designed and developed to reduce the prevalence and cure muscle wasting associated with different medical conditions like cancer. Today, this supplement is used by athletes for building muscles and improving exercise endurance. LGD-3033 increases muscle mass by improving water retention. Interestingly, the benefits of this SARM are not limited to muscle mass growth. LGD-3033 has other health benefits and is known to have milder side effects than LGD-4033.

Overall Health Benefits of LGD-3033

• Improves muscle mass and strength [1-6]
• Maintains bone strength and quality [7-16]
• Improves sexual function [17-24]
• Decreases urinary tract infections [25-26]

Proven Health Benefits by LGD 3033

LGD-3033 – Improves Muscle Mass and Strength

Like other SARMs, LGD-3033 can help enhance muscle strength by increasing muscle mass:

1. In rats, LGD-3033 was associated with increased muscle activity. [1]
2. In female rats, LGD-3033 administration resulted in increased muscle weight. [2]
3. In cancer patients with muscle wasting, LGD-3033 consistently increased lean body mass and improved physical function and quality of life. [3]
4. In healthy men, LGD-3033 increased lean muscle mass and improved functional measures. [4]
5. In patients with muscle wasting, LGD-3033 increased lean muscle mass without any adverse side effects. [5]
6. In cancer patients with muscle wasting, it improved muscle mass and strength, thereby allowing the subjects to undergo more intensive treatments such as radiation and chemotherapy. [6]

Maintains Bone Strength and Quality

LGD-3033 has been shown to improve bone health by preventing bone loss and increasing bone formation:

1. In female rats, combination therapy with LGD-3033 and alendronate may be helpful in treating osteoporosis. [7]
2. In men and women, SARMs were shown to have beneficial effects on osteoporosis. [8]
3. A study showed that SARMs can both prevent bone loss and stimulate bone formation. [9]
4. In patients with osteoporosis, SARMs such as LGD 3033 increased bone mineral density (BMD). [10]
5. In preclinical models, LGD-3033 increased BMD and bone strength at various skeletal sites. [11]
6. In rats, the administration of LGD 3033 promoted bone growth and prevented bone breakdown. [12-15]
7. In animal models, LGD-3033 accelerated the healing of bone injuries. [16]

LGD-3033 – Improves Sexual Function

A number of studies suggest that LGD 3033 can help treat sexual dysfunction:

1. In female rats, it was shown that LGD-3033 can stimulate female sexual behavior. [17]
2. A study showed that SARMs increased sexual motivation in rats who had surgical removal of the ovaries. [18]
3. In women, LGD-3033 enhanced libido and other parameters of sexuality. [19]
4. In rats, LGD-3033 enhanced the sexual preference of females for males. [20]
5. In female rats who had surgical removal of the ovaries, LGD-3033 increased sexual motivation. [21]
6. In female rats, LGD 3033 administration stimulated sexual behavior. [22]
7. In male rats, LGD-3033 and other SARMs improved mounts, intromissions, ejaculations, and copulation efficiency. [23]
8. In castrated rodent models, LGD-3033 appears to maintain male reproductive behavior. [24]

Decreases Urinary Tract Infections

LGD-3033 has also been shown to combat certain infections such as UTI:

1. In rats, it was shown that SARMs were effective in treating stress urinary incontinence (SUI). [25]
2. In mice who had surgical removal of the ovaries, SARMs decreased symptoms associated with stress urinary incontinence (SUI). [26]

References:

1. Vajda EG, López FJ, Rix P, Hill R, Chen Y, Lee KJ, O’Brien Z, Chang WY, Meglasson MD, Lee YH. Pharmacokinetics and pharmacodynamics of LGD-3033[9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoromethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an orally available nonsteroidal-selective androgen receptor modulator. J Pharmacol Exp Ther. 2009 Feb;328(2):663-70. doi: 10.1124/jpet.108.146811. Epub 2008 Nov 18. PMID: 19017848.
2. Vajda EG, Hogue A, Griffiths KN, Chang WY, Burnett K, Chen Y, Marschke K, Mais DE, Pedram B, Shen Y, van Oeveren A, Zhi L, López FJ, Meglasson MD. Combination treatment with a selective androgen receptor modulator q(SARM) and a bisphosphonate has additive effects in osteopenic female rats. J Bone Miner Res. 2009 Feb;24(2):231-40. doi: 10.1359/jbmr.081007. PMID: 18847323.
3. Dalton JT, Taylor RP, Mohler ML, Steiner MS. Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer. Current opinion in supportive and palliative care. 2013; 7(4):345-51.
4. Retrieved from http://www.biotechduediligence.com/uploads/6/3/6/7/6367956/lgnd_sarm_poster.pdf
5. Chekler E. L.. Tissue selective androgen receptor modulators (SARMs): A path to a clinical candidate. Abstracts of Papers, 250th ACS National Meeting & Exposition, Boston, MA, United States, August 16–20, 2015; MEDI-345.
6. Narayanan R, Mohler ML, Bohl CE, Miller DD, Dalton JT. Selective androgen receptor modulators in preclinical and clinical development. Nuclear Receptor Signaling. 2008;6:e010. doi:10.1621/nrs.06010.
7. Vajda EG, Hogue A, Griffiths KN, Chang WY, Burnett K, Chen Y, Marschke K, Mais DE, Pedram B, Shen Y, van Oeveren A, Zhi L, López FJ, Meglasson MD. Combination treatment with a selective androgen receptor modulator q(SARM) and a bisphosphonate has additive effects in osteopenic female rats. J Bone Miner Res. 2009 Feb;24(2):231-40. doi: 10.1359/jbmr.081007. PMID: 18847323.
8. Narayanan R, Mohler ML, Bohl CE, Miller DD, Dalton JT. Selective androgen receptor modulators in preclinical and clinical development. Nucl Recept Signal. 2008;6:e010. doi:10.1621/nrs.06010.
9. Rosen J, Negro-Vilar A. Novel, non-steroidal, selective androgen receptor modulators (SARMs) with anabolic activity in bone and muscle and improved safety profile. J Musculoskelet Neuronal Interact. 2002 Mar;2(3):222-4. PMID: 15758439.
10. Cilotti A, Falchetti A. Male osteoporosis and androgenic therapy: from testosterone to SARMs. Clinical Cases in Mineral and Bone Metabolism. 2009;6(3):229-233.
11. Miner JN, Chang W, Chapman MS, et al. An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on the prostate. Endocrinology.
12. Kearbey JD, Gao W, Fisher SJ, Wu D, Miller DD, Dalton JT. Effects of selective androgen receptor modulator (SARM) treatment in osteopenic female rats. Pharmaceutical research. 2009; 26(11):2471-7.
13. Gao W, Reiser PJ, Coss CC, Phelps MA, Kearbey JD, Miller DD, Dalton JT. Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats. Endocrinology. 2005;146:4887–4897.
14. Gao W, Reiser PJ, Kearbey JD, Phelps MA, Coss CC, Miller DD, Dalton JT. Effects of Novel Selective Androgen Receptor Modulator (SARM) on Skeletal Muscle Mass and Strength in Castrated Male Rats. The Endocrine Society; New Orleans: 2004.
15. Kearbey JD, Gao W, Narayanan R, Fisher SJ, Wu D, Miller DD, Dalton JT. Selective Androgen Receptor Modulator (SARM) treatment prevents bone loss and reduces body fat in ovariectomized rats. Pharmaceutical research. 2007;24:328–335.
16. Seeman E. Periosteal bone formation–a neglected determinant of bone strength. The New England journal of medicine. 2003; 349(4):320-3.
17. Kudwa AE, López FJ, McGivern RF, Handa RJ. A selective androgen receptor modulator enhances male-directed sexual preference, proceptive behavior, and lordosis behavior in sexually experienced, but not sexually naive, female rats. Endocrinology. 2010 Jun;151(6):2659-68. doi: 10.1210/en.2009-1289. Epub 2010 Apr 14. PMID: 20392832.
18. Negro-Vilar A. Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium. The Journal of clinical endocrinology and metabolism. 1999; 84(10):3459-62.
19. Kudwa AE, López FJ, McGivern RF, Handa RJ. A selective androgen receptor modulator enhances male-directed sexual preference, proceptive behavior, and lordosis behavior in sexually experienced, but not sexually naive, female rats. Endocrinology. 2010; 151(6):2659-68. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/20392832.
20. Jones A, Hwang DJ, Duke CB. Nonsteroidal selective androgen receptor modulators enhance female sexual motivation. The Journal of pharmacology and experimental therapeutics. 2010; 334(2):439-48.
21. Retrieved from https://academic.oup.com/endo/article/151/6/2659/2456825.
22. Miner JN, Chang W, Chapman MS. An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on the prostate. Endocrinology. 2007; 148(1):363-73. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17023534.
23. Miner JN, Chang W, Chapman MS, Finn PD, Hong MH, Lopez FJ, Marschke KB, Rosen J, Schrader W, Turner R, van Oeveren A, Viveros H, Zhi L, Negro-Vilar A. An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on the prostate. Endocrinology. 2007;148:363–373.
24. Jones A, Hwang DJ, Duke CB 3rd, He Y, Siddam A, Miller DD, Dalton JT. Nonsteroidal selective androgen receptor modulators enhance female sexual motivation. J Pharmacol Exp Ther. 2010 Aug;334(2):439-48. doi: 10.1124/jpet.110.168880. Epub 2010 May 5. PMID: 20444881; PMCID: PMC2913771.
25. Kadekawa K, Kawamorita N, Shimizu T, Kurobe M, Turnbull PS, Chandra S, Kambara T, Barton JC, Russell AJ, Yoshimura N. Effects of a selective androgen receptor modulator (SARM), GSK2849466A, on stress urinary incontinence and bladder activity in rats with ovariectomy-induced oestrogen deficiency. BJU Int. 2020 Jun;125(6):911-919. doi: 10.1111/bju.15022. Epub 2020 Mar 20. PMID: 32011085; PMCID: PMC7261644.
26. Miller CP, Shomali M, Lyttle CR, et al. Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Medicinal Chemistry Letters. 2011;2(2):124-129. doi:10.1021/ml1002508. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018048/.