Wow..now that looks interesting!
I've been keeping one eye on the development of SARMS (Selective Androgen Receptor Modulator). It appears many of the labs are able to pin point exactly what receptors to bind to, which avoids many problems associated with regular TRT. So, you can design a SARM that has anabolic, libidio enhancing characteristics that will not effect hair loss (or may even grow hair), will not convert to estrogen, will not damage liver function, blood pressure or lipids. Also, it is ORALLY available.
here is a recent abstract:
Endocrinology. 2006 Oct 5; [Epub ahead of print] Links
An Orally-Active Selective Androgen Receptor Modulator is Efficacious on Bone, Muscle and Sex Function with Reduced Impact on Prostate.
* 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.
Research and Development, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121; NIEHS/NIH - Environmental Diseases & Medicine Program, Research Triangle Park, NC; Metabasis Therapeutics, Inc. 11119 North Torrey Pines Rd., La Jolla, CA 92037; Department of Nutrition and Exercise Sciences, Oregon State University, 127 Milam Hall, Corvallis, OR 97331.
A number of conditions, including osteoporosis, frailty and sexual dysfunction in both men and women have been improved using androgens. However, androgens are not widely used for these indications because of the side effects associated with these drugs. We describe an androgen receptor ligand that maintains expected anabolic activities with substantially diminished activity in the prostate. LGD2226 is a non-steroidal, non-aromatizable, highly selective ligand for the androgen receptor (AR), exhibiting virtually no affinity for the other intracellular receptors. We determined that AR bound to LGD2226 exhibits a unique pattern of protein-protein interactions compared with testosterone, fluoxymesterone (an orally available steroidal androgen) and other steroids, suggesting that LGD2226 alters the conformation of the ligand binding domain (LBD). We demonstrated that LGD2226 is fully active in cell-based models of bone and muscle. LGD2226 exhibited anabolic activity on muscle and bone with reduced impact on prostate growth in rodent models. Biomechanical testing of bones from animals treated with LGD2226 showed strong enhancement of bone strength above sham levels. LGD2226 was also efficacious in a sex behavior model in male rats measuring mounts, intromissions, ejaculations and copulation efficiency. These results with an orally-available, non-aromatizable androgen demonstrate the important role of the androgen receptor and androgens in mediating a number of beneficial effects in bone, muscle and sexual function independent from the conversion of androgens into estrogenic ligands. Taken together, these results suggest that orally-active, non-steroidal SARMs may be useful therapeutics for enhancing muscle, bone and sexual function.
PMID: 17023534 [PubMed - as supplied by publisher]
Wow..now that looks interesting!
...keeps fingers crossed it live up to the hype...........
probably wont be for a while....
its about time, they have had the AR's mapped forever.
I believe GTx, Inc. "The Men's Health Biotech Company." ticker: GTXI owns this patent. They also make FARESTON (which may be familiar to some of you) and ACAPODENE. I own the stock and it's been doing well.The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
OSTARINE will be the name of the muscle-wasting SARM.
Where can i get some?
Do you know why GTx is limiting the application of ostarine to "muscle wasting" and treatment of sarcopenia in aging males? You would think that treat of hypogonadism/andropause would have a larger market.
Originally Posted by blackheart
I wouldn't rule additional applications of this drug out (Another reason why I continue to like the stock). But if you breeze through the patent document, you'll see that they have included a large number of potential drugs within the scope of the patent, focused on various applications. It's possible that there's something better than OSTARINE in there, but I am not qualified to say. ACAPODENE is intended both for the Treatment for the side effects of Androgen Deprivation Therapy (I believe it may become to SERM of choice for athletes) and for Prevention of prostate cancer in men.Originally Posted by Random987
(for some reason i cannot post a linked image, but see the attached graphic)Selective Androgen Receptor Modulators (SARMs)
A selective androgen receptor modulator, or SARM, is a small molecule that binds to and selectively modulates androgen receptors depending on tissue type. In men, SARMs may be able to:
* Stimulate testosterone's beneficial action in bone, muscle and brain
* Block testosterone's harmful action in the prostate and skin
* Either cross or not cross into the central nervous system to affect lipids
Because of these properties, we believe SARMs could be developed to treat a range of medical conditions and physiological functions, including:
if you find some, let me know!Originally Posted by CHAPS
Yeah, it almost seems like they can make it a designer drug, you want muscle building, pro-sexual effects, hair gain, no aramotase, and orally available, come on down.
Might be hard to get past the FDA. Somewhat like the Melanotan battle, the drug that tans you, helps out sexual and may cause you to lose weight. They felt they needed to split it up to get approval. Too many effects.
Originally Posted by blackheart
anything that can change the health of someone for the better in more ways than one will always be controlled. Why is that they keep things that can be good for us out of our hands? Its not like tylenol or any other OTC drug cant be abused...They just make more profit from selling it with prescription only. But again we have to look at all the benefiets of this SARM and know that there has to be a gang of sides to come along with it, unless its the perfect male drug.
.......but patent expires............Originally Posted by pistonpump
I could start a whole thread about the pharma industry....Originally Posted by pistonpump
acapodene = toremifene citrate?
dat sounds very familiar!
Indeed, the same compound is marketed as FARESTON in the US for treatment of advanced breast cancer and is in phase III trials for Adrogen Deprivation Therapy and Prostate Cancer under the ACAPODENE name.Originally Posted by faustus
personally i am not too impressed with these compounds...it seems the main point of their creation is to provide the bone strengthening and muscle sustaining effects of steroids without the effect on cholesterol and androgenic side effects. this is sounds useful for cancer or aids...but not for bodbuilders
i love androgenic compounds, their effect on muscle hardness, strength, and agression are benefeits in my eyes, and i willingly accept the acne and truckloads of saw palmeto i need to buy to control benign prostate hypertophy.
also it states they are being considered for use as a form of male birth control, so they are obviously supressive. we already have primarily anabolic compounds such as anavar and primabolan, i am sure SARMS will prove a useful addition to an athletes/bodybuilder's arsenal, but i highly doubt they will replace conventional anabolic/androgenic steroids.
give me a SARM that doesnt raise my cholesterol, doesnt give me acne, doesnt supress me, doesnt make my prostate grow, improves my bone structure, aromatizes in the perfect amount, and gives me the mass building effects of m1t combined with the muscle hardness of tren or masteron and ill be impressed.
How and why:Originally Posted by Random987
A likely explanation as to how these synthetic ligands act
as agonists or antagonists is related to their ability to induce
specific conformational changes in AR. The AR ligand
binding domain is composed of 12 alpha-helices. In the
crystal structure, relatively few amino acid residues were
found to interact directly with the steroidal agonists, DHT
and methyltrienolone (R1881). Most of these residues
are hydrophobic in nature and interact with hydrophobic
moieties in the ligand, whereas fewer residues are hydrophilic
and may form hydrogen bonds with polar atoms in the
ligand. In the case of nonsteroidal ligands, AR binding is
likely to be influenced by stereoisomeric conformation and
steric and electronic effects. It remains to be determined
whether the same amino acids in the ligand binding pocket
interact with both steroidal and nonsteroidal ligands. As
evidenced by structure-function studies of nonsteroidal ligands,
minor differences in ligand structure can lead to either
agonist or antagonist activity. The AR can use different
transactivation domains, AF-1 and AF-5 in the amino-terminal
domain and AF-2 in the carboxy-terminal domain
.The AF-2 function is strongly dependent upon interaction
with nuclear receptor coactivators, whereas strong
agonist, but not antagonist, binding induces ligand-dependent
interaction internally between the AF-2 and AF-1 domains
. When steroid agonists bind to AR, helix 12
containing the AF-2 region in the ligand binding domain
closes over the binding pocket revealing an interface for
coactivator interaction. Conversely, binding of antagonists
maintains helix 12 in an open conformation directed away
from the binding pocket. Therefore, tissue selectivity of
action may depend upon ligand-induced
AR conformation and recruitment of a tissue-specific repertoire
of coregulatory factors that function as coactivators corepressors.
Steroid Receptor Coactivators - Cutting Edge Muscle Forums
Steroid Receptor Coactivators
Selective Agonist Receptor Modulators - Cutting Edge Muscle Forums
Selective Agonist Receptor Modulators
I think the advantages would be that it is orally available (no shots or gels), doesn't aramotize, doesn't convert to DHT, doesn't affect fertility, etc. In other words, it is more selective in its effects (sledgehammer v. scapel). It wouldn't be as much of a balancing act.
From the journal cited above:
Given the FDA, I don't believe we would get to this level in the near future, but wouldn't it make your job easier, if you could "design" a specific SARM for a particular patient, i.e. Jim wants anabolic effects, but doesn't want kids. John want anabolic effects, but wants kids, etc, etc.As shown in Figure 3, S-
4 acted as a full AR agonist in the levator ani muscle, as indicated its
ability to fully maintain the muscle to that of control level. However,
S-4 acted as a partial agonist in the prostate (Emax = 35% of control
values), indicating that S-4 was potent and efficacious in anabolic
tissues but not in androgenic tissues. In contrast, castrated rats
treated with testosterone propionate had near identical, and nonselective
growth of the prostate and levator ani muscle as compared
to control animals.
Originally Posted by Dr. John