Radioimmunoassay of zidovudine: extended use and potential application.

When first approved, the dosing regimens for zidovudine were 1,200-1,500 mg/day; however, because toxicity developed, the daily dose had to be reduced to 500-600 mg/day. At these lower doses, plasma concentrations for a considerable segment of the dosing interval are often below the assay sensitivity for the high-performance liquid chromatography (HPLC) method. Although commonly used, the zidovudine radioimmunoassay has had minimal documentation for the quantitative analysis of clinical samples, especially at current doses. The authors' findings indicate that plasma, urine treated with phosphate buffer, and cerebrospinal fluid samples may be assayed using a commercially available radioimmunoassay. A good correlation was found for clinical samples measured by radioimmunoassay and HPLC (R 2 = 0.85). The greater assay sensitivity, ability to process multiple specimens, and the relatively rapid turnaround time suggest that the zidovudine radioimmunoassay may have an important role in clinical trials evaluating zidovudine pharmacokinetics. This report summarizes the authors' experience with the zidovudine radioimmunoassay and focuses on its potential use in studying the role of therapeutic drug monitoring for zidovudine.