Adipotide

Obesity Fighter

Combat Obesity: Discover the Powerful Benefits of Adipotide

Adipotide is a synthetic peptide designed to specifically target and kill fat cells, also known as adipocytes. The molecule operates by homing in on a particular protein found predominantly on the surface of the blood vessels that supply blood to adipose (fat) tissue. Once bound to these blood vessels, Adipotide disrupts their function, leading to reduced blood flow to the adipose tissue. This decrease in blood supply causes the fat cells to undergo programmed cell death, or apoptosis. The primary aim of using Adipotide is to reduce body fat, which makes it a potential candidate for treating obesity and related metabolic disorders.

Potential Benefits Under Research

• Targeted action: Adipotide specifically targets and kills fat cells, leading to a direct reduction in body fat.
• Reduced risk of side effects: Because it selectively affects fat cells without impacting other cell types, the potential for side effects is lower compared to less targeted therapies.
• Potential to treat obesity: By reducing body fat, Adipotide could help manage obesity and its associated health conditions such as diabetes, heart disease, and hypertension.
• Improved metabolic health: Reduction in excessive fat tissue can lead to improvements in various metabolic parameters, including blood sugar levels and cholesterol.
• Enhanced insulin sensitivity: By decreasing fat mass, Adipotide may improve insulin sensitivity, which is crucial for the control of blood sugar levels and can help prevent or manage type 2 diabetes.

Dosing Protocol for Research Purposes

• 100-150 lbs: 455-680 mcg daily for up to 28 days
• 151-200 lbs: 685-905 mcg daily for up to 28 days
• 201-250 lbs: 910-1,150 mcg daily for up to 28 days

Overview 

Adipotide (a.k.a. FTPP or proapoptotic peptide) kills fat cells, plain and simple, by targeting the blood supply of those cells. Interestingly, adipotide is able to discern the blood vessels in fat cells from the blood vessels throughout the rest of the body and is therefore highly selective. Research in monkeys shows that adipotide not only causes weight loss, it actually boosts insulin sensitivity and offsets some of the effects of type 2 diabetes.

Structure

Sequence: Cys-Lys-Gly-Gly-Arg-Ala-Lys-Asp-Cys­Gly-Gly–(Lys-Leu-Ala-Lys-Leu-Ala-Lys)2 Molecular Formula: C152H2s2N44042
Molecular Weight: 2611.41 g/mol

Adipotide Research

1. Adipotide And Fat Loss

Adipotide was developed and placed into phase I clinical trials in 2011 to investigate its ability to kill fat cells. Tests in rhesus monkeys revealed that adipotide causes targeted apoptosis in the blood vessels of white adipose tissue (fat). Without a blood supply, the fat cells simply died. The net result was rapid weight loss, rapid decrease in body mass index (BMI), and improved insulin resistance characteristics. Interestingly, treatment with adipotide and subsequent fat loss not only improved weight, but actually contributed to changes in eating behavior. Monkeys who lost weight with adipotide also showed a decrease in food consumption.

1. Percent weight loss in control groups (blue) versus those treated with adipotide (two differing doses, shown in red)
   B. Percent reduction in BMI (control versus treatment)
   Source: PubMed
   A. Shows the change in insulin requirements (area under the curve) for treated (red) and control (blue) groups. The AUC was calculated from an IVGTT test.
2. Shows the insulinogenic index for before and after in the treatment (red) and control (blue) groups. Treated groups show a dramatic decrease in insulin secretion.
   C. Change in biscuit consumption in treated (red) and control (blue) groups. 

Source: PubMed 

The targeting of adipotide to the blood vessels serving fat cells may be mediated by a protein receptor called prohibitin. Prohibitin is a membrane protein that may only be found in blood vessels serving white fat and in cancer cells. It has been demonstrated that adipotide associates with this protein. If it turns out that prohibitin is found only in fat vasculature and cancer tissue, then adipotide testing will be responsible for identifying a fat­-specific target that can be used not just for therapeutic purposes, but for diagnostic purposes as well. 

2. Adipotide and Cancer

Prohibitin, the molecule that adipotide likely targets in fat cells, has been associated with certain types of cancer. Cancer cells are known to require substantial blood supplies in order to grow and metastasize. The ability to target prohibitin in cancer cells may provide for advanced therapies that target cancer without harming surrounding tissues. 

3. Adipotide and Glucose Tolerance

Glucose tolerance is a term that refers to higher than normal levels of blood sugar. The condition is generally diagnosed with a blood test and confirmed by testing fasting glucose levels or by administering a glucose tolerance test in which a set amount of sugar is consumed and then blood levels of sugar are measured. Glucose tolerance is a proxy measure for diabetes, with increased glucose tolerance indicating a trend toward diabetes. 

Treating elevated glucose levels can be done with diet and exercise, but these methods require dedication and motivation. They also take considerable time to have an effect. In general, most people with impaired glucose tolerance go on to develop overt type 2 diabetes and require drugs like metformin and, in some cases, insulin. Research into adipotide has revealed that the peptide produces rapid and weight-independent improvement in glucose tolerance. The latter part is critical, because it indicates that a reduction in white fat by adipotide is effective in reducing glucose tolerance regardless of the impact on weight. In other words, it is the fat loss that is important, not the weight loss. These findings not only open the pathway for developing new treatments for pre-diabetes and diabetes, they help to clarify and explain the mechanisms that lead to diabetes in the first place. 

There is some argument as to whether adipotide directly causes fat loss or simply decreases food intake which indirectly leads to fat loss. It is likely that adipotide directly causes fat loss. This hypothesis is supported by the fact that the peptide causes changes in fat cell density without causing weight loss and affects glucose tolerance without causing weight loss. 

Future Adipotide Research 

The primary area of adipotide research is in fat loss and diabetes. The peptide targets specific cells in the blood vessels that supply fat tissue, causing those blood vessels to die and, as a result, causing the fat cells they supply to die. Adipotide is an anti­angiogenic peptide, which means it targets blood vessels. Anti-angiogenic molecules are of keen interest right now in the treatment of cancer. There is limited, but promising research, on the role of adipotide in cancer. 

Adipotide exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. 

Article Author

The above literature was researched, edited and
organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology. 

Scientific Journal Author 

Kirstin Barnhart. MD, lead author of “A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys,” is Associate Director, Senior Pathologist at AbbVie – a leading pharmaceutical research and development company. Dr. Barnhart led a study where the 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. 

Kirstin Barnhart, MD is being referenced as one of the leading scientists involved in the research and development of Adipotide. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Guide to Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide. Dr. Barnhart is listed in [6] under the referenced citations.

Adipotide Resources

1. K. F. Barnhart et al., “A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys,” Sci. Transl. Med., vol. 3, no. 108, p. 108ra112, Nov. 2011.
2. 2. M. G. Kolonin, P. K. Saha, L. Chan, R Pasgualini, and W. Arag, “Reversal of obesity­ targeted ablation of adipose tissue,” Nat. Med., vol. 10, no. 6, Qp. 625-632, Jun. 2004. 
3. F. I. Staquicini et al., “Vascular ligand-receptor mapping by direct combinatorial selection in cancer patients,” Proc. Natl. Acad. Sci. U. S. A., vol. 108, no. 46, pp. 18637-18642, Nov. 2011. 
4. D.-H. Kim et al., “Rapid and weight­- independent improvement of glucose tolerance induced by peptide designed to elicit apoptosis in adipose tissue endothelium,” Diabetes, vol. 61, no. 9, p11, 2299-2310,Sep. 2012. 
5. L. Criscione, “Comment on ‘a peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys,”‘ Sci. Transl. Med., vol. 4, no. 131, pp. 131Ie2; author reply 131Ir2, AP-r. 2012. 
6. Barnhart KF, Christianson DR, Hanley PW, et al. A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys. Sci Transl Med. 2011;3(108):108ra112. doi:10.1126/scitranslmed.3002621