Serum and urine concentrations of oral bromovinyldeoxyuridine in humans as monitored by a bioassay system based on varicella‐zoster virus focus inhibition

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Abstract
A simple and sensitive bioassay method for measuring (E)‐5‐(2‐bromovinyl)‐2′‐deoxyuridine (BVDU) concentrations in human serum and urine has been established. This method is based on the inhibitory effect of BVDU on varicella‐zoster virus (VZV) focus formation in vitro. The minimal concentration of BVDU that could be detected in serum by this method was 0.2 μg/ml. Following a single oral administration of 250 mg BVDU, serum BVDU concentrations of 1.2‐2.2 μg/ml were attained 1 hr later; at 5 and 7 hr, serum BVDU levels were below 0.2 μg/ml. Upon repeated administration of 125 mg BVDU at 8 hr intervals, the serum BVDU concentrations reached 0.7‐1.1 μg/ml at 2 hr after the fourth administration. These concentrations are approximately 300‐‐450‐fold higher than the 50% inhibitory dose of BVDU for VZV in vitro. Urinary BVDU concentrations were on average 10 to 20 times higher than the serum BVDU concentrations.