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Peptide Encyclopedia / Adipotide

Encyclopedia

Adipotide

Adipotide is a proapoptotic peptidomimetic designed to home to the blood vessels feeding white fat and starve those depots by killing their lining. Weight loss showed up in mice and monkeys, but no human efficacy trial was completed and development stopped, leaving it a research chemical. Educational, not medical advice.

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CategoryGLP-1 / Metabolic
Regulatory statusNot FDA-approved.

Mechanism

A proapoptotic peptidomimetic (sequence CKGGRAKDC linked to a D(KLAKLAK)2 proapoptotic domain) that homes to prohibitin on the blood vessels feeding white adipose tissue and triggers endothelial apoptosis, cutting off blood supply to fat depots.

Half-life

Not well established in humans; pharmacokinetic data are limited. It is a peptidomimetic.

Regulatory status

Not FDA-approved. Clinical development was halted; sold (when available) as a research chemical / for laboratory use only.

Safety

Major concern is renal toxicity -- animal studies showed elevated creatinine and renal tubular injury, which contributed to discontinuation of development. Human safety is unestablished and the kidney risk is a serious flag.

Evidence

Preclinical only -- demonstrated weight loss in mice and rhesus monkeys; no completed human efficacy trials; development discontinued.

Sources

  1. Kolonin MG, Saha PK, Chan L, Pasqualini R, Arap W. Reversal of obesity by targeted ablation of adipose tissue. Nat Med. 2004;10(6):625-632. https://pubmed.ncbi.nlm.nih.gov/15133506/
  2. 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. https://pubmed.ncbi.nlm.nih.gov/22072637/
  3. Kim DH, Woods SC, Seeley RJ. Peptide designed to elicit apoptosis in adipose tissue endothelium reduces food intake and body weight. Diabetes. 2010;59(4):907-915. https://pubmed.ncbi.nlm.nih.gov/20103704/
  4. Kim DH, Sartor MA, Bain JR, et al. Rapid and weight-independent improvement of glucose tolerance induced by adipotide. Diabetes. 2012;61(9):2299-2310. https://pubmed.ncbi.nlm.nih.gov/22733798/
  5. Criscione L. Comment on 'A peptidomimetic targeting white fat causes weight loss...' Sci Transl Med. 2012;4(131):131le2. https://pubmed.ncbi.nlm.nih.gov/22539771/
  6. Salameh A, Daquinag AC, Staquicini DI, et al. Prohibitin/annexin 2 interaction regulates fatty acid transport in adipose tissue. JCI Insight. 2016;1(10):e86351. https://insight.jci.org/articles/view/86351
  7. Daquinag AC, Tseng C, Zhang Y, et al. Targeted proapoptotic peptides depleting adipose stromal cells inhibit tumor growth. Mol Ther. 2016;24(1):34-40. https://pubmed.ncbi.nlm.nih.gov/26316391/
  8. Staquicini FI, Cardo-Vila M, Kolonin MG, et al. Vascular ligand-receptor mapping by direct combinatorial selection in cancer patients. PNAS. 2011;108(46):18637-18642. https://pubmed.ncbi.nlm.nih.gov/22049339/

PepWise is an informational and educational tracking tool, not medical advice and not a medical device. Adipotide may be experimental, restricted, or prescription-only; many research peptides are not FDA-approved. Consult a licensed healthcare provider before starting, changing, or stopping any protocol. Operated by STC Consulting, Inc.