The bicyclam AMD3100 story

Nat Rev Drug Discov. 2003 Jul;2(7):581-7. doi: 10.1038/nrd1134.


The discovery and development of the bicyclam AMD3100--a chemokine receptor antagonist--has highlighted the therapeutic potential of such compounds in HIV infection, inflammatory diseases, cancer and stem-cell mobilization. Here, I describe the development process of AMD3100, which began about 15 years ago with the isolation of an impurity, and the basis for the clinical application of AMD3100 and its congeners.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Anti-HIV Agents / pharmacology*
  • HIV Envelope Protein gp120 / drug effects
  • Heart / drug effects
  • Heart / physiology
  • Heterocyclic Compounds / pharmacology*
  • Heterocyclic Compounds / therapeutic use
  • Humans
  • Molecular Sequence Data
  • Neoplasms / drug therapy
  • Receptors, CXCR4 / antagonists & inhibitors*
  • Receptors, CXCR4 / chemistry


  • Anti-HIV Agents
  • HIV Envelope Protein gp120
  • Heterocyclic Compounds
  • Receptors, CXCR4
  • plerixafor