Determination of MK-383, a non-peptide fibrinogen receptor antagonist, in human plasma and urine by radioimmunoassay.
MK-383 is a novel, non-peptide fibrinogen receptor antagonist. A sensitive and specific radioimmunoassay has been developed for the determination of this drug candidate in plasma and urine. The immunogen was prepared by coupling to albumin via the N-hydroxysuccinimide ester from which the radioligand was also prepared by reaction with [I125]iodotyrosine. The method was specific and no immunoreactive material other than the parent drug was detectable in plasma and urine from dosed volunteers. This direct assay, using 5 microliters of plasma or 0.5 microliter of urine, is sensitive to 1 and 10 ng ml-1, respectively, without matrix interference and has sufficient sensitivity, specificity, accuracy, and precision for the analysis of clinical samples.
Hand
E L
EL
Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486.
Gilbert
J D
JD
Yuan
A S
AS
Olah
T V
TV
Hichens
M
M
D000818:Animals; D000918:Antibody Specificity; D005260:Female; D005343:Fibrinolytic Agents / Q000097:blood* / Q000276:immunology / Q000652:urine*; D006493:Heparin / Q000737:chemistry; D006801:Humans; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors*; D011817:Rabbits / Q000276:immunology; D011863:Radioimmunoassay; D000077466:Tirofiban; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000097:blood / Q000276:immunology / Q000652:urine
D005343:Fibrinolytic Agents; D007457:Iodine Radioisotopes; D010980:Platelet Membrane Glycoproteins; D014443:Tyrosine; D006493:Heparin; D000077466:Tirofiban