Adipotide
An experimental peptidomimetic designed to target adipose vasculature; development was suspended due to kidney toxicity findings in primate studies.
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What is Adipotide?
Important safety note: Adipotide produced significant kidney toxicity (reduced kidney function with histological evidence of renal proximal tubule damage) in obese rhesus monkey studies. Further clinical development was suspended due to these findings, and the compound has never been tested in humans. Adipotide should not be considered analogous to other peptides in this catalog with regards to safety profile. This entry is included for completeness and scientific reference.
Adipotide is an experimental peptidomimetic compound designed at MD Anderson Cancer Center by Renata Pasqualini, Wadih Arap, and colleagues as a research anti-obesity compound with a distinctive mechanism: selective destruction of the vasculature supplying white adipose tissue. The compound is a hybrid molecule combining a targeting peptide (CKGGRAKDC) that recognizes prohibitin (a protein expressed on the surface of blood vessels supplying white fat) with a pro-apoptotic peptide sequence (D(KLAKLAK)2) that disrupts mitochondrial membranes and triggers cell death.
Adipotide is notable in research as a cautionary case study in targeted therapy development. The conceptual rationale was elegant: white adipose tissue requires its own vascular supply, and selectively destroying this vasculature would theoretically deprive fat tissue of blood supply. Early proof-of-concept studies in obese mice demonstrated significant fat loss. However, when the compound was advanced to obese rhesus monkey studies, significant kidney toxicity was observed, with histological evidence of damage to renal proximal tubules. These findings led to suspension of further development, and the compound has never been tested in human clinical trials.
Mechanism of action
Adipotide’s mechanisms of action have been investigated across multiple pathways:
- Prohibitin targeting: The CKGGRAKDC peptide portion is designed to recognize and bind prohibitin, a protein expressed on the surface of blood vessels supplying white adipose tissue.
- Pro-apoptotic membrane disruption: The D(KLAKLAK)2 portion disrupts mitochondrial membranes upon cellular internalization, triggering apoptotic cell death in target cells.
- Targeted vascular destruction: The combined hybrid molecule is designed to destroy blood vessels supplying adipose tissue specifically, depriving fat tissue of vascular supply and producing fat tissue regression.
- Off-target vascular effects: Subsequent research revealed that prohibitin is expressed on vasculature in other tissues including kidney vasculature, providing the mechanistic explanation for the kidney toxicity observed in primate studies.
- Distinct from metabolic regulators: Unlike conventional anti-obesity research compounds that work through metabolic regulation, Adipotide works through targeted destruction of blood vessels, a fundamentally different and irreversible mechanism with different safety implications.
These pathways are characterized in mouse and non-human primate models. Human studies have not been conducted.
Research applications
Important safety note: Adipotide produced significant kidney toxicity (reduced kidney function with histological evidence of renal proximal tubule damage) in obese rhesus monkey studies. Further clinical development was suspended due to these findings, and the compound has never been tested in humans. Adipotide should not be considered analogous to other peptides in this catalog with regards to safety profile. This entry is included for completeness and scientific reference.
Adipotide research has been limited to preclinical contexts:
- Mouse model research: Studies in obese mouse models demonstrated significant reductions in body weight and fat mass with relatively favorable preliminary safety profile in initial studies.
- Non-human primate research: Obese rhesus monkey studies demonstrated reductions in fat mass and body weight but also produced dose-dependent kidney toxicity including reduced glomerular filtration rate and histological damage to renal proximal tubules. These findings were the basis for suspension of further development.
- Targeting mechanism research: The compound has served as a research tool for studying targeted vascular destruction approaches and the limitations of prohibitin as a selective targeting molecule across tissues.
- Cancer biology connection: Some research has examined adipose vasculature targeting in the broader context of tumor vasculature research, since solid tumors share the dependency on vascular supply that drives the adipose-targeting rationale.
This compound is intended for laboratory research use only. It has not been approved for human therapeutic use by any regulatory agency.
Storage & reconstitution
Important note: Adipotide is included in this catalog for scientific reference only. Significant kidney toxicity in primate studies led to suspension of clinical development. Researchers handling this compound should be aware of these safety findings.
In its lyophilized form, Adipotide is typically stored at -20°C, protected from light. Properly stored lyophilized peptidomimetic remains stable for 24 months or longer, though the compound’s unusual hybrid structure may have specific stability considerations not fully characterized for most research-grade material.
Once reconstituted with bacteriostatic water for injection, solutions should be stored refrigerated at 2-8°C and used within 28 days. Avoid repeated freeze-thaw cycles, which can degrade peptide structure and reduce activity.
Visual inspection should be performed before each use. The reconstituted solution should be clear and colorless. Reject any solution that appears cloudy, discolored, or contains visible particulate matter.
For step-by-step reconstitution calculations, see our reconstitution calculator.
For laboratory research use only. The compound described on this page is intended exclusively for in vitro research and laboratory experimentation by qualified researchers and is not for human or veterinary use. It is not a drug, food, dietary supplement, or cosmetic, and has not been approved by the FDA, Health Canada, EMA, or any other regulatory authority for the diagnosis, treatment, cure, mitigation, or prevention of any disease or medical condition. The information provided on this page is for educational and reference purposes only and does not constitute medical advice. By accessing this content you confirm that you are a qualified researcher purchasing for legitimate laboratory purposes.