Fab fragments of ovine antibody to colchicine enhance its clearance in the rat

Clin Toxicol (Phila). 2015 Jun;53(5):427-32. doi: 10.3109/15563650.2015.1030026. Epub 2015 Apr 10.

Abstract

Context: Colchicine is an anti-inflammatory alkaloid used for the treatment of acute gout, but has a narrow therapeutic index. Colchicine overdoses are relatively rare, but have high mortality requiring rapid treatment.

Objective: To evaluate the ability of a newly available ovine fragment antigen-binding (Fab) antibody to colchicine (ColchiFab(™)) to protect rats against renal and other injury 24 h after colchicine ingestion.

Materials and methods: Rats were gavaged with colchicine (5 mg/kg), then 2 h later injected intraperitoneally with 5 ml of sterile saline, or Fab anti-colchicine, a newly available ovine antibody to colchicine. Samples of blood were taken at 1, 2, 5 and 24 h after gavage, and urine was collected from 5 to 24 h after gavage. Concentrations of colchicine in tissue, blood and urine were measured by liquid chromatography/mass spectrometry, concentrations of Fab anti-colchicine, urinary neutrophil gelatinase-associated lipocalin (NGAL) and kidney injury molecule-1 or KIM-1 by enzyme-linked immunosorbent assay or ELISA, while concentrations of creatine kinase and creatinine (Cr) were measured enzymatically.

Results: Colchicine equilibrated rapidly throughout the body and increased serum creatine kinase. Fab anti-colchicine also rapidly redistributed to the blood and remained at high concentrations over 24 h. Fab anti-colchicine caused a rapid 7.1-fold increase in serum colchicine level, followed by excretion of both colchicine and Fab anti-colchicine through the urine. This was associated with the accumulation of colchicine in the kidney, a reversal of colchicine-induced diarrhoea, and increasing urinary NGAL level; from 168 ± 48 to 477 ± 255 ng/mmol Cr [mean ± standard deviation or SD].

Discussion: Fab anti-colchicine greatly increased the clearance of colchicine, although increasing NGAL level suggested the presence of mild kidney damage.

Conclusion: These data suggest clinical utility for Fab anti-colchicine in the treatment of colchicine overdose.

Keywords: ColchiFab; Colchicine; Fab antibody; Kidney; NGAL; Urine.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute-Phase Proteins / urine
  • Animals
  • Anti-Inflammatory Agents / blood
  • Anti-Inflammatory Agents / immunology
  • Anti-Inflammatory Agents / pharmacokinetics
  • Anti-Inflammatory Agents / toxicity*
  • Anti-Inflammatory Agents / urine
  • Antidotes / administration & dosage
  • Antidotes / pharmacokinetics
  • Antidotes / pharmacology*
  • Biomarkers / blood
  • Biomarkers / urine
  • Cell Adhesion Molecules / urine
  • Colchicine / blood
  • Colchicine / immunology
  • Colchicine / pharmacokinetics
  • Colchicine / toxicity*
  • Colchicine / urine
  • Creatine Kinase / blood
  • Diarrhea / chemically induced
  • Diarrhea / diagnosis
  • Diarrhea / drug therapy
  • Immunoglobulin Fab Fragments / administration & dosage
  • Immunoglobulin Fab Fragments / blood
  • Immunoglobulin Fab Fragments / pharmacology*
  • Immunoglobulin Fab Fragments / urine
  • Injections, Intraperitoneal
  • Kidney / drug effects
  • Kidney / metabolism
  • Kidney Diseases / chemically induced
  • Kidney Diseases / diagnosis
  • Kidney Diseases / drug therapy
  • Lipocalin-2
  • Lipocalins / urine
  • Liver / drug effects
  • Liver / metabolism
  • Male
  • Metabolic Clearance Rate
  • Poisoning / blood
  • Poisoning / drug therapy*
  • Poisoning / urine
  • Proto-Oncogene Proteins / urine
  • Rats
  • Rats, Sprague-Dawley
  • Renal Elimination / drug effects
  • Sheep
  • Tissue Distribution

Substances

  • Acute-Phase Proteins
  • Anti-Inflammatory Agents
  • Antidotes
  • Biomarkers
  • Cell Adhesion Molecules
  • Havcr1protein, rat
  • Immunoglobulin Fab Fragments
  • Lcn2 protein, rat
  • Lipocalin-2
  • Lipocalins
  • Proto-Oncogene Proteins
  • Creatine Kinase
  • Colchicine