PMID: 7535991Dec 1, 1994Paper

In vitro protein-binding characteristics of atevirdine and its N-dealkylated metabolite

Antiviral Research
L M RosserG Morse

Abstract

The in vitro protein-binding characteristics of atevirdine (ATV), a non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, and its N-dealkylated metabolite (N-ATV) were studied using equilibrium dialysis. ATV and N-ATV were studied at concentrations of 5, 10, 20, and 30 microM in five protein-containing solutions [albumin 4%, plasma, serum, immune globulin (IgG) 1.5%, alpha 1-acid glycoprotein (AAG)] for 5 h at 37 degrees C. All samples were analyzed by high-performance liquid chromatography. The free fraction of atevirdine in plasma, albumin, and serum was 0.01-0.02 over the range of drug concentrations studied. The fraction unbound (fu) in these protein solutions statistically differed from IgG and AAG (P < 0.05), where the fraction unbound averaged 0.96 and 0.53, respectively. N-ATV had a similar binding profile as ATV with a fraction unbound of 0.04, 0.03, 0.03 in albumin, plasma and serum, respectively. A difference existed in N-ATV binding when compared to IgG and AAG with an average fu of 0.87 and 0.59 (P < 0.05 vs. plasma). The potential clinical implications of the high degree of protein binding for ATV and N-ATV are discussed.

References

Jun 1, 1984·Journal of Pharmaceutical Sciences·F D Boudinot, W J Jusko
Jan 1, 1984·Clinical Pharmacokinetics·R H Levy, T A Moreland

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Citations

Jun 6, 2000·Advanced Drug Delivery Reviews·X Li, W K Chan
Aug 10, 2001·Drug Metabolism Reviews·Z H Israili, P G Dayton
Nov 17, 2004·Reviews in Medical Virology·Nathalie Strazielle, Jean-François Ghersi-Egea
Mar 1, 1996·Antimicrobial Agents and Chemotherapy·G D MorseC P Wajszczuk

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