Adipotide The New Peptide Fat Burner

liberate

New member
Very interested in this one. I searched the forums first, but couldn't find any info or logs out there yet so I started my own thread:

Adipotide
An obesity drug that 'kills' fat cells

Most weight-loss drugs help burn fat by speeding up metabolism, suppressing appetite, or both. But a new drug currently being tested on obese rhesus monkeys goes a step further: It reportedly "kills" fat cells. Researchers at the University of Texas think the drug could one day help fight obesity in humans. Here's what you should know:

What is this fat-killing drug?
The experimental drug is called Adipotide, and it works by targeting the cells found in white fat tissue, says Steven Reinberg at USA Today. Adipotide kills fat "by attaching itself to fat cells in the blood vessels and triggering a synthetic protein that causes the cell to die." Afterward, those dead cells are reabsorbed by the body and metabolized.

And it made these fat monkeys skinny?
Skinnier, at least. In just four weeks, the obese monkeys lost 11 percent of their body weight. The monkeys also shed 27 percent of their abdominal fat, says Tim Barribeau at io9. Caveat: "Monkeys that were already thin didn't shed pounds at all, meaning it might only target extra weight, not the stuff we need to survive."

Would this work on humans?
It's promising. Usually, fat burning drugs are tested on mice. Researchers believe this research is particularly "relevant because it was done with primates," says Jennifer Booton at Fox Business. Plus, the fatter monkeys in the study had grown portly thanks to their own overeating and lack of exercise ***8212; just like many obese humans.

An obesity drug that 'kills' fat cells - The Week


An animal study says a new experimental drug may lead to significant and rapid weight loss by destroying blood supply to fatty cells. The drug called Adipotide helped obese rhesus monkeys lose on average 11 percent of their body weight after four weeks of treatment. The drug which works on the basis of a new cancer treatment targets proteins on the surface of blood vessels that feed white fat cells and destroys them by releasing a synthetic molecule that triggers a natural process of cell death. Researchers led by scientists at the University of Texas first studied the efficacy of the new drug on obese mice which decreased 30 percent of their body weight. The next trial was carried out on 15 monkeys as their similarities to mankind make them a good model to predict the possible effectiveness and side effects of a medication in human. After four weeks, the 10 primates that received a daily injection of Adipotide lost on average 38.7 percent of their total body fat, compared to 14.8 percent for the five others who were given placebo. Treated monkeys also lost 27 percent of their abdominal fat, scientists wrote in the journal Science Translational Medicine. [1] Body mass index (BMI) and abdominal circumference (waistline) also were reduced, while all three measures were unchanged in untreated control monkeys. "Development of this compound for human use would provide a non-surgical way to actually reduce accumulated white fat, in contrast to current weight-loss drugs that attempt to control appetite or prevent absorption of dietary fat," Renata Pasqualini, co-senior author of the study, said. Previous attempts to treat obesity have predominantly focused on drugs aimed at suppressing appetite or increasing metabolism, but these efforts have been hampered by their toxic side-effects. The new drug designed by the MD Anderson group includes a homing agent that binds to a protein on the surface of fat-supporting blood vessels and a synthetic peptide that triggers cell death, as soon as their blood supply gone, fat cells are reabsorbed and metabolized. In earlier preclinical research, obese mice lost about 30 percent of their body weight with the drug, Adipotide, which acts drug acts on white adipose tissue, the scientific name for the unhealthy type of fat that accumulates under the skin and around the abdomen, and is a disease and mortality predictor. [2] The MD Anderson group designed a new drug, which includes a homing agent that binds to a protein on the surface of fat-supporting blood vessels and a synthetic peptide that triggers cell death. Their blood supply gone, fat cells are reabsorbed and metabolised. Co-senior author Professor Wadih Arap, said: "Obesity is a major risk factor for developing cancer, roughly the equivalent of tobacco use, and both are potentially reversible." In earlier preclinical research, obese mice lost about 30 per cent of their body weight with the drug, now called Adipotide. [3]

As a result of the challenges in developing weight-loss drugs there's presently only one FDA-approved obesity drug on the market, Alli, which blocks the absorption of some of the fat people eat. "There can be no doubt about the need for new strategies here," he said. "And this represents a quantum leap in terms of a new strategy for treating obesity." Pasqualini and Dr. Wadih Arap, her husband and also an M.D. Anderson researcher, were able to develop the obesity drug after devising a technique to "map" the various networks of blood vessels in the human body. During more than a decade of research, they have identified the tiny bits of protein that bind with various networks of blood vessels in the body. In essence, then, they have identified "ZIP codes" for each of these kinds of blood vessels, and now are sending agents to the ZIP code for fat cell blood vessels that can shut them down. Their initial work in obese mice several years ago produced astounding results in which the mice lose more than 30 percent of their body weight following treatment with the drug. They were able to subsequently test the drug in primates at M.D. Anderson's monkey facility near Bastrop. [4] Several drugs have failed so far to clear regulatory hurdles, hampered especially by safety worries. At M.D. Anderson, Renata Pasqualini and Wadih Arap, a wife-and-husband research team, and their laboratory colleagues have developed a map of the body's blood-vessel system as part of an effort to develop more effective cancer treatments. Their work has shown that different blood-vessel cells have distinct molecular signatures that the researchers liken to ZIP codes. The researchers theorized they could deprive tumors of their blood supply by combining a lethal therapy with a molecule that homed in on the ZIP code of cells in blood vessels that feed cancerous growths. After identifying ZIP codes they thought might work in prostate cancer, they wondered about the possibility of targeting vessels that feed white fat cells, which accumulate under the skin and around organs in the abdomen, and are associated with weight gain. [5]

The report has also claimed that during the experiments the very same drug has enhanced various metabolic activities among monkeys and insisted that around three species of primates have responded to synthetic peptide vaccination and alerted the metabolic functions. Dr. Wadih Arap, the co-author of the study, who is serving as an oncologist at the M. D. Anderson Cancer Center in Houston, in collaboration with his wife Renata Pasqualini, an expert performing cancer related research have applauded the research results with significant weight loss and improved metabolic activities. During the study course, a team of experts at the MD Anderson Cancer Center, situated in Houston, had treated a few monkeys with a protein compound named as adipotide, which is believed to influence and kill the fat cells through fluctuated blood supply to them. Afterwards, they observed excellent results in a short span of time, only after 28 daily injections, where monkeys shed more than 11% of their body weight. [6] Targeted approach provides a new avenue for potential anti-obesity medication. HOUSTON -- Obese rhesus monkeys lost on average 11 percent of their body weight after four weeks of treatment with an experimental drug that selectively destroys the blood supply of fat tissue, a research team led by scientists at The University of Texas MD Anderson Cancer Center reports in Science Translational Medicine. [7] A research team led by scientists at the University of Texas MD Anderson Cancer Center tested a group of overweight rhesus monkeys with a drug that selectively destroys the blood supply of fat tissue. After just four weeks, the primates lost on average 11 percent of their body weight and the researchers measured drops in body mass index (BMI) and waistline, according to the study published in the journal Science Translational Medicine. [8] An experimental drug that selectively destroys the blood supply of fat tissue is being considered as an opportunity by scientists to provide a new avenue for anti-obesity medication. Researchers at the University of Texas MD Anderson Cancer Center treated "spontaneously" obese rhesus monkeys with the drug for four weeks and found that they lost on average 11 percent of their body weight. [2]

Obese monkeys lost significant amount of weight with a new drug that kills fat cells, paving the way for its development for use in humans, a study finds. Obese monkeys lost an average 11 percent of their weight in four weeks of treatment with the drug, according to researchers at The University of Texas MD Anderson Cancer Center. It also trimmed their waistlines by eradicating 27 percent of their abdominal fat. [9] Could a drug kill fat cells? That's the tantalizing promise of a new study on an experimental drug developed by scientists at the University of Texas MD Anderson Cancer Center. The researchers tested the drug on rhesus monkeys and found that they lost 11 percent of their body weight after four weeks of treatment. [10]

For years, doctors have recommended low-calorie, high-fiber diets and exercise routines that encourage good health and better physiques. Unfortunately, these recommendations inspire little hope in those who have big upcoming plans that require quick weight loss. Americans like things to happen quickly, and many spend hundreds of dollars on pills and diet plans that promise to show them how to lose weight fast. Sometimes these products work; sometimes they don't. One thing appears certain: if a new drug called adipotide hits the market any time soon, a lot of these companies may be out of business. A research study at MD Anderson Cancer Center has given new hope to those in search of an effective pill that provides quick weight loss. According to the researchers, when they gave overweight monkeys a specific protein compound, each one lost about 11 percent of their original body weight despite not exercising at all. [11] Dr. Kirstin Barnhart feeds a handful of peanuts to a monkey used. Dr. Kirstin Barnhart (left) poses for a portrait along with fellow scientist Patrick Hanley after feeding peanuts to two monkeys used in a recent study for a new drug developed by Houston scientists that caused obese monkeys to lose 10 percent of their body weight in a month, at the MD Anderson Cancer Center Keeling Center for Comparative Medicine and Research, Wednesday, Nov. 9, 2011, in Bastrop. Several Rhesus macaque monkeys were selected from the colony of 950 due to their naturally obese bodies and lifestyles, helping provide a perfect test model for human obesity and Type 2 diabetes treatment. [4]

Appetite is also curbed. When monkeys that had become fat by overeating and not exercising were given daily jabs of the drug, they shed 11 per cent of their weight in just four weeks. In human terms, an obesity drug is usually seen as beneficial if a person loses around 5 per cent of their weight in six months. The animals also shed 39 per cent of their overall body fat and bellies were trimmed by 27 per cent, the journal Science Translational Medicine reports. Some kidney problems were noted but researchers, from the MD Anderson Cancer Centre at the University of Texas, believe these can be overcome. They plan to give the drug to obese prostate cancer patients, in the hope of improving their overall health. [12] With Britain batting the worst weight problem in Europe, scientists believe a drug that works by cutting off the blood supply to fat cells could offer a new way to tackle obesity. If injected on a daily basis, researchers believe the medication could help people lose 40 per cent of their body fat in just four weeks. The U.S. team behind the new drug believe their formulation will be safer than previous diet drugs, which have been banned over safety fears in recent years, as it works directly on the body rather than the brain. Adipotide hones in on the blood vessels that supply fat cells with blood, causing them to perish and also curbing appetite. Monkeys injected with the drug shed 11 per cent of their weight in a month. The journal Science Translational Medicine reports that the animals also shed 39 per cent of their overall body fat and their bellies were trimmed by 27 per cent. [13] Researchers behind the drug, following the same strategy used to fight some cancers, designed Adipotide to kill fat cells by destroying the blood vessels that feed them, the Los Angeles Times reports. The researchers confirmed that the monkeys--which they call the "couch potatoes" of the colony--had shed the white body fat linked to Type 2 diabetes and heart disease. They hope to begin human trials of the drug within a year. The monkeys began to put on weight again four weeks after they stopped taking the drug. Its creators say that if it works in humans, it should be used as a way to kick-start a diet and exercise program for permanent weight loss. [14]

A drug that kills a type of fat cell by choking off its blood supply caused significant weight loss in obese monkeys, potentially setting the stage for a new pharmaceutical approach to attacking obesity, according to a study released Wednesday. After four weeks of treatment, obese monkeys given daily injections of the drug, called adipotide, lost an average of 11% of their body weight. They also had big reductions in waist circumference and body-mass index and, importantly, striking improvement in their ability to process insulin, researchers said. [5] WASHINGTON -- There is new hope in the fight against fat after a surprising discovery made by scientists looking for new ways to treat cancer. Historically, weight loss products have targeted appetite or fat absorption, but scientists say this new technique kills fat cells by cutting off their blood supply. In a study published on Wednesday in the journal Science Translational Medicine, researchers from the University of Texas say injecting a peptide called "adipotide" into obese monkeys made the animals eat less, shed belly fat and increased their metabolic function -- without any change to their diets or exercise regimens, The Los Angeles Times reports. It also resulted in improved insulin resistance, which could be helpful in the treatment of Type 2 diabetes. [15]

The drug, called Adipotide, targets the blood supply of fat cells and the researchers say the treated monkeys' health improved in a number of ways afterwards: weight, BMI and abdominal circumference continued to drop. The only major side effect was on the kidneys, but the researchers said it was manageable and depended on the amount of the dose. The next step is studying this drug in humans. The researchers say they hope to begin testing it on obese prostate cancer patients since the hormone therapy used in prostate cancer often brings on weight gain, which would add to the health risks for these patients. Given the highly experimental nature of this drug, it's way too soon to say whether this will ever help humans struggling to lose weight but it's always interesting to note a new approach to an old problem. In the meantime, the best advice for those who want to lose pounds is still eat less, exercise more. [10]

In tests the drug Adipotide, when given on a daily basis, reduced body fat by 39% and stomach fat by 27% in four weeks. Researchers allowed monkeys to gain weight by eating too much and not exercising, then injected them with the drug. The monkeys lost 11% of their weight in a month and the team said the results were so promising they were keen to start testing the drug on obese people. Although the team from the MD Anderson Cancer Centre at the University of Texas said some of the monkeys had kidney problems from the jab, they thought this issue could be resolved. The injectable targets blood vessels in the body which give fat a blood supply and makes them die, while also reducing appetite. [16] Researchers at MD Anderson Cancer Center in Houston gave monkeys a drug, a protein compound called adipotide, that targets the blood supply to fat cells and kills them. After only 28 daily injections of the drug the monkeys lost an average of 11 percent of their body weight. [17]

SOURCES

1. PressTV - Experimental drug can help weight Loss
2. Soon, pill to help obese lose weight in 1 month! - Times Of India
3. New drug could help obese patients lose tenth of their weight in just one month - Telegraph
4. Fat-zapping drug proves not to be monkey business - San Antonio Express-News
5. Arrowhead Research Corp : The Wall Street Journal: Drug Offers Hope in Obesity Fight | 4-Traders
6. Experts Applaud a Cancer Drug for Immediate Weight Loss | News Tonight
7. Obese monkeys lose weight on drug lim. JPost - Health & Science
8. Drug Kills Fat Cells In Obese Monkeys | Fox News
9. Medical Daily: Drug Helped Obese Monkeys Lose Weight, Human Trial Ahead
10. Fat-Fighting Drug | Health Goes Strong
11. How Do You Lose Weight Fast? New Drug May Be the Answer
12. Pot belly blaster: A jab to banish 40% of body fat in just a month | Mail Online
13. Jab to banish body fat | Marie Claire
14. Drug Slims 'Couch Potato' Monkeys - Experimental fat-zapping drug works on chunky monkeys
15. WTOP Mobile
16. New jab gets rid of 39% of body fat in a month - AOL Lifestyle UK
17. Drug helps monkeys lose weight, are humans next? - TODAY Health - TODAY.com
18. US Research Reveals Trial Drug to Shed Weight of Monkeys | News Tonight
19. Novel Drug Shrinks Monkeys' Waistlines - ScienceNOW
20. Experimental drug slims obese monkeys - USATODAY.com

Looks like this thread has come a long way!!! Thanks everyone for all the knowledge and information you're throwing at it!!! Don't forget to rep up the OP!!!
<--
 
Last edited:
Some more info off PubMed

A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys.

Barnhart KF, Christianson DR, Hanley PW, Driessen WH, Bernacky BJ, Baze WB, Wen S, Tian M, Ma J, Kolonin MG, Saha PK, Do KA, Hulvat JF, Gelovani JG, Chan L, Arap W, Pasqualini R.
Source

David H. Koch Center, University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USA.
Abstract

Obesity, defined as body mass index greater than 30, is a leading cause of morbidity and mortality and a financial burden worldwide. Despite significant efforts in the past decade, very few drugs have been successfully developed for the treatment of obese patients. Biological differences between rodents and primates are a major hurdle for translation of anti-obesity strategies either discovered or developed in rodents into effective human therapeutics. Here, we evaluate the ligand-directed peptidomimetic CKGGRAKDC-GG-(D)(KLAKLAK)(2) (henceforth termed adipotide) in obese Old World monkeys. Treatment with adipotide induced targeted apoptosis within blood vessels of white adipose tissue and resulted in rapid weight loss and improved insulin resistance in obese monkeys. Magnetic resonance imaging and dual-energy x-ray absorptiometry confirmed a marked reduction in white adipose tissue. At experimentally determined optimal doses, monkeys from three different species displayed predictable and reversible changes in renal proximal tubule function. Together, these data in primates establish adipotide as a prototype in a new class of candidate drugs that may be useful for treating obesity in humans.

PMID:
22072637
[PubMed - in process]
 
Adipotide

Dear all:

I am new here and have a background in biomedical research. I have read the paper by Barnhardt et al on adipotide and can reply to the last few posts. This is a breakthrough for weight loss as it uses an entirely new mechanism of action (killing the blood vessels that support the fat tissue) and does not target the nervous system. It is spectacular science and I suggest you read the paper to see for yourself. You can get a copy of the paper at ScienceTranslationalMedicine.org for $15.

First, it does not cause kidney failure as "GreatWhitePeptides" claims. Here is what the paper says on page 8:

"The primary side effect is relatively
mild, predictable, and reversible renal injury and altered tubular
function, demonstrating that the efficacy of adipotide in highly relevant
primate models of human obesity suggests that it is a promising
candidate drug for translation into clinical applications."

In figure 7 they show images of kidney tubules before, during and after treatment and as you can see the kidneys are not damaged very much by the treatment and they recover completely.

Secondly, it will be 5-10 years before the clinical trials are performed and the drug has FDA approval and gets on the market. They have started human trials in Houston at the Anderson Cancer Center on patients with prostate cancer that might benefit from lower fat levels because it is easier to get approval for trials on cancer patients. This proves that the authorities are convinced by the animal studies that toxicity is not an issue.

On page 5 of the Science paper, they say the following concerning toxicity:

"Although detailed
single- and multiple-dose toxicology studies will be published elsewhere,
here, we report that dose-dependent toxicity in monkeys receiving
single doses of adipotide up to 100 mg/kg (~133-fold of the corresponding
therapeutic dose) did not result in lethality."

In other words, if they give monkeys 133 times the dose needed to lose weight (10-15% of body mass is lost in 60 days after 30 days of treatment) it does not kill them. It sounds quite safe to me.

Concerning availability before FDA approval, that is a grey area and it depends where you are. The University of Texas owns the patent rights which have been licensed to a company in Pasadena, California called Ablaris. It has been patented in the US, the EU and will soon be patented in Canada so if you are not in these countries you can probably make, sell and buy the peptide without breaking the law. There are hundreds of peptide synthesis companies around the world, and the peptide is only 25 amino acids in length and quite easy to synthesize. The cost would be less than 10,000 dollars for 1 gram, enough for a 30 day treatment for one person weighing 100 kg. This is the cost for a custom synthesis of a 25 amino acid peptide purified to 98% and delivered as the acetate salt. A bulk synthesis of 1 kg of the peptide will cause the cost per treatment to drop by at least 20 fold. Once the drug companies start making it, the cost per dose will drop to a few dollars. Its all a matter of scale, and what can be purchased from a peptide lab today is a small scale custom synthesis, so of course the price is very high. Peptide labs make and sell peptides of any sequence all the time and leave it up to the buyer to determine if the sequence is patented, and they keep the orders confidential. Peptides are inherently safe and have not been abused by recreational drug users , so the authorities do not regulate their production.

OK, so if you really wanted to try this new weight loss drug then you can do it. Order the peptide yourself, preferably from a lab that is not located in a country where the patents have been issued, such as Israel, Japan, or India. There are plenty of good peptide labs in these countries. Maybe Mexico if you can find a good lab. Then self administer the peptide to yourself (280 micrograms per kilo per day, subcutaneously in saline solution) in a country where the patents are not issued.

You should do this under a doctor's supervision. You might have to tell him that you are trying a new weight loss treatment, without going into the details, because most doctors will not participate in a treatment that it not approved by the authorities. Have a serum and urine tests done before, during, and after treatment and check for the same parameters that they look at in the monkeys in the science paper. This will cost extra, but is worth it to make sure nothing is going wrong.

If the monkey studies (done on obese rhesus monkeys) is any indication, then you should lose 10-15% of body mass and 40% of body fat in 60 days without any change in lifestyle. The fat, lazy monkeys (all female by the way) continued to be lazy, they just did not eat as much of the high calorie foods. here is what the paper says on page 3:

" Monkeys receiving adipotide remained bright and alert throughout
both experiments. They maintained a consistent level of activity,
interacted with their caretakers appropriately, and presented no overt
clinical signs of nausea, vomiting, or food aversion. Monkeys were fed
a specified amount of commercially produced primate biscuits and
enrichment supplements, and the amount of each food type consumed
was documented daily. All treated and control monkeys consumed
nearly all of their enrichment supplements throughout the
treatment interval; in contrast, the number of monkey chow biscuits
consumed by treated monkeys decreased in an inversely proportional
manner with the dose of adipotide administered and/or the amount of
weight lost over time (Fig. 5C and fig. S3)."

I am convinced that adipotide is the miracle cure for obesity that the world has been waiting for. Unfortunately the FDA is very cautious (overly cautious in my opinion) when approving new weight loss drugs and it will be many years before it becomes available.

Whatever you do, do not buy "adipotide" online. It will not be the real thing. If the seller insists it is, ask to see the HPLC results and the mass spectra, which all legitimate peptide synthesis labs provide with their products. The mass should be about 2,557 Daltons. The sequence is:

CKGGRAKDC-GG-D(KLAKLAK)2



DBrown
 
Last edited:
self administering adipotide

One more thought on self-administering adipotide.

It would be very similar to self administering insulin, something millions of obese people do every day. Insulin is normally injected under the skin using disposable prefilled syringes with fine needles to minimize discomfort. The insulin is in an aqueous solution. The injection volumes are small, ranging from .3 to 1 ml.

Now compare insulin with adipotide. Here is brief description of insulin from wikipedia:

"Human insulin is a peptide hormone composed of 51 amino acids and has a molecular weight of 5808 Da. "

Adipotide is also a peptide, but somewhat smaller, 25 amino acids, with a mass of about 2,557 Da Both can easily be self-administered by injecting an aqeous solution (volume between .3 and 1 ml) of the peptide under the skin daily.

Therefore self-administering adipotide could be the same as self-administering insulin, which is known to be safe, easy, and cheap.

DBrown
 
You could try Tesamorelin we carry that

Tesamorelin 2MG

— The US Food and Drug Administration (FDA) has approved tesamorelin acetate injection (Egrifta; Theratechnologies, Inc, and marketed by EMD Serono) as the first and only treatment indicated to reduce excess abdominal fat in HIV-infected patients with lipodystrophy.

Tesamorelin is a synthetic analog of growth hormone–releasing factor — a hypothalamic peptide that acts on pituitary cells in the brain to stimulate the production and release of endogenous growth hormone.

"The FDA recognizes the need for therapies to treat patients with HIV-lipodystrophy," said Curtis Rosebraugh, MD, MPH, director of the Office of Drug Evaluation II in the FDA's Center for Drug Evaluation and Research, in an agency news release. "The presence of excess fat with this condition may contribute to other health problems as well as affect a patient's quality of life, so treatments that demonstrate they are safe and effective at treating these symptoms are important."

FDA approval followed a positive endorsement from the Endocrinologic and Metabolic Drugs Advisory Committee and was based on data from 2 multicenter, randomized, double-blind, placebo-controlled phase 3 studies of 816 patients, showing that once-daily treatment with tesamorelin significantly reduced visceral adipose tissue (VAT) at 26 weeks.

Mean VAT at baseline ranged from 178 cm2 to 186 cm2 for the active-treatment group and 171 cm2 to 195 cm2 for patients randomly assigned to placebo, as assessed by computed tomography scan at the L4–L5 vertebral level.

Computed tomography scan results of the first study showed that tesamorelin therapy yielded an 18% least-squares mean decrease from baseline in VAT compared with an increase of 2% for placebo (***916;, ***8722;20%; 95% confidence interval [CI], ***8722;24% to ***8722;15%). In the second study, tesamorelin-treated patients experienced a likewise significant 14% decrease from baseline in VAT compared with a 2% decrease among those given placebo (***916;, ***8722;12%; 95% CI, ***8722;16% to ***8722;7%).

Both studies also showed significant decreases in VAT as measured by least-squares mean decreases from baseline in waist circumference (study 1, ***8722;3 cm vs ***8722;1 cm; ***916;, ***8722;2 cm; 95% CI, ***8722;2.8 cm to ***8722;0.9 cm; study 2, ***8722;2 cm vs ***8722;1 cm; ***916;, ***8722;1 cm; 95% CI, ***8722;2.5 cm to ***8722;0.3 cm).

The decreases in VAT and waist circumference were sustained in patients who received extended therapy with tesamorelin for 52 weeks.

The recommended dose of tesamorelin is 2 mg (2 vials) injected subcutaneously once daily in the abdomen. Adverse events most commonly reported in tesamorelin-treated study patients included arthralgia (13% vs placebo, 11%), pain in extremity (6.1% vs 4.6%), myalgia (5.5% vs 1.9%), injection-site erythema (8.5% vs 2.7%), injection-site pruritus (7.6% vs 0.%), and peripheral edema (6.1% vs 2.3%).

FDA officials note that the long-term cardiovascular benefit and safety of tesamorelin have not been studied, and there are no data to support improved compliance with antiretroviral therapies. Also, tesamorelin should not be used for weight-loss management.

"As HIV-infected patients are living longer, a substantial number may develop metabolic complications associated with HIV, such as abdominal lipohypertrophy," said Morris Schambelan, MD, professor of medicine from the University of California–San Francisco, in a company news release. "With the approval of Egrifta, doctors are now able to provide appropriately selected patients with a treatment option shown to reduce [VAT]."

Because tesamorelin induces the release of endogenous growth hormone, it should not be used in patients with active malignancy, whether newly diagnosed or recurrent. Tesamorelin increases serum levels of insulin-like growth factor 1 (IGF-1), which has an unknown effect on the development or progression of malignancies. Discontinuation of therapy should be considered in patients with persistent IGF-1 elevations greater than 3 standard deviations, particularly if the efficacy response is not robust. In clinical trials, IGF-1 levels were measured every 3 months.

Tesamorelin therapy may also result in glucose intolerance and an increased risk for diabetes mellitus. Glucose status should be carefully evaluated before initiating therapy and monitored periodically thereafter. Caution is advised when treating patients who develop glucose intolerance or diabetes, and discontinuation of therapy should be considered in those who do not demonstrate a clear efficacy response. Diabetic patients should be monitored at regular intervals for the potential development or worsening of retinopathy.

Treatment with tesamorelin is contraindicated in patients with disruption of the hypothalamic–pituitary axis resulting from hypophysectomy, hypopituitarism, or pituitary tumor/surgery; active malignancy; or pregnancy and in patients with known hypersensitivity to tesamorelin and/or mannitol.

The safety and efficacy of tesamorelin have not been established in pediatric patients and in those with renal or hepatic impairment; discontinuation of therapy should be considered in critically ill patients.

As a condition of approval, the company is required to conduct a clinical trial to assess whether tesamorelin has an effect on diabetic retinopathy, and a long-term observational safety study for a single-vial formulation of the drug (tesamorelin).


ref: Medscape: Medscape Access
 
Re:dbrown

OK, so if you really wanted to try this new weight loss drug then you can do it. Order the peptide yourself, preferably from a lab that is not located in a country where the patents have been issued, such as Israel, Japan, or India. There are plenty of good peptide labs in these countries. Maybe Mexico if you can find a good lab. Then self administer the peptide to yourself (280 micrograms per kilo per day, subcutaneously in saline solution) in a country where the patents are not issued.

dbrown,

Will peptide systhesis labs create and sell peptides to anyone? Or do you have to have some sort of liscense to purchase these?
 
dbrown,

Will peptide systhesis labs create and sell peptides to anyone? Or do you have to have some sort of liscense to purchase these?[/QUOTE]

Hi Slang;

Yes. Peptides are unregulated and as long as you can pay, you can order any peptide you want. You do not need a license to purchase a custom peptide.
 
Wait a minute. Tesamorelin does not help with weight loss, even the manufacturer says so. It has been shown to work in HIV patients that have lipodystrophy, a condition where fat accumulates at high levels in the abdomen. But that does not mean it will help otherwise healthy people lose weight. here is what I found at
virus.emedtv.com/tesamorelin/what-is-tesamorelin-used-for.html

An Overview of Uses for Tesamorelin
Tesamorelin acetate (Egrifta***8482;) is an injectable medication approved to diminish excess abdominal body fat in people who have a condition called lipodystrophy as a result of the medicine they take for human immunodeficiency virus (HIV)....This medication is not approved for weight loss and will not cause weight loss.


With that said, it might also be useful in obese pateints that have a growth hormone deficiency and the manufacturer is now testing this in clinical trials. From the Theratechnologies website:

Strategy
Theratechnologies is supporting a Phase 2 clinical study led by the Massachusetts General Hospital and Dr. Steven Grinspoon, by providing tesamorelin for the study. Dr. Grinspoon has obtained a grant from the National Institutes of Health to conduct this study evaluating tesamorelin for the treatment of growth hormone deficiency associated with abdominal obesity. This single-center, double-blind clinical trial will evaluate tesamorelin in GH-deficient abdominally obese subjects. Theratechnologies will retain the benefits from the results generated from this study.

I think its too early to say if Tesmorelin will help the average person lose weight. I suggest waiting until the clinical trials mentioned above are published before trying it.
 
one more question. When ordering do I just need to give them the sequence CKGGRAKDC-GG-D(KLAKLAK)2? Or is there some other information I need to give them? Do I ask for it in some type of solution? Or would I just inject it as it is?
 
Dear Slang;

I purposefully left out an important detail about the synthesis of this peptide, so if you ask for standard CKGGRAKDC-GG-D(KLAKLAK)2, it will probably not work. It needs to be modified.

Peptides are normally delivered as a lyophilized powder. The lab will tell you the mass of the peptide sample, and then it is up to you to dissolve it. This peptide has many positively charged lysine residues (the Ks in the sequence) and is highly soluble in water, so it can be dissolved in sterile saline solution. The peptide lab might be willing to deliver it already dissolved in sterile saline solution, you would have to ask. The volume of saline solution should be calculated so that 0.3 to 1 ml of the peptide solution contains the therapeutic daily dose, which will depend on the mass of the patient. The authors of the Science paper calculate the estimated dose for humans in supplementary table 8 based on surface area vs theraputic dose in mice, monkeys, and extrapolated to humans. They calculate that the human dose will be 0.28 mg per kg per day. This would be a good place to start.

But don't go out and order the peptide now! Are you sure you want to spend many thousands of dollars without looking into it a bit first?
 
Last edited:
dbrown,

Im not planning on buying it now. Not only for safety reasons but cost also. I just want to know as much as possible in case in the future I decide to try to buy it. But that will be down the road a ways.
 
dbrown,

even though I don't plan on getting this stuff because of cost and safety, I still want to make sure I understand correctly. If you had 200ug of the powder you would mix .6ml of saline solution to get the solution needed? Then from that solution how would much of that solution would you need to measure for a daily dose? Sorry just trying to understand....I'm not good at the conversion stuff.
 
Hi Slang;

<<even though I don't plan on getting this stuff because of cost and safety, I still want to make sure I understand correctly. If you had 200ug of the powder you would mix .6ml of saline solution to get the solution needed? Then from that solution how would much of that solution would you need to measure for a daily dose? Sorry just trying to understand....I'm not good at the conversion stuff. >>

200 ug is not enough for a single day's worth for a dwarf! The estimated dose for humans is 280 ug per kg per day. If you weigh 100 kg then you will need 28 mg per day. You will probably need to take the treatment at least 30 days, so this works out to 840 mg for the treatment (28 x 30). If you order 840 mg and want to inject 1 ml of solution per day (1 ml is a convenient amount to inject subcutaneously) then you should dissolve the 840 mg in 30 ml of saline and inject 1 ml per day.

The FDA approved trials in prostate cancer patients that are planned to start in January, 2012 in Houston, Tx will give the patients only 30 micrograms per kg per day. This is because they don't know for sure that 280 ug/kg/day is a safe dose in humans so they are starting the first human trials with much less (almost 10 times less). They will be looking for side effects, including kidney damage. Once they determine that 30 ug/kg/day is safe then they will increase the dose. The whole process will take years and this is why Adipotide will not be FDA approved for many years (7 to 10 in my estimate).
 
bippal,

Did you contact GWP privately to find out that they will be selling in Jan? Also, do you know what they plan on pricing it for?
 
Back
Top