Pharmacokinetics and disposition of the lipid‐lowering drug acifran in normal subjects and in patients with renal failure

  title={Pharmacokinetics and disposition of the lipid‐lowering drug acifran in normal subjects and in patients with renal failure},
  author={Mitchell N. Cayen and Eckhardt S. Ferdinandi and David R. Hicks and Raquel Gonz{\'a}lez and L Cosyns and J. F. Dubuc and M. Kraml and Kathleen D. Edwards},
  journal={Clinical Pharmacology \& Therapeutics},
The pharmacokinetics and metabolic fate of the antihyperlipidemic drug acifran were assessed after a single oral dose of the 14C‐labeled drug to healthy male volunteers. Peak serum acifran and radioactivity concentrations were attained 1 to 2 hours after dosing, and the drug was eliminated with a half‐life of 1.6 hours. Virtually all of the recovered dose was excreted in the urine. All of the serum and urinary radioactivity was caused by unconjugated acifran. In patients with moderate chronic… 
Niacin: a re‐emerging pharmaceutical for the treatment of dyslipidaemia
  • H. Vosper
  • Biology, Medicine
    British journal of pharmacology
  • 2009
The purpose of this review is to emphasize that the search for agonists that show higher tolerability must take into account all aspects of signalling through this receptor.
NMR Studies of Drugs. Applications of Achiral and Chiral Lanthanide Shift Reagents to Acifran Methyl Ester. LSR Binding to a Multifunctional Substrate.
Abstract The antihyperlipoproteinemic agent, acifran, has been studied as its racemic methyl ester, 1, by 60 MHz 1H NMR in CDC13 solution at 28±1° with the added achiral lanthanide shift reagent


The metabolic disposition of acifran, a new antihyperlipidemic agent, in rats and dogs.
The disposition of acifran was similar in rats and dogs; the drug was rapidly absorbed and eliminated, and underwent no detectable biotransformation, and there was no tissue retention and excretion was mainly in the urine.
The metabolic disposition of etodolac in rats, dogs, and man.
It was concluded that, in rats and dogs, etodolac is well absorbed, is subject to extensive enterohepatic circulation, undergoes partial biotransformation, and is excreted primarily into the feces.
Controlled trial of acifran in type II hyperlipoproteinemia
The safety and efficacy demonstrated in this short‐term therapeutic trial justify additional long‐term studies with acifran, and no subject failed to complete the study because of drug intolerance or side effects.
Acifran: a double-blind, randomized, placebo-controlled efficacy study in type IIa hyperlipoproteinemic patients.
In this 12-week study acifran provided safe and effective treatment for Type IIa hyperlipoproteinemia and there was no apparent relationship between changes in plasma lipid concentrations and ac ifran dose or treatment duration.
Effect of AY-25,712 and Other Lipid-Lowering Agents on Liver Catalase and Liver Carnitine Acetyltransferase in Rats 1
The results show that AY-25,712 and nicotinic acid did not induce changes in the livers of rats which are associated with treatment by various other hypolipidemic agents.
Automated reaction-rate method for determination of serum creatinine with the CentrifiChem.
Results of precision studies and correlation with a manual method requiring adsorption of creatinine on ion-exchange resin are reported, and Spectroscopic data suggest that the product of reaction between picrate and Creatinine is a 1:1 adduct of the two starting molecules.