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Galapagos chooses molecule for cachexia trial
05 Jan 2009
Pharmaceuticals firm Galpagos has chosen a candidate drug to enter trials for the treatment of a weight loss disease.

LGD-3303 - SARMs Profile

lgd-3303 Sarm Structure

Family: Selective Androgen Receptor Modulator

Half Life: About 2.5 – 5 hours

Formula: Unpublished

Chemical Structure: Unpublished

Anabolic Rating: Equal to Testosterone Propionate 

Facts:  

Selective androgen receptor modulators (SARMs) are a relatively new class of molecules that were developed to maintain the beneficial effects of androgens such as testosterone (increased muscle mass, bone density, etc…) with significantly reduced side effects. At this stage of development, the pharmacokinetic/pharmacodynamic mechanisms and properties have not fully been elucidated.  

In a castrated (and therefore androgen deficient) rodent, LGD-3303 was shown to have potent activity on the levator ani muscle (a measure of the anabolic effect), with some slight stimulatory effects on the ventral prostate preputial gland. The stimulatory effect that it did have on the prostate did not increase weight or size to the level of the non-castrated (androgen intact) control group of rodents (1). Interestingly, there was a much greater muscular hypertrophic activity relative to prostate activity but local tissue concentrations were actually higher in the prostate than the muscle. It has been speculated that primary mechanism for tissue selective activity was as a result of altered molecular interactions at the level of the androgen receptor (1). 

Again, it is important to note that this compound is still in the very early stages of research and development and there are few published and peer-reviewed medical journal articles that address LGD-3303 in detail.  

In another LGD-3303 study, this one on female rodents (ovaries removed) and male rodents (testes removed), treated with LGD-3303, it was again shown to be a potent SARM with anabolic effects on muscle and cortical bone (2). Research indicates that it has the potential to be more effective than Fosamax (R) (an osteoporosis medication) at increasing bone mineral density in the femur and spine, by the deposition of new bone in those areas (3). It appears to me, at this early stage of development that it is going to be primarily marketed as a treatment for osteoporosis, as the company has primarily been touting its effects on bone mineral density.  

Still, at a 1mg/kg/day dose, LGD-3303 was able to combat androgen-deficiency related muscle wasting (1), without a commensurate increase in prostate size or noteworthy effect on luteinizing hormone.  

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Practical Use: This SARM can be used effectively for osteoporosis or androgen replacement therapy, by both men and women. As a performance enhancing drug, it shows great potential, as increasing the dose above the therapeutic range has been shown in studies to greatly increase muscle size.

Side Effects: Side effects with this compound would likely be unnoticeable except in cases of extremely high doses.

Used By: This compound is still in the developmental stages, and I am unaware of any human trials as of yet.  

Typical Dose: I am speculating here, but 1mg/kg/day would be enough to constitute an acceptable level of hormone replacement (in studies it completely halted the effects of muscle wasting associated with lack of androgens in castrated rodents). Since LGD-3303 appears like it will have very few noticeable side effects, I am speculating that an increase in muscle size and strength will be realized with 1mg/kg/day, although a very strong anabolic effect would be probable with anything above that.  

Stacks Well With: This drug could replace testosterone in most cycles, and therefore would stack well with virtually anything.  

Producing/Developing Company:

1. Ligand Pharmaceuticals Incorporated 

Availability: Not yet available

Counterfeited: Not yet 

References:

  1. J Pharmacol Exp Ther. 2008 Nov 18. [Epub ahead of print]
  2. J Bone Miner Res. 2008 Oct 10. [Epub ahead of print]
  3. Ligand Announces Positive Preclinical Data on Selective Androgen Receptor Modulator LGD-3303. SAN DIEGO--(BUSINESS WIRE)--Sep 17, 2007
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