Substance P-saporin for the treatment of intractable pain

Hugh Nymeyer, Douglas A. Lappi, Denise Higgins, Carl E. Noe, Arthur E. Frankel

Research output: Chapter in Book/Report/Conference proceedingChapter


Pain is a worldwide chronic health issue, and additional therapies are needed for the management of severe pain. Substance P-Saporin (SP-SAP) covalently links a biological toxin (SAP) and an endogenous peptide (SP) that targets that toxin to the subset of neurons expressing the NK1 receptor. SP-SAP, currently in phase I clinical trials, is unique as the only targeted toxin for pain to undergo human testing.We review the history of SP-SAP and related NK1-receptor targeted toxins. We review animal data on the safety and efficacy of SP-SAP for the treatment of pain in light of the results of NK1 receptor antagonists and knockouts/knockdowns of either SP or the NK1 receptor. Finally, we discuss possible mechanisms of action of SP-SAP.

Original languageEnglish (US)
Title of host publicationMilestones in Drug Therapy
PublisherSpringer Basel
Number of pages24
StatePublished - 2017

Publication series

NameMilestones in Drug Therapy
ISSN (Print)2296-6056


  • Allodynia
  • Hyperalgesia
  • NK1
  • Pain
  • SP-SAP
  • Substance P

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics (miscellaneous)


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