Adipotide (FTPP) 10mg

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Size: 10mg
Contents: Adipotide (FTPP) (10mg)
Form: Lyophilized powder
Purity: >99%
SKU: P-ADIPOTID-10
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Adipotide for sale

A number of studies have been done with Adipotide peptide, also known as FTPP peptide, or Fat Targeted Proapoptotic Peptide, or proapoptotic peptide. The studies have shown notable Adipotide benefits such as:

  • improved insulin function
  • accelerated decrease in weight in the subjects.

Guide to Adipotide (FTPP)

Obesity is a worldwide health concern, often referred to as an epidemic. Multiple anti-obesity medications and dietary pills have been researched and developed over time, and only a few have proven to be fruitful, with minimal side effects.

Recently, peptides have been in the highlights for showing several health benefits with limited contraindications. One such peptide is Adipotide, also known as fat targeted proapoptotic peptide (a.k.a. FTPP).

Adipotide is a highly selective fat burning peptide that has proven to show its anti-obesity effects in multiple preclinical studies, described further in the article.

Introduction

Being true to its name, adipotide is a proapoptotic peptide that kills fat cells in the body by mode of apoptosis.

Prohibitins are natural proteins found in the body which regulate bodily functions such as cell formation, metabolism, and inflammation. Adipotide is one such prohibitin targeting peptide that has been a part of several research studies and clinical applications and have proven to show promising results (1).

FTPP Peptide History

Adipotide was first discovered and researched by a Houston oncologist, Dr. Wadih Arap, and his wife, Renata Pasqualini, who was also a cancer researcher at the same cancer center. What was initially implied to be an anti-cancer drug, Adipotide showed promising results in obesity, leaving the research pioneers “at a loss of words.” (2)

It was presumed that Adipotide would prevent blood supply to the carcinogenic cells, resulting in carcinogenic cell death and growth inhibition. Upon research, it was discovered that the peptide exhibited the same mechanism of action but on the fat cells instead. Finding this an interesting search, the researchers called the study as “proof of concept,” adding that the peptide would have to be studied further to understand its full potential and effects on human cells.

In order to aid in further study, the Cancer center formed an alliance with Arrowhead Research Corporation while the researchers founded the subsidiary called Ablaris Therapeutics Inc. Research studies were further carried out with hopes that FTPP would be the next breakthrough in obesity treatment. (2)

Review How Adipotide Works

Researcher Kolonin and his team isolated a naturally occurring peptide (sequence CKGGRAKDC) via phage display methodology and combined it with a proapoptotic sequence, forming the now called adipotide compound. Adipotide is homologous to the peptide sequence found in the white adipose tissue.

Owing to this development and characteristics, the peptide targets the prohibitin PHB1 found at the surface of the adipose tissue – attaching and thereby damaging them, resulting in blood supply disruption to the adipocytes (fat forming cells). (1) (3)

Prohibitins act as a vascular marker of the fatty tissues in the body and adipotide identifies these markers and conducts apoptosis or, in layman terms, kills these fat cells. (3)

It was assumed that Adipotide would essentially burst these fat cells which could be a point of concern because the burst cells would potentially cause a rapid influx of fat cells into the bloodstream leading to metabolism disruption and increased appetite. Adipotide burns these fat cells as fuel. As a result, increased appetite, which is the most common outcome of anti-obesity drugs, was not a risk here at all. This made the peptide compelling enough to research about more. (2)

Adipotide Benefits

Below are the main advantages of the peptide:

  • Loss of weight
  • No negative impact to appetite
  • Improved insulin resistance
  • Potential use in cancer treatment

Based on the early preclinical studies on monkeys, it was noted that post treatment with Adipotide, the monkeys showed high insulin resistance. Consequently, it was discovered that adipotide could potentially be used to diagnose and potentially treat type II diabetes.

Anti-cancer medication works by the same mechanism as that of Adipotide i.e., inhibition of angiogenesis – which could also be the basis of using adipotide for cancer treatment. Furthermore, based on initial studies, which are described below, when Adipotide was administered in obese and lean monkeys, only obese monkey lost weight. This indicated that the compound was highly selective towards obese fatty tissues only – which was another of the many advantages associated with this peptide so far.(4)

Adipotide Research and Clinical Studies

Early research and discovery

To evaluate the effects of the compound, Adipotide was injected in three different species of Old White monkeys daily for four weeks. No deliberate changes were made to their diet or exercise routine. After the treatment, it was noted that the monkeys lost about 11% of their body weight and 39% of the fat deposits in their bodies.(5)

However, there was one key issue reported pertaining to drug safety – mild renal dysfunction. Below image highlights results of two studies – dose finding study (A) and (C); and fixed dose study (B) and (D).

Serum creatinine levels increased in both the studies (as seen in (A) and (B)), however, upon discontinuation of the peptide, these returned to optimal levels. Whereas the BUN levels remained unchanged in dose finding study (C) while it fluctuated in the fixed dose study (D). Since these effects were reversible and mild, the potential use of the peptide as an anti-obesity medication was not completely ruled out.

Use in cancer treatment

Scientists surveyed a number of blood vessels and tissues (both normal and carcinogenic) and isolated and studied the various peptides and molecules distributed in them. Peptide, protein, and certain molecular distribution are non-random and differentially expressed in normal and cancer tissues – which are appealing targets for treatment.

Through various chemical isolation and analytical techniques, researchers discovered four native ligand receptors that are specific to certain types of carcinogenic cells. These receptors could in turn be the vascular markets for treatment, and certain highly selective peptides such as Adipotide could be incredibly useful in cancer treatment.(6)

Use in diabetes treatment

In these studies, obese mice were treated with adipotide to potentially study further its effect and mechanism on obese cells. Interestingly, it was noted that within 2 to 3 days of treatment, the mice exhibited improved glucose tolerance and decreased levels of serum triglycerides. These effects were seen prior to peptide induced weight loss. This study suggested the potential use of the peptide in diabetes treatment.

It was initially assumed that since Adipotide mainly works via apoptosis, it would damage the vascular tissues, leading to its impaired functionality. However, even though Adipotide reduces the fat tissue cell mass, it improvises its functioning – which is why there were improved hormone secretion and gene expression which thereby resulted in improved glucose tolerance in the obese mice.(7)

Adipotide Clinical trials

After witnessing promising results of adipotide in rodents and primates, researchers announced the first clinical trials on patients in 2011-2012.

Clinical trial phase I was designed for patients with prostate cancer undergoing no additional treatment. It was outlined to be conducted for 28 days where Adipotide would be injected daily under the skin (subcutaneous) for up to 5 dose levels.(8)

However, as of 2019, these in-human studies have since been discontinued and this peptide is still in the development phases. There is no clinical, in-human data available till date.(9)

Adipotide Side Effects

Below listed are the side effects reported with adipotide, some of which are minor and commonly seen with other peptides, whereas some are more specific to adipotide intake:

  • Nausea
  • Dry mouth
  • Lightheadedness
  • Fatigue, temporary tiredness
  • Renal dysfunction
  • Dehydration
  • Redness, puffiness at the injection site
  • Obesity reversal

Studies have shown that while Adipotide exhibits comparatively quick results, discontinuing its use would reverse all its effects, including weight loss.

Discontinuing the administration of the peptide leads to resorption of the white adipose tissues and decreased metabolism rate to usual – both of which would have otherwise been regulated by adipotide peptide – thus causing obesity reversal, but without any added side effects. This is most likely the case for all effects of the peptide, regardless of whether these are good or bad.(10)

Can Adipotide be used for human consumption?

While studies have been conducted on rodents and monkeys with promising results, per kg dosage in these animals does not scale to humans. Owing to biological differences between these rodents and primates, it has become increasingly difficult to translate the adipotide effects in these animals into effective human therapeutic medications.

Adipotide has not yet been studied in humans and there is no data available for human consumption to date.

In conclusion, Adipotide is not available for human consumption and can only be used for research purposes.

Summary

Adipotide, or fat targeted proapoptotic peptide (a.k.a. FTPP), is a highly selective synthetic peptide that targets the prohibitins (PHB) on the white adipose tissues and causes apoptosis of these tissues. As a result, FTPP leads to the destruction of fatty cells resulting in weight loss.

Adipotide has exhibited promising, compelling effects – such as highly selective nature that targets obese cells only and does not cause weight loss in lean animals. Furthermore, it does not cause an increase in appetite and improved glucose tolerance levels in the body. Owing to its mechanism of angiogenesis inhibition, it has become an interesting potential candidate for anti-cancer drug research and development.

Future studies and research

While studies have shown certain side effects of the FTPP use, including renal dysfunction and dehydration, these have been identified to be dose dependent, predictable, and reversible.(5)

Having multiple potential uses in treatment of cancer, obesity and diabetes, Adipotide is a promising candidate and further clinical research studies are to be conducted to determine the optimal human dosage and route of administration, its pharmacokinetics and effects in the human body.

References:

1. Thuaud, F., Ribeiro, N., Nebigil, C. G., & Désaubry, L. (2013). Prohibitin ligands in cell death and survival: mode of action and therapeutic potential. Chemistry & biology, 20(3), 316–331. https://doi.org/10.1016/j.chembiol.2013.02.006

2. Melissa H., Cancer treatment shows promise for rapid weight loss, Los Angeles Times, 10 Nov 2011. https://www.latimes.com/local/la-xpm-2011-nov-10-la-he-drug-fat-loss-20111110-story.html

3. Kolonin, Mikhail G et al. “Reversal of obesity by targeted ablation of adipose tissue.” Nature medicine vol. 10,6 (2004): 625-32. https://pubmed.ncbi.nlm.nih.gov/15133506/

4. Experimental Drug Slims Obese Monkeys https://www.medicinenet.com/script/main/art.asp?articlekey=151452

5. Barnhart, Kirstin F et al. “A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys.” Science translational medicine vol. 3,108 (2011): 108ra112. doi:10.1126/scitranslmed.3002621. https://pubmed.ncbi.nlm.nih.gov/22072637/

6. Staquicini, Fernanda I et al. “Vascular ligand-receptor mapping by direct combinatorial selection in cancer patients.” Proceedings of the National Academy of Sciences of the United States of America vol. 108,46 (2011): 18637-42. doi:10.1073/pnas.1114503108. https://pubmed.ncbi.nlm.nih.gov/22049339/

7. Kim, Dong-Hoon et al. “Rapid and weight-independent improvement of glucose tolerance induced by a peptide designed to elicit apoptosis in adipose tissue endothelium.” Diabetes vol. 61,9 (2012): 2299-310. doi:10.2337/db11-1579. https://pubmed.ncbi.nlm.nih.gov/22733798/

8. Arrowhead Announces Dosing of First Patient with Anti-Obesity Treatment Adipotide® in a Phase 1 Clinical Trial, 11 Jul 2012. https://www.businesswire.com/news/home/20120711005485/en/

9. Drug profile – Prohibitin targeting peptide 1 (adipotide; prohibitin – TP01). https://adisinsight.springer.com/drugs/800035229

10. Kolonin, Mikhail G et al. “Reversal of obesity by targeted ablation of adipose tissue.” Nature medicine vol. 10,6 (2004): 625-32. doi:10.1038/nm1048. https://pubmed.ncbi.nlm.nih.gov/15133506/

 


 

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