Adipotide

Adipotide Peptide Overview

Adipotide (also known as FTPP, HKPao, or Prohibitin-TP01) is a synthetic proapoptotic peptidomimetic designed to selectively target and induce apoptosis in the vascular endothelium supplying white adipose tissue (WAT). Developed as a novel approach to obesity research, this compound represents a “hunter-killer” peptide composed of two distinct functional domains.

The peptide structure combines a homing sequence that specifically targets prohibitin receptors expressed on adipose tissue vasculature with a proapoptotic domain that triggers mitochondrial disruption and programmed cell death. Unlike many anti-obesity drug candidates that act on the central nervous system to control appetite, Adipotide acts directly on fat tissue by disrupting its blood supply.

⚠️ Critical Research Context: As of 2026, Adipotide is not FDA-approved for human use. No completed, published human efficacy trials exist. A Phase 1 oncology trial was announced in 2012 but produced no peer-reviewed published results. The primary safety concern identified in preclinical studies is dose-dependent renal tubular toxicity.

Mechanism of Action

Adipotide functions through a targeted two-step mechanism:

Targeted Homing:

• The CKGGRAKDC N-terminal sequence selectively binds to prohibitin receptors expressed on the surface of vascular endothelial cells that supply white adipose tissue

• This homing domain facilitates targeted intracellular delivery specifically to fat-supporting blood vessels

Proapoptotic Action:

• The D(KLAKLAK)2 C-terminal domain consists of D-amino acids that enhance stability

• Once internalized, this domain migrates toward mitochondria, inducing the formation of transient pores in mitochondrial membranes

• These pores allow efflux of cytochrome c, triggering programmed cell death (apoptosis) in endothelial cells

• The resulting vascular disruption starves adipose tissue of blood supply, leading to fat cell resorption and metabolism

Metabolic Effects:

• Treatment results in rapid improvement in metabolic markers, including improved insulin sensitivity and glucose tolerance, often preceding significant weight loss

• In research models, this has been associated with decreased serum insulin and triglycerides

Key Research Applications:

• White adipose tissue vascular biology studies

• Obesity and metabolic syndrome research

• Insulin resistance and glucose metabolism investigations

• Adipose tissue function and hormone secretion studies

• Targeted proapoptotic compound research

Product Specifications

Research Background

Mechanism of Weight Loss

Adipotide induces weight loss through two primary pathways:

1. Direct Fat Metabolism: As fat cells are deprived of blood supply, they are metabolized by the body

2. Metabolic Changes: Altering the vasculature feeding excess white fat changes metabolic parameters that lead to decreased food intake

Preclinical Research Findings

Mouse Studies:

• Diet-induced obese mice treated with Adipotide lost approximately 30% of body weight over 28 days

• Rapid improvement in glucose tolerance observed within 2-3 days of treatment, independent of weight loss

• Significant reduction in serum insulin and triglycerides

Rhesus Monkey Study (Published in Science Translational Medicine, 2011):

• Spontaneously obese rhesus macaques (n=10 treated, n=5 controls) received 0.43 mg/kg subcutaneously daily for 28 days

• Treated monkeys lost an average of 10.6% body weight (range: 7-15%)

• 38% reduction in total body fat and 27% reduction in abdominal fat

• Marked improvements in insulin resistance (p=0.019)

• Weight loss confirmed by MRI and DEXA to be from fat reduction, not fluid loss or muscle wasting

Encapsulated Formulation Research:

• PEGylated liposomal encapsulation (KLA-PTNP) at 1 mg/kg (one-third the dose of unencapsulated Adipotide) resulted in 14% body weight reduction from baseline in obese mice

• Encapsulated formulation demonstrated reduced ectopic fat accumulation in liver and muscle tissue

• Significant reduction in adipocyte size and improved adipokine profile (reduced leptin, increased adiponectin)

Clinical Development Status

Phase 1 Trial (Announced 2012):

• FDA cleared a Phase 1 trial in obese patients with castrate-resistant prostate cancer

• Trial conducted by MD Anderson Cancer Center

• No peer-reviewed published results from this trial exist as of 2026

Regulatory Status:

• Not FDA-approved for any indication

• No completed, published human efficacy or safety trials

• As of 2026, not on the FDA’s 503A compoundable substances list

Key Safety Concerns

Renal Toxicity Signal:

• The 2011 primate study reported dose-dependent, reversible renal tubular degeneration and regeneration

• Elevated serum creatinine was observed, which normalized post-treatment

• Kidney is the primary concern because the CKGGRAKDC peptide is processed renally after clearance from adipose binding sites

Caveats:

• Reversibility was demonstrated only in a 28-day primate study

• Chronic dosing safety, higher dose effects, and human tolerability remain entirely uncharacterized

• The D(KLAKLAK)2 domain’s mitochondria-disrupting activity is not inherently selective for adipose tissue if delivered at sufficient concentration to renal tubular cells

Published Research References

Key publications include:

• Science Translational Medicine (2011): “A Peptidomimetic Targeting White Fat Causes Weight Loss and Improved Insulin Resistance in Obese Monkeys”

• Diabetes (2010): “Peptide Designed to Elicit Apoptosis in Adipose Tissue Endothelium Reduces Food Intake and Body Weight”

• Nature Medicine (2004): Foundational study demonstrating weight loss in obese mice

• Cell Metabolism (2012): “Treating Obesity Like a Tumor”

Why Development Stalled

Despite promising preclinical data, Adipotide’s clinical development was not advanced due to:

• Uncharacterized renal toxicity threshold in humans

• No established human tolerated dose range

• No human pharmacokinetic profile

• No long-term safety data in any human population

Storage & Reconstitution Guidelines

Storage Conditions:

• Lyophilized (Long-term): -20°C, protected from light, dry, sealed

• Lyophilized (Short-term): 2°C – 8°C (refrigerated)

• Reconstituted: 4°C for up to 7 days; aliquot for extended storage; avoid repeated freeze-thaw cycles

• Powder Stability: 3 years at -20°C

Reconstitution Protocol:

1. Allow vial to reach room temperature

2. Add sterile bacteriostatic water or 0.9% sodium chloride solution

3. Gently swirl (do not vortex) until fully dissolved

4. Dispense into individual aliquots to minimize freeze-thaw degradation

Note: Peptides are sensitive to formulation, process, and environmental conditions that may lead to aggregation and degradation.

Important Notice

⚠️ FOR RESEARCH USE ONLY

This product is not intended for human consumption, diagnostic use, therapeutic application, or clinical administration. Adipotide is a research chemical intended exclusively for in-vitro and laboratory research purposes.

• Not approved by the FDA for human use

• No completed human efficacy or safety trials published

• Not a dietary supplement, food additive, or pharmaceutical for over-the-counter purchase

• Renal toxicity concerns identified in preclinical studies

• Intended solely for qualified researchers and scientific institutions

By purchasing this product, you confirm that you are a licensed researcher or laboratory professional and agree to use this compound in compliance with all applicable local, national, and international regulations.

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Adipotide Peptide – ≥95% Purity
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