ADH-1

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ADH-1
ADH-1.svg
Clinical data
Trade names Exherin
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C22H34N8O6S2
Molar mass 570.69 g/mol
3D model (JSmol)

ADH-1 (brand name Exherin) is a small, cyclic pentapeptide vascular-targeting drug. It was developed by Adherex Technologies.

ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis.[1] N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell–cell adhesion and signaling mechanisms;[1] may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels.[1]

In 2006, Adherex and NCI formed a Clinical Trial Agreement stating that NCI will sponsor clinical trials of ADH-1 in a variety of cancer types. ADH-1 received orphan drug status from the FDA in 2008.[2]

In a pilot study (phase I trial), ADH-1 intravenous pretreatment before chemotherapy in metastatic melanoma completely destroyed tumors in half of patients. It is being investigated for advanced extremity melanoma in phase II trials.[3][4]

References[edit]

  1. ^ a b c "ADH-1". NCI Drug Dictionary. 
  2. ^ "ADH-1". AdisInsight. Retrieved 3 February 2017. 
  3. ^ Yarom N, Stewart D, Malik R, Wells J, Avruch L, Jonker DJ (Feb 1, 2013). "Phase I clinical trial of Exherin (ADH-1) in patients with advanced solid tumors". Curr Clin Pharmacol. 8 (1): 81–88. PMID 22280327. 
  4. ^ Physorg:Drug combination may be effective against deadly melanoma, pilot study shows