# OSTA Rx -- SARM



## heavyiron (Apr 5, 2012)

*OSTA Rx -- SARM*

*Selective Androgen Receptor Modulator (SARM)* 








*-Non-hormonal Anabolic Compound*
-Increases Lean Muscle Mass
-Promotes Fat Loss
-Promotes Recovery
-Increases Libido
-Safe for Males & Females
-Can be used for PCT and Bridging  

*IronMagLabs Bodybuilding Supplements & Prohormones: Osta Rx*


*(MK-2866) ~ ((2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide) * 







Osta Rx??? is a Selective Androgen Receptor Modulator. A SARM is exactly  what it sounds like: a compound (not an anabolic steroid) which has the  ability to stimulate the androgen receptor (much the same way as  anabolic steroids). Osta Rx??? is an orally active (and highly  bioavailable) selective agonist for androgen receptors which was shown  to have anabolic effects in muscle and bone tissue. It has been shown to  have no measurable effect on lutenizing hormone (LH) or  follicle-stimulating hormone (FSH), but it has been shown to have some  effect on prostate weight, with an androgenic potency around 1/3rd of  its anabolic potency. Still, this is a good trade-off, because it???s  anabolic effect has been measured to be roughly the same as  testosterone. It has also been shown to produce dose-dependent increases  in bone mineral density and mechanical strength in addition to being  able decrease body fat and
increase lean body mass.    
	

	
	
		
		

		
		
	


	




Selective androgen receptor modulators (SARMs) bind to the androgen  receptor and demonstrate osteo (bone) and myo (muscular) anabolic  activity. Binding and activation of the Androgen receptor alters the  expression of genes and increases protein synthesis, hence builds  muscle. So in essence, SARMs such as Osta Rx??? causes muscle growth in  the same manner as steroids, however unlike testosterone and other  anabolic steroids and prohormones, SARMs (as nonsteroidal agents) don???t  produce the growth effect on prostate and other secondary sexual organs. 

Osta Rx??? in particular exerts its anabolic effects on muscle tissue  almost exclusively. So not only does it represent a new potential  treatment option for a wide spectrum of conditions from muscle wasting  diseases (from age-related to AIDS or cancer-related), but is also has  immense potential for muscle building for Bodybuilders, fitness,  athletes and an agent to minimize atrophy during recovery periods from  serious surgery or similar situations. 
*
Support Ingredients in Osta Rx???*

*Mucuna Pruriens* ~ contains a very powerful  neurotransmitter pre-cursor L-Dopa. Mucuna pruriens is a reputed remedy  of Ayurveda in nervous and sexual diseases. Traditionally, Mucuna  pruriens is commonly used as carminative, hypertensive and hypoglycemic  agent. Mucuna pruriens has been found to contain L-DOPA, 40 mg/g of the  plant. The plant/seeds contain the bioactive alkaloids mucunine,  mucunadine, mucuadinine, pruriendine and nicotine, besides B-sitosterol,  glutathione, lecithin, oils, venolic and gallic acids. Studies in  experimental model show L-Dopa also helps in the reduction of  cholesterol and blood sugar levels. 

*L-Dopa* is an amino acid that converts into dopamine.  Dopamine is an essential component of our body and it's required for  proper functioning of the brain.  Research discovered the body converts  the amino acid tyrosine into L-dopa; L-dopa is then converted into  dopamine. Without the neurotransmitter dopamine to serve a damping  effect on neural transmissions, muscles become tense and tremble. 

*Benefits of Mucuna Pruriens L-Dopa:* 

    -Improved sleep (promotes deep sleep)
    -Reduced bodyfat & decreased cellulite
    -Improved skin texture & appearance
    -Increased bone density and reversal of osteoporosis
    -Increased lean muscle mass
    -Improved mood and sense of well-being
    -Enhanced libido & sexual performance
    -Increased energy levels
    -Improved cholestorol profile & regeneration of organs (heart, kidney, liver, lungs)
    -Dramatically strengthens immune system 

*Mucuna: Human Growth Hormone* 

L- Dopa contains natural secretagogues which may support the body's  ability to stimulate the natural release of growth hormone. The blood  carries the dopamine into the brain, where it naturally increases HGH  production from the pituitary gland. The increased dopamine levels also  optimize the production of other hormones, including testosterone,  leading to increased sex drive and improved sexual performance for both  men and women,  beneficial in stimulating muscle growth, as well as  burning fat from fat cells.   

*Fenuside *~ is a testosterone booster containing  Fenuside saponins, extracted from the herb Fenugreek (Trigonella  foenum-graecum). Fenuside is designed to boost testosterone levels,  muscle size and sex drive, and is considered one of the very latest  testosterone boosters in the sports supplement market. It is important  to note that there are over 100 natural chemicals in Fenugreek, but it's  only standardised Fenuside saponins that are proven to offer  bodybuilders, gym users and athletes beneficial effects on muscle size,  testosterone levels and body composition. 

The fenuside saponins found in Fenuside are designed to support hormone  levels and act as a powerful but safe testosterone booster in  individuals desiring fast and noticeable enhancements in muscle size,  strength and performance. The supplement is useful for strength and  power athletes, body builders, and serious gym users. 

Research suggests that Fenuside mechanism of action is initially as an  adrenal cortex stimulator, subsequently activating the hypothalamus and  boosting natural production of corticotropin releasing hormone (CRH).  CRH switches on the powerful pituitary gland, enhancing production of  the key adrenocorticotrophin hormone (ACTH). ACTH is a potent stimulant  on the adrenal cortex to increase androgen synthesis. Because androgens  are precursors to Testosterone and possess "Testosterone like activity",  Testofen naturally supports the activity of the luteinizing hormone,  acting as a testosterone booster. 

*Horny Goat Weed* ~ Icariin is the active element of  Epimedium Extract (also commonly known as Horny Goat Weed Extract) and  this ingredient when extracted to high purity's is an exceptionally  powerful nitric oxide and testosterone booster. Icariin is a very fine  grade of extract and boasts quality's which simply can't be obtained  from the lower grade's of Epimedium Extract. The increased blood flow  and oxygen to the muscles obtained from Icariin of this quality feeds  the body with the energy and the drive required to perform and  out-perform when under activities of physical and mental endurance.


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## ~RaZr~ (Apr 5, 2012)

Heavy, you going to try it?


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## heavyiron (Apr 5, 2012)

I will definitely try it. I'm thinking of adding it to my wife's Halo for Her stack as well.


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## ~RaZr~ (Apr 5, 2012)

Good deal 

At least this way, other females will be able to see how it works. I does look VERY promising.


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## _LG_ (Apr 5, 2012)

Heavy,
What is your opinion on the possibilities of this being suppressive?


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## Vibrant (Apr 5, 2012)

Heavy, why do you guys say that it can be used for pct and bridging?

Patrick arnold says ostarine is suppressive, therefore wouldn't it be bad for pct?


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## heavyiron (Apr 5, 2012)

Some history and performance data;


*GTx, Inc. Announces Positive Clinical Results and Development Plans for Ostarine*

PRNewswire-FirstCall
Sept. 7 05

GTx, The Men's Health Biotech Company, announced today that results from  its Phase I clinical trials for ostarine, its second selective androgen  receptor modulator (SARM), were consistent with anabolic activity  without evidence of unwanted androgenic side effects on prostate and  skin sebaceous glands. GTx intends to begin a Phase II clinical trial of  ostarine for the treatment of muscle wasting associated with burns  during the fourth quarter of 2005.

"We are excited with the outcome of our Phase I clinical trials of  ostarine. Now that ostarine is poised to enter Phase II clinical trials,  it becomes our lead SARM compound," said Mitchell Steiner, MD, chief  executive officer of GTx.

"Results from our recently completed multiple-ascending dose clinical  trial have allowed us to pick doses of ostarine to advance into Phase II  clinical trials. We have also zeroed in on developing ostarine for  muscle wasting associated with an acute condition, burns, for which we  believe ostarine fills an unmet medical need and which may provide us  with an efficient path to market.

We remain excited by other, broader market possibilities for ostarine,  such as muscle wasting associated with andropause, and we intend to  initiate a second Phase II clinical trial of ostarine for this  indication in the first half of 2006."

About Ostarine

Ostarine is a non-steroidal, oral SARM, all rights to which are held by  GTx. GTx believes that ostarine has the potential to treat muscle  wasting associated with chronic conditions, such as end-stage renal  disease, frailty and andropause, as well as muscle wasting associated  with acute conditions, such as burns.

Ostarine is the second SARM that GTx has brought from discovery into  clinical trials. GTx also discovered andarine, a SARM that GTx and its  collaborator, Johnson & Johnson's subsidiary, Ortho Biotech Products  L.P., are developing to treat cancer cachexia.

Planned Phase II Clinical Trials for Ostarine

GTx plans to initiate Phase II clinical trials of ostarine first for  muscle wasting associated with burns because acute indications have a  relatively expeditious and defined clinical development and regulatory  pathway. Burn patients are hypermetabolic and lose significant lean body  weight, which adversely affects their healing and recovery.

GTx expects to begin its Phase II clinical trial of ostarine for muscle  wasting associated with burns in the fourth quarter of 2005. Studies  have already established proof-of-concept for the use of anabolic agents  in the treatment of burns. Because ostarine has a long half life (24  hours) and provides levels of circulating androgens unattainable with  anabolic steroidal agents, GTx believes that this selective, potent,  non-steroidal anabolic agent would be an important step forward in the  treatment of burn patients.

"We believe that the treatment of burn patients represents an excellent  first path for GTx to pursue for ostarine," said Dr. Steiner. "A  powerful anabolic agent without unwanted steroidal side effects could  help speed the recovery of burn victims. For GTx, the treatment of burn  patients offers a relatively expeditious route to market for its lead  SARM."

GTx plans to continue clinical development of ostarine for chronic  muscle wasting due to low testosterone in aging men (a condition also  known as andropause). Between 30 and 60 years of age, men on average  gain a pound of fat and lose a half pound of muscle, and muscle loss  accelerates after age 60. This loss of muscle mass can lead to frailty  and loss of independence. GTx plans to initiate Phase II clinical  testing for the treatment of andropause during the first half of 2006.

About Ostarine's Phase I Multiple Ascending Dose Clinical Trial Results

The Phase I multiple-ascending dose clinical trial evaluated the safety,  tolerability and specific pharmacodynamic characteristics of ostarine  in a double-blind, placebo-controlled study in 48 healthy male  volunteers, 18-45 years of age, and 12 elderly males with truncal  obesity, who averaged 68 years of age.

Safety and pharmacodynamic measurements were taken at the beginning of  the study and after 14 days of daily oral dosing. These measurements  included routine blood chemistry and hematology, sex hormones and  gonadotropins, serum prostate specific antigen, metabolic markers of  bone and muscle, cutaneous sebum analysis and DEXA scanning for body  composition.

Ostarine is designed to have anabolic building activity without unwanted  androgenic side effects on prostate and skin sebaceous glands. Overall,  clinical laboratory values and hormonal effects determined from the  study were consistent with anabolic activity. Comparisons of DEXA  assessments from the beginning of the study to DEXA assessments after 14  days showed positive changes in body composition, with lean body mass  and fat mass in study patients moving in a direction consistent with  anabolic activity.

Based on other tests, ostarine did not appear to have unwanted side  effects on the prostate or the skin. GTx believes that these  observations support the potential ability of ostarine to selectively  modulate androgen receptors in a tissue-specific manner.

There were no drug-related serious adverse events related to ostarine in  the clinical trial. Doses that were found to be safe in this study were  selected to enter Phase II testing later this year.

About GTx

GTx is a biopharmaceutical company dedicated to the discovery,  development and commercialization of therapeutics for cancer and serious  conditions related to men's health. GTx's lead drug discovery and  development programs are focused on small molecules that selectively  modulate the effects of estrogens and androgens, two essential classes  of hormones.

GTx, headquartered in Memphis, Tenn., currently has four clinical programs.

GTx is developing ACAPODENE(R) (toremifene citrate), a selective  estrogen receptor modulator, or SERM, in two separate clinical programs  in men: (1) a pivotal Phase III clinical trial for the treatment of  serious side effects of androgen deprivation therapy for advanced  prostate cancer and (2) a pivotal Phase III clinical trial for the  prevention of prostate cancer in high risk men with precancerous  prostate lesions.

In its third clinical program, GTx is developing ostarine for the  treatment of muscle wasting associated with acute conditions such as  burns and chronic conditions such as andropause. GTx expects to begin  Phase II clinical trials of ostarine for muscle wasting associated with  burns in the fourth quarter of 2005 and for andropause during the first  half of 2006.

In its fourth clinical program, GTx and its collaborator, Ortho Biotech  Products, L.P., a subsidiary of Johnson & Johnson, are developing  andarine, another one of GTx's SARMs, for the treatment of cancer  cachexia. GTx is working with Ortho Biotech to plan a Phase II clinical  trial of andarine.


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## heavyiron (Apr 5, 2012)

*GTX Inc. Starts Ostarine Mid-Stage Trial
*
AP
May 15, 2006
Chron.com

MEMPHIS, Tenn. ? Biotech company GTX Zoek Inc. said Monday it has  initiated a mid-stage trial of ostarine Zoek for the treatment of  osteoporosis.

Neo-androgeen

The trial will evaluate the drug's safety and its ability to build  muscle and promote bone in 120 elderly men and postmenopausal women.

Ostarine, a first-in-class drug, is a selective androgen receptor  modulator, or SARM. Zoek In preclinical trials, ostarine distinguished  itself from current osteoporosis drugs which only treat bone loss by  also increasing muscle.

Mitchell S. Steiner, Zoek chief executive of GTX, said "The clinical  data will determine ostarine's novel anabolic effects and tissue  selectivity. These data will support further development of ostarine for  acute muscle-wasting indications such as cancer, end-stage renal  disease, or burn-injury wasting conditions, and for chronic indications  such as osteoporosis and age-related frailty."

The company, which has all rights to ostarine, expects to report clinical data in the second half of the year.

GTX develops therapeutics for cancer and serious conditions related to  men's health. Shares rose 65 cents, or 7.6 percent, to $9.20 on the  Nasdaq.


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## heavyiron (Apr 5, 2012)

*GTx Announces That Ostarine Achieved Primary Endpoint Of  Lean Body Mass And A Secondary Endpoint Of Improved Functional  Performance*

*GTx, Inc.*
_09 Dec 2006_

*GTX, the Men's Health Biotech Company,                    today announced that ostarine, a first-in-class selective                    androgen receptor modulator (SARM), met its primary endpoint                    in a Phase II proof of concept double blind, randomized,                    placebo controlled clinical trial in 120 subjects (60 elderly                    men and 60 postmenopausal women).  *

 Without a prescribed diet or                    exercise regimen, all subjects treated with ostarine had a                    dose dependent increase in total lean body mass (muscle), with                    the 3 mg cohort achieving an increase of 1.3 kg compared to                    baseline and 1.4 kg compared to placebo (p<0.001) after three                    months of treatment.  

 Treatment with ostarine also resulted in                    a dose dependent improvement in functional performance                    measured by a stair climb test, with the 3 mg cohort achieving                    a clinically significant improvement in both speed (p=0.006)                    and power (p=0.005).  

Ostarine continued to demonstrate a                    favorable safety profile, with no serious adverse events                    reported. Ostarine also exhibited tissue selectivity with                    beneficial effects on lean body mass and performance and with                    no apparent change in measurements for serum PSA (prostate),                    sebum production (skin and hair), or serum LH (pituitary)                    compared to placebo. 

The Phase II clinical trial evaluated four doses of ostarine                    (0.1 mg, 0.3 mg, 1 mg, and 3 mg) versus placebo for three                    months in 60 elderly men (average age 66 years) and 60                    postmenopausal women (average age 63 years). The trial was                    conducted in five clinical sites in the United Kingdom and                    Germany. 

*A summary of the topline data is as follows: *

-- Among females (n=56), ostarine treatment resulted in a dose                    dependent increase in LBM with the 3 mg dose having an                    increase of 1.7 kg compared to baseline and an increase of 1.4                    kg compared to placebo (p=0.02). 

                   -- Among males (n=58), treatment with a 1 mg dose of ostarine                    resulted in a LBM increase of 0.7 kg compared to baseline and                    an increase of 1.2 kg compared to placebo (p=0.03), and                    treatment with a 3 mg dose of ostarine resulted in an increase                    of 1.0 kg compared to baseline and an increase of 1.4 kg                    compared to placebo (p=0.005). 

                   -- Total tissue percent fat decreased compared to placebo in a                    dose dependent fashion and achieved statistical significance                    at the 1 mg dose (p=0.02) and 3 mg dose (p=0.006) of ostarine.  

Total fat mass was lower in subjects receiving either the 3 mg                    or 1 mg ostarine dose, although not at a statistically                    significant level (p = 0.08 for both doses). For subjects                    receiving the 3 mg ostarine dose, total fat on average                    declined 0.6 kg compared to placebo.  

 The site of fat loss                    differed among male and female subjects, with males losing fat                    primarily from the trunk and abdomen, and females losing fat                    primarily from the thighs and legs. 

-- In this short trial, ostarine had no apparent effect on                    bone mineral density, and bone turnover markers results were                    mixed. In preclinical in vitro and in vivo models, ostarine                    demonstrated both anabolic and antiresorptive activity on                    bone. A longer clinical study is necessary to demonstrate the                    actual effects of ostarine on bone. 

                   -- Ostarine continued to demonstrate a favorable safety                    profile, with no serious adverse events reported. 

                   -- At the end of three months, no subject had clinically                    meaningful levels in liver enzyme tests. However, one female                    discontinued the study per protocol due to elevated liver                    enzymes which returned to baseline. 

                   -- Ostarine treatment resulted in a dose dependent decrease in                    both LDL and HDL cholesterol levels, with the average LDL/HDL                    ratio for all doses tested remaining in the low cardiovascular                    risk category. 

-- Ostarine treatment resulted in no apparent effect on serum                    PSA (prostate), sebum production (skin and hair), *or serum LH                    (pituitary). *


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## Curt James (Apr 5, 2012)

heavyiron said:


> *GTX Inc. Starts Ostarine Mid-Stage Trial
> *
> AP
> May 15, *2006 *(snip)
> ...



Was curious where they were as far as the Nasdaq was concerned some six years later. 

Looks like $3.85.



*Last Sale:*$ 3.85Change Net/%:0.09 
	

	
	
		
		

		
		
	


	




 2.39%Best Bid /Ask:N/A / N/A1 Year Target:6Today's High/Low:$ 3.92 / $ 3.62Share Volume:291,64650 Day Avg. Daily Volume804,280Previous Close:$ 3.76*52 Week High */Low:*$ 6.864* / $ 2.34


From *GTXI stock quote - GTx, Inc. stock price - NASDAQ.com*

Also found this:

*enobosarm (Ostarine®; GTx-024)*

enobosarm is an oral selective androgen receptor modulator that GTx is developing for the prevention and treatment of muscle wasting in patients with non-small cell lung cancer.

*About Muscle Wasting, a Common Cancer Related Symptom
*
Muscle wasting is a common cancer related symptom which can begin early in the course of a patient’s malignancy resulting in decline in physical function and other detrimental clinical consequences. Muscle wasting and muscle weakness are also side effects of many chemotherapy drugs. There are no drugs approved for the prevention and treatment of muscle wasting in patients with cancer.

At diagnosis, approximately 50% of advanced non-small cell lung cancer (NSCLC) patients have severe muscle loss, and approximately 70% of these patients will lose muscle before death. Muscle weakness and functional limitations are highly prevalent, with 88% of NSCLC patients reporting difficulty climbing stairs, lifting and carrying 10 lbs, walking a quarter mile, or stooping, crouching or kneeling. Muscle loss is a predictor of performance status, tolerability to cancer treatment, progression free survival and overall survival. Limitations in physical function predict the ability of a NSCLC patient to tolerate chemotherapy, and patients with functional limitations are less likely to be offered treatment. Functional status is also a predictor of survival.

To date, GTx has evaluated enobosarm in eight clinical trials involving approximately 600 subjects including three efficacy studies. A four month Phase IIb enobosarm clinical trial enrolled 159 patients with NSCLC, colorectal cancer, breast cancer, non-Hodgkin’s lymphoma, or chronic lymphocytic leukemia. *The study met its primary endpoint of absolute change in total lean body mass (muscle) compared to placebo and the secondary endpoint of muscle function (performance). *The incidence of serious adverse events, deaths and tumor progression were similar among placebo and the treatment arms. The most common side effects reported among all subjects in the trial were fatigue, anemia, nausea and diarrhea.

From *GTx, Inc. enobosarm (Ostarine® or GTx-024) : Preventing and Treatment Muscle Wasting in Lung Cancer Patients*


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## Deity (Apr 5, 2012)

Will this hinder the effectiveness of gains in the next blast if taken on a bridge. I guess what I'm saying is will it cause an increase in myostatin levels?


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## heavyiron (Apr 6, 2012)

Little Guy said:


> Heavy,
> What is your opinion on the possibilities of this being suppressive?



At the doses tested no effect on serum LH was seen in the results but higher doses may cause suppression.


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## thebeastijwc (Apr 11, 2012)

what would be a good mg to run for standalone? kinda want to try this out


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## Arnold (Apr 11, 2012)

thebeastijwc said:


> what would be a good mg to run for standalone? kinda want to try this out



don't exceed 3 caps daily (20mg).


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## withoutrulers (Apr 11, 2012)

This looks extremly promising as I've run ostarine in my rats before and I've used mucuna pruriens in  conjunction with a test booster as well with great results. These things stacked together ought to be an exceptional OTC supp. IML has got some good things going on.


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## heavyiron (Apr 13, 2012)

withoutrulers said:


> This looks extremly promising as I've run ostarine in my rats before and I've used mucuna pruriens in  conjunction with a test booster as well with great results. These things stacked together ought to be an exceptional OTC supp. IML has got some good things going on.



Yeah, this is an amazing product. Can't wait to talk my wife into using it...


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## squigader (Apr 13, 2012)

Any logs out there yet on this baby? Would love to see some.


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## Vibrant (Apr 13, 2012)

squigader said:


> Any logs out there yet on this baby? Would love to see some.



I'll be doing one starting next week with bloodwork.


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## heavyiron (Apr 14, 2012)

Vibrant said:


> I'll be doing one starting next week with bloodwork.



Thank you brother


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## Hybridp (Apr 15, 2012)

heavyiron said:


> Thank you brother



PM'd you, but I did so before even realizing the date of this thread. Sorry.  Is she going to run a log? That would be awesome to see, I'd like to find some before ordering some for the girlfriend.


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## larry79 (May 21, 2012)

Why is the dosage split up 3x a day, when the half life is 24 hours ?? Couldn't I just take all 3 in the morning ?


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## heavyiron (May 21, 2012)

Hybridp said:


> PM'd you, but I did so before even realizing the date of this thread. Sorry.  Is she going to run a log? That would be awesome to see, I'd like to find some before ordering some for the girlfriend.



She isn't going to anytime soon but here is another female log;

TrishaB Osta RX log


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## heavyiron (May 21, 2012)

larry79 said:


> Why is the dosage split up 3x a day, when the half life is 24 hours ?? Couldn't I just take all 3 in the morning ?



All at once is fine.


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## larry79 (May 21, 2012)

Thanks Heavy


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## NJ-Surfer (Jun 17, 2012)

This is such a fucking joke. The Ph-1 trials are over 6 years old. Merck was the big Pharma company backing these trials and they pulled out because it doesn't work. The whole SARM mechanism has been abandoned by Pharma as it doesn't work. You're being duped by these snake oil salesmen who are buying this low quality shit from China and passing off to teenagers who think gaining 3 lbs in a month is cause for celebration. Where are the ethics with these fuckers who will do anything to earn a dollar. These fucking companies should all be shit down and these pricks thrown in jail like crack dealers.


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## girpy (Jun 17, 2012)

NJ-Surfer said:


> This is such a fucking joke. The Ph-1 trials are over 6 years old. Merck was the big Pharma company backing these trials and they pulled out because it doesn't work. The whole SARM mechanism has been abandoned by Pharma as it doesn't work. You're being duped by these snake oil salesmen who are buying this low quality shit from China and passing off to teenagers who think gaining 3 lbs in a month is cause for celebration. Where are the ethics with these fuckers who will do anything to earn a dollar. These fucking companies should all be shit down and these pricks thrown in jail like crack dealers.



Care to post up anything to back this up?


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## NJ-Surfer (Jun 18, 2012)

"*GTx Mum as Merck Discontinues Phase II SARM Ostarine/MK-2866 *
Four months after GTx Inc. suffered a devastating FDA setback with lead program toremifene, the biotech's second program - Phase II muscle loss drug Ostarine/MK-2866 - has been discontinued by partner Merck and Co. Inc. 

The news was buried deep within a 10-k Merck filed on Monday. It said the big pharma had "discontinued internal development" of Ostarine and is "discussing next steps" with GTx. 

As of press time on Thursday, GTx had yet to make its own announcement. Spokesman McDavid Stilwell told BioWorld Today the biotech would provide an update in the future, but he declined to specify when or offer any additional comment on the matter. 

Investors appear to be picking up on the news, slowly but surely. Shares of GTx (NASDAQ:GTXI) slid about 14 percent between Merck's Monday filing and the close of business Wednesday. The stock gained back 6 cents to close at $3.69 on Thursday. 

According to Morningstar Research, Ostarine drives "the lion's share" of GTx's valuation. It has since last fall, when the FDA delivered a complete response letter for toremifene 80 mg in the reduction of bone fractures associated with prostate cancer therapy. (See BioWorld Today, Nov. 3, 2009.) 

GTx markets toremifene 60 mg under the brand name Fareston for metastatic breast cancer in postmenopausal women. The drug is not a big moneymaker, with net sales of just $719,000 in third-quarter 2009. 

Hopes were higher in the prostate bone health indication, but the FDA asked for a new Phase III trial - something Cowen & Co. analyst Eric Schmidt predicted would not be worth GTx's while. 

GTx said it planned to meet with the FDA to discuss next steps. Stilwell confirmed that the meeting has taken place, but he declined to comment further ahead of the biotech's 2009 earnings call, slated for March 15. 

Toremifene, a selective estrogen receptor modulator, also is being studied in a low-dose Phase III trial for prostate cancer prevention. Data are expected this year, but Schmidt and other analysts are not optimistic. 

Instead, most had shifted their focus to the selective androgen receptor modulator (SARM), Ostarine. 

The drug was partnered with Merck as part of a $500 million SARM collaboration. The deal included $40 million in cash up front, $30 million in equity, $15 million in research reimbursements and $422 million in milestone payments. Additionally, Merck was covering all development costs. (See BioWorld Today, Nov. 7, 2007.) 

None of the milestone payment triggers have been reached yet, Stilwell confirmed. 

About a year after signing the Merck deal, GTx released data from a Phase IIb cancer cachexia trial, which showed Ostarine significantly improved lean body mass and muscle function as measured by a 12-step stair climb test, although not grip strength and gait speed. But things appeared to be moving forward: GTX said last fall that Merck was planning Phase II trials in chronic sarcopenia and muscle loss associated with chronic obstructive pulmonary disease. 

Those trials were never started, and now it looks as if they won't be - at least not by Merck. It is unknown whether GTx and Merck's broad SARM collaboration will continue. 

Schmidt wrote in a research note that Merck's internally developed SARM, MK-0773, which was also part of the collaboration, seems to be absent from the big pharma's recently revised pipeline. He noted that the entire SARM deal "may be a causality of Merck's merger with Schering Plough." 

Which isn't to say that, if Merck backed out of the collaboration, GTx wouldn't find another partner. The biotech said several parties were interested when it was originally shopping the program back in 2007. 

GTx's pipeline also includes GTx-758, an oral luteinizing hormone inhibitor for the treatment of advanced prostate cancer. Phase II trials are slated to start this year. 

The Memphis, Tenn.-based biotech reported $55.5 million in cash, equivalents and short-term investments as of Sept. 30, 2009, after posting a net loss of $12.8 million for the quarter. "

No other Pharma companies have partnered with GTx to develop this compound since Merck backed out over 2 years ago. Pharm does not drop big bucks and pull out if the compound works or is safe. Also, this is still a patented drug owned by GTx so anything sold over the internet is imported from overseas as "research chemicals not for human consumption" to circumvent the US patent. I would not trust that these compounds are of any good quality and potentially don't even contain what is claimed on the bottle.


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