Characterizing biopersistence potential of the metabolite 5:3 fluorotelomer carboxylic acid after repeated oral exposure to the 6:2 fluorotelomer alcohol

Toxicol Appl Pharmacol. 2020 Feb 1:388:114878. doi: 10.1016/j.taap.2020.114878. Epub 2020 Jan 7.

Abstract

Our previous report on pharmacokinetic (PK) evaluation of 6:2 fluorotelomer alcohol (6:2 FTOH) examined the biopersistence potential of its metabolites based on data published from single inhalation and occupational 6:2 FTOH exposure studies. We calculated internal exposure estimates of three key metabolites of 6:2 FTOH, of which 5:3 fluorotelomer carboxylic acid (5:3 acid) had the highest internal exposure and the slowest clearance. No oral repeated 6:2 FTOH exposure data were available at the time to fully characterize the biopersistence potential of the metabolite 5:3 acid. We recently received additional data on 6:2 FTOH and 5:3 acid, which included a 90-day toxicokinetic study report on repeated oral 6:2 FTOH exposure to rats. We reviewed the study and analyzed the reported 5:3 acid concentrations in plasma, liver, and fat using one-compartment PK modeling and calculated elimination rate constants (kel), elimination half-lives (t1/2) and times to steady state (tss) of 5:3 acid at three 6:2 FTOH doses. Our results showed that tss of 5:3 acid in plasma and evaluated tissues were approximately close to 1 year, such that the majority of highest values were observed at the lowest 6:2 FTOH dose, indicating its association with the biopersistence of 6:2 FTOH. The results of our PK analysis are the first to characterize biopersistence potential of the 5:3 acid after repeated oral exposure to the parent compound 6:2 FTOH based on steady state PK parameters, and therefore, may have an impact on future study designs when conducting toxicity assays for such compounds.

Keywords: 5:3 acid; 6:2 fluorotelomer alcohol; Biopersistence; Elimination half-life; Elimination rate constant; Pharmacokinetics; Time to steady state.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipose Tissue / chemistry
  • Adipose Tissue / drug effects
  • Administration, Oral
  • Animals
  • Female
  • Fluorocarbon Polymers / administration & dosage
  • Fluorocarbon Polymers / analysis
  • Fluorocarbon Polymers / pharmacokinetics*
  • Fluorocarbon Polymers / toxicity
  • Half-Life
  • Liver / chemistry
  • Liver / drug effects
  • Male
  • Metabolic Clearance Rate
  • Rats
  • Research Design
  • Time Factors
  • Toxicity Tests, Chronic / methods

Substances

  • Fluorocarbon Polymers