A combination of the metabolic enzyme inhibitor APO866 and the immune adjuvant L-1-methyl tryptophan induces additive antitumor activity

Exp Biol Med (Maywood). 2010 Jul;235(7):869-76. doi: 10.1258/ebm.2010.010001.

Abstract

Many types of malignant cells have a higher nicotinamide adenine dinucleotide (NAD) turnover rate than normal cells, as well as the ability to escape immune responses. Indoleamine 2,3-dioxygenase (IDO) is reported to be a negative immune regulator. Overexpression of IDO in dendritic cells is observed in tumor-draining lymph nodes. IDO-expressing dendritic cells suppress T-cell activation and promote immune tolerance. The nicotinamide phosphoribosyl transferase (NAMPT) inhibitor APO866 (also called FK866 or WK175) selectively inhibits tumor growth through intracellular NAD depletion. The IDO-specific inhibitor L-1-methyl-tryptophan (L-1MT) activates immune responses and reduces tumor volume in murine tumor models. We combined L-1MT and APO866 treatments and tested their antitumor effects in the murine gastric and bladder tumor models. In immune-competent mice, a combination of APO866 and L-1MT had a better therapeutic effect than did either L-1MT or APO866 alone. The intracellular level of NAD was suppressed by APO866 but not L-1MT. However, an additive inhibitory effect on tumor growth was not observed in tumor-bearing immune-deficient mice. The new strategy of combining a metabolic inhibitor and an immune adjuvant induced a potent therapeutic effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylamides / administration & dosage
  • Acrylamides / pharmacology*
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Colonic Neoplasms / drug therapy
  • Drug Synergism
  • Drug Therapy, Combination
  • Female
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / antagonists & inhibitors*
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / metabolism
  • Liver Neoplasms, Experimental / drug therapy
  • Mice
  • Mice, Inbred C3H
  • Mice, Inbred ICR
  • Mice, Inbred NOD
  • Neoplasms, Experimental / drug therapy*
  • Neoplasms, Experimental / enzymology
  • Nicotinamide Phosphoribosyltransferase / antagonists & inhibitors*
  • Nicotinamide Phosphoribosyltransferase / metabolism
  • Piperidines / administration & dosage
  • Piperidines / pharmacology*
  • Tryptophan / administration & dosage
  • Tryptophan / analogs & derivatives*
  • Tryptophan / pharmacology
  • Urinary Bladder Neoplasms / drug therapy

Substances

  • Acrylamides
  • Antineoplastic Agents
  • Indoleamine-Pyrrole 2,3,-Dioxygenase
  • N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
  • Piperidines
  • Tryptophan
  • Nicotinamide Phosphoribosyltransferase
  • 1-methyltryptophan