Human pharmacokinetics of 1-[2-[2-(4 pyridyl)-2-imidazolinyl-(1)]-ethyl]-3-(4-carboxyphenyl) urea (CGP 15720A).

Pharmacokinetics of CGP 15720A have been studied in patients receiving this drug in a short I.V. infusion during its phase I clinical trial. Plasma decay was biphasic with a mean t1/2 beta of 4.9 +/- 2.47h. The drug was cleared rapidly from plasma (7.02 +/- 5.95 L/h). Renal clearance (4.13 +/- 1.65 L/h) appears to be the major clearance pathway. The steady state volumes of distribution of the drug indicate limited tissue distribution for the drug. Studies with plasma and urine of patients receiving 14[C] GCP 15720A indicate that the drug is not metabolized. CGP 15720A could be measured in cerebrospinal fluid.