Therapeutic and Prophylactic Vaccines to Counteract Fentanyl Use Disorders and Toxicity

J Med Chem. 2020 Dec 10;63(23):14647-14667. doi: 10.1021/acs.jmedchem.0c01042. Epub 2020 Nov 20.

Abstract

The incidence of fatal overdoses has increased worldwide due to the widespread access to illicit fentanyl and its potent analogues. Vaccines offer a promising strategy to reduce the prevalence of opioid use disorders (OUDs) and to prevent toxicity from accidental and deliberate exposure to fentanyl and its derivatives. This study describes the development and characterization of vaccine formulations consisting of novel fentanyl-based haptens conjugated to carrier proteins. Vaccine efficacy was tested against opioid-induced behavior and toxicity in mice and rats challenged with fentanyl and its analogues. Prophylactic vaccination reduced fentanyl- and sufentanil-induced antinociception, respiratory depression, and bradycardia in mice and rats. Therapeutic vaccination also reduced fentanyl intravenous self-administration in rats. Because of their selectivity, vaccines did not interfere with the pharmacological effects of commonly used anesthetics nor with methadone, naloxone, oxycodone, or heroin. These preclinical data support the translation of vaccines as a viable strategy to counteract fentanyl use disorders and toxicity.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Bacterial Proteins / chemistry
  • Bacterial Proteins / immunology
  • Cattle
  • Diphtheria Toxin / chemistry
  • Diphtheria Toxin / immunology
  • Female
  • Fentanyl / immunology*
  • Haptens / chemistry
  • Haptens / immunology
  • Hemocyanins / chemistry
  • Hemocyanins / immunology
  • Male
  • Mice, Inbred BALB C
  • Opioid-Related Disorders / prevention & control*
  • Opioid-Related Disorders / therapy*
  • Piperidines / chemical synthesis
  • Piperidines / immunology
  • Proof of Concept Study
  • Rats, Sprague-Dawley
  • Serum Albumin, Bovine / chemistry
  • Serum Albumin, Bovine / immunology
  • Sufentanil / immunology
  • Vaccines / immunology*

Substances

  • Bacterial Proteins
  • Diphtheria Toxin
  • Haptens
  • Piperidines
  • Vaccines
  • Serum Albumin, Bovine
  • Hemocyanins
  • Sufentanil
  • keyhole-limpet hemocyanin
  • Fentanyl